연구용
Rimonabant (SR141716) Cannabinoid Receptor 길항제
제품 번호S3021
화학 구조
분자량: 463.79
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품질 관리
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순도:
99.67%
99.67
세포 배양, 처리 및 작업 농도
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| CHO cells | Function assay | Ability to displace [3H]-SR- 141716A binding to human CB1 receptor expressed in CHO cell membranes, Ki=8.9 nM | 10465552 | |||
| CHO | Function assay | Antagonistic activity towards cannabinoid receptor 1 expressed as [3H]Arachidonic acid release in CHO cells, Kd=0.002512μM | 14736243 | |||
| CHO | Function assay | Displacement of CP-55940 binding from recombinant human cannabinoid receptor 1 expressed in CHO cells, Ki=0.025μM | 14736243 | |||
| CHO | Function assay | Affinity to displace CP-55940 binding from Cannabinoid receptor 2 of human expressed in CHO cells, Ki=1.58μM | 14736243 | |||
| CHO | Function assay | Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells, IC50=0.006μM | 15713403 | |||
| CHO | Function assay | In vitro cannabinoid receptor 1 antagonism of [3H]arachidonic acid release by CHO cells, Kd=0.002512μM | 15771428 | |||
| CHO | Function assay | In vitro displacement of CP-55940 binding to human CB1 receptor expressed in CHO cells, Ki=0.025μM | 15771428 | |||
| CHO | Function assay | In vitro displacement of CP-55940 binding to human CB2 receptor expressed in CHO cells, Ki=1.58μM | 15771428 | |||
| CHO | Function assay | Inhibition of [3H]SR-141,716A binding to human CB1 receptor expressed in CHO cells, Ki=0.0054μM | 15801840 | |||
| CHO | Function assay | Antagonistic activity against cannabinoid receptor 1 measured by CP-55940 induced arachnoid acid release in CHO cells, Kd=0.002512μM | 16140010 | |||
| CHO | Function assay | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 1, Ki=0.025μM | 16140010 | |||
| CHO | Function assay | Displacement of specific CP-55940 binding in CHO cells stably transfected with human cannabinoid receptor 2, Ki=1.58μM | 16140010 | |||
| CHOK1 | Function assay | Functional activity at human CB1 receptor transfected in CHOK1 cells by [35SGTP]gammaS assay, Ki=0.001μM | 16263283 | |||
| HEK293 | Function assay | Displacement of [3H]SR-141716 from human CB1 receptor transfected in HEK293 cells, Ki=0.0021μM | 16263283 | |||
| CHO | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0054μM | 16279809 | |||
| HEK293 | Function assay | Displacement of [3H]SR-141716 from human CB1 receptor expressed in HEK293 cells, Kd=0.0018μM | 17004712 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0071μM | 17004712 | |||
| HEK293 | Function assay | Displacement of [3H]WIN-55212-2 from human CB1 receptor expressed in HEK293 cells, Ki=0.018μM | 17004712 | |||
| CHO | Function assay | Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells, IC50=0.0061μM | 17181138 | |||
| CHO | Function assay | Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells, IC50=0.6μM | 17181138 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells, IC50=0.0061μM | 17293109 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells, IC50=0.6033μM | 17293109 | |||
| HEK293 | Function assay | Displacement of [3H]CP-559440 from human CB1 receptor expressed in HEK293 cells, Ki=0.0011μM | 17383180 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.016μM | 17942307 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=1.64μM | 17942307 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.047μM | 17979261 | |||
| CHOK1 | Function assay | Displacement of [3H]WIN-552122 from human recombinant CB2 receptor expressed in CHOK1 cells, Ki=1.99μM | 17979261 | |||
| HEK293 | Function assay | Displacement of radioligand from human CB1 receptor expressed in HEK293 cells, Ki=0.0018μM | 18083560 | |||
| HEK293 EBNA | Function assay | Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay, EC50=0.004μM | 18083560 | |||
| HEK293 | Function assay | Displacement of radioligand from human CB2 receptor expressed in HEK293 cells, Ki=0.554μM | 18083560 | |||
| CHOK1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay, IC50=0.12μM | 18243711 | |||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM | 18243711 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 18293908 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 18293908 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells, Ki=0.006μM | 18335976 | |||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells, IC50=1.76μM | 18337096 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM | 18342403 | |||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, Ki=1.58μM | 18342403 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.0024μM | 18363352 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=0.56μM | 18363352 | |||
| SF9 | Function assay | Antagonist activity at rat CB1 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00031μM | 18448340 | |||
| SF9 | Function assay | Antagonist activity at human CB1 receptor expressed in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.00043μM | 18448340 | |||
| SF9 | Function assay | Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level, IC50=0.00135μM | 18448340 | |||
| SF9 | Function assay | Antagonist activity at human CB2 receptor in SF9 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, Ki=0.815μM | 18448340 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 form human recombinant CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.04μM | 18511157 | |||
| CHO-K1 | Function assay | Displacement of [3H]SR141716 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.00118μM | 18512901 | |||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated [35S]GTPgammaS binding, Kd=0.00257μM | 18512901 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM | 18512901 | |||
| CHO-K1 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM | 18512901 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.008μM | 18579386 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 18579386 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.012μM | 18680276 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, Ki=0.79μM | 18680276 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM | 18712856 | |||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM | 18712856 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=1.9398μM | 18712856 | |||
| HEK293 | Function assay | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as decrease in [35S]gammaGTP binding relative to control | 18712856 | |||
| CHO | Function assay | Antagonist activity at human CB1 receptor in CHO cells assessed as GTPgammaS binding, Kb=0.000698μM | 18800770 | |||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM | 18954042 | |||
| CHO | Function assay | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells, IC50=1.76μM | 19022666 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells, IC50=0.0019μM | 19095444 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells, IC50=0.015μM | 19095444 | |||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding, EC50=0.0182μM | 19095444 | |||
| CHO-K1 | Function assay | Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay, Ki=0.00019μM | 19102698 | |||
| HEK293 | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells, Ki=0.0009μM | 19102698 | |||
| CHOK1 | Function assay | Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry, IC50=1.76μM | 19269817 | |||
| CHOK1 | Function assay | Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=0.24μM | 19328683 | |||
| CHOK1 | Function assay | Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity, EC50=31.21μM | 19328683 | |||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human recombinant CB1 receptor expressed in HEK293 cells, Ki=0.001995μM | 19338356 | |||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human recombinant CB2 receptor expressed in HEK293 cells, Ki=0.39811μM | 19338356 | |||
| CHOK1 | Function assay | 10 mins | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay, Ki=0.0016μM | 19351113 | ||
| HEK293 | Function assay | Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting, Ki=0.0019μM | 19520572 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells, IC50=0.0132μM | 19530697 | |||
| HEK293 | Function assay | Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding, EC50=0.0157μM | 19530697 | |||
| HEK293 | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells, IC50=1.6311μM | 19530697 | |||
| HEK293 | Function assay | 10 uM | Intrinsic activity at human recombinant CB1R expressed in HEK293 cells assessed as Eu-GTP binding at 10 uM relative to basal level | 19530697 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 19595596 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 19595596 | |||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor transfected in CHO-K1cells by GTPgamma[35S] binding assay, Ki=0.0016μM | 19683918 | |||
| CHO | Function assay | Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.0925μM | 19850473 | |||
| CHOK1 | Function assay | Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells, IC50=1.76μM | 19850473 | |||
| CHO-K1 | Function assay | Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding, IC50=0.0045μM | 19954978 | |||
| CHO-K1 | Function assay | Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay, IC50=0.0029μM | 20015647 | |||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding, IC50=0.0045μM | 20015647 | |||
| COS7 | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells, IC50=0.0051μM | 20015647 | |||
| CHO | Function assay | Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay, IC50=0.108μM | 20045337 | |||
| CHO | Function assay | 60 mins | Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins, EC50=0.00011μM | 20047779 | ||
| CHO | Function assay | 3 hrs | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.00074μM | 20047779 | ||
| CHO | Function assay | 10 mins | Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader, IC50=0.0032μM | 20047779 | ||
| CHO | Function assay | 3 hrs | Displacement of [3H]CP-55940 from human recombinant cannabinoid CB2 receptor expressed in CHO cells after 3 hrs by liquid scintillation counting, Ki=0.126μM | 20047779 | ||
| CHO | Function assay | Antagonist activity at human CB1 receptor expressed in CHO cells assessed as inhibition of CP-55940-induced [3H]arachidonic acid release, Kd=0.002512μM | 20363132 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells, Ki=0.025μM | 20363132 | |||
| CHO | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO cells, Ki=1.58μM | 20363132 | |||
| CHO-K1 | Function assay | 1 hr | Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting, IC50=1.76μM | 20673729 | ||
| HEK | Function assay | Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK cells, Ki=0.012μM | 20718492 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK cells, Ki=0.79μM | 20718492 | |||
| CHO | Function assay | Agonist activity at human CB1 receptor expressed in CHO cells co-expressing Galpha16 protein assessed as mobilization of intracellular calcium, Ke=0.0011μM | 20845959 | |||
| HEK293 | Function assay | Displacement of [3H]SR141716 from human CB1 receptor expressed in HEK293 cells, Ki=0.00118μM | 20845959 | |||
| HEK293 | Function assay | Displacement of [3H]CP55940 from human CB1 receptor expressed in HEK293 cells, Ki=0.00618μM | 20845959 | |||
| CHOK1 | Function assay | Displacement of [3H]CP55940 from human CB2 receptor expressed in CHOK1 cells, Ki=0.313μM | 20845959 | |||
| HEK | Function assay | Displacement of [3H]CP-55,940 from recombinant human CB1 receptor transfected in HEK cells, Ki=0.012μM | 20943290 | |||
| HEK | Function assay | Displacement of [3H]CP-55,940 from recombinant human CB2 receptor transfected in HEK cells, Ki=0.79μM | 20943290 | |||
| CHO | Function assay | Displacement of [3H]SR141716A from human CB1 receptor expressed in CHO cells, Ki=0.0009333μM | 21334892 | |||
| Sf9 | Function assay | Displacement of [3H]CP55940 from human recombinant CB2 receptor expressed in Sf9 cells, Ki=0.85114μM | 21334892 | |||
| CHO | Function assay | Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay, IC50=0.004μM | 21376588 | |||
| HEK293 | Function assay | Noncompetitive inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells by Dixon plot, Ki=1.4μM | 21511945 | |||
| HEK293 | Function assay | Noncompetitive inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells by Dixon plot, Ki=4μM | 21511945 | |||
| HEK293 | Function assay | Induction of MRP2-mediated E2-17betaG transport in human MRP2 expressing HEK293 cells in presence of 2 uM E2-17betaG | 21511945 | |||
| HEK293 | Function assay | Inhibition of MRP3-mediated E2-17betaG transport in human MRP3 expressing HEK293 cells in presence of 15 uM E2-17betaG | 21511945 | |||
| HEK293 | Function assay | Inhibition of MRP1-mediated E2-17betaG transport in human MRP1 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG | 21511945 | |||
| HEK293 | Function assay | Inhibition of MRP4-mediated E2-17betaG transport in human MRP4 expressing HEK293 cells in presence of 0.6 to 5 uM E2-17betaG | 21511945 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells, Ki=0.012μM | 21702498 | |||
| HEK | Function assay | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells, Ki=0.79μM | 21702498 | |||
| CHO | Function assay | 1 hr | Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting, IC50=1.98μM | 21741835 | ||
| HEK293 | Function assay | 5 mins | Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay, IC50=2.79μM | 21741835 | ||
| CHO | Function assay | 90 mins | Displacement of [3H]BMS-725519 from human CB1 receptor expressed in CHO cells after 90 mins by scintillation counting, Ki=0.00073μM | 21962575 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells co-expressing Galphaq16 assessed as inhibition of CP55940-induced intracellular calcium mobilization by fluorometry, Ke=0.0011μM | 22372835 | |||
| CHO-K1 | Function assay | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO-K1 cells, Ki=0.0062μM | 22372835 | |||
| CHO-K1 | Function assay | Displacement of [3H]CP55940 from CB2 receptor expressed in CHO-K1 cells, Ki=0.313μM | 22372835 | |||
| HEK | Function assay | Displacement of [3H]CP-55,940 from human recombinant CB1 receptor transfected in HEK cells, Ki=0.012μM | 22548457 | |||
| HEK | Function assay | Displacement of [3H]CP-55,940 from human recombinant CB2 receptor transfected in HEK cells, Ki=0.79μM | 22548457 | |||
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.0126μM | 22916707 | ||
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counter, Ki=0.9μM | 22916707 | ||
| CHO | Function assay | Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level, IC50=0.051μM | 22959249 | |||
| CHO | Function assay | 1 hr | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHO cells incubated for 1 hr, Ki=0.0106μM | 23072339 | ||
| CHO | Function assay | > 0.1 nM | 1 hr | Inverse agonist activity at human recombinant CB1 receptor transfected in CHO cells assessed as reduction of [35S]GTPgammaS binding at > 0.1 nM after 1 hr by liquid scintillation spectrometry | 23357307 | |
| N1E-115 | Function assay | 1 uM | 5 mins | Inverse agonist activity at CB1 receptor in mouse N1E-115 cells assessed as inhibition of WIN 55,212-2-induced ERK1/2 phosphorylation at 1 uM treated 5 mins prior to WIN 55,212-2 challenge by Western blot analysis | 23357307 | |
| CHO | Function assay | Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay, IC50=10.1μM | 23679955 | |||
| HEK | Function assay | 1 hr | Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis, EC50=0.0015μM | 24175572 | ||
| CHOK1 | Function assay | 1 hr | Displacement of [3H]CP55940 from human CB1 receptor expressed in CHOK1 cells after 1 hr by liquid scintillation counting analysis, Ki=0.0059μM | 24175572 | ||
| CHO | Function assay | 45 mins | Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=0.013μM | 24445310 | ||
| CHO | Function assay | 45 mins | Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay, IC50=9.8μM | 24445310 | ||
| CHO-K1 | Function assay | 10 mins | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting, Ki=0.0016μM | 24900484 | ||
| HEK293 | Function assay | 60 mins | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting, Ki=0.0018μM | 24900484 | ||
| CHO-K1 | Function assay | 60 mins | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting, Ki=0.522μM | 24900484 | ||
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from recombinant human CB1 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.0126μM | 24900561 | ||
| CHO | Function assay | 2 hrs | Displacement of [3H]CP55,940 from recombinant human CB2 receptor expressed in CHO cells after 2 hrs by liquid scintillation counting, Ki=0.9μM | 24900561 | ||
| CHO | Function assay | 90 mins | Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay, EC50=2.01μM | 24900561 | ||
| RD-HGA16 | Function assay | Antagonist activity at CB1-OX1 heterodimer (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of orexin A-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.001μM | 24944734 | |||
| RD-HGA16 | Function assay | Antagonist activity at CB1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as inhibition of CP55940-induced calcium mobilization by fluorometric imaging plate reader analysis, Ke=0.0011μM | 24944734 | |||
| Sf9 | Function assay | 20 mins | Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05μM | 25096297 | ||
| Sf9 | Function assay | 20 mins | Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay, EC50=0.05012μM | 25096297 | ||
| CHO | Function assay | Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=0.0135μM | 26151231 | |||
| CHO | Function assay | Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay, IC50=9.1μM | 26151231 | |||
| HEK293 | Function assay | Immediate antagonist/Inverse agonist activity at hemagglutinin-tagged human CB1 receptor expressed in HEK293 cells assessed as reversal of 1 uM CP55,940-induced inhibition of 5 uM forskolin-induced cAMP accumulation by kinetic cAMP assay | 26203658 | |||
| HEK293 | Function assay | 90 mins | Displacement of [3H]-CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.012μM | 26756097 | ||
| HEK293 | Function assay | 90 mins | Displacement of [3H]-CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells after 90 mins by Competition binding assay, Kieq=0.79μM | 26756097 | ||
| CHO-K1 | Function assay | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP55940-induced intracellular calcium mobilization by Calcein-4 AM-staining based FLIPR assay, Ke=0.0011μM | 26827137 | |||
| CHO | Function assay | 90 secs | Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay, EC50=0.005μM | 26827137 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| CHOK1 | Function assay | 90 mins | Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay, EC50=0.015μM | 29939744 | ||
| HEK293 | Function assay | Antagonist activity at human CB1 receptor expressed in HEK293 cells by GTPgammaS binding assay, Ke=0.0002μM | 30077609 | |||
| HEK293 | Function assay | 90 secs | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells co-expressing Galphaq16 assessed as inhibition of calcium mobilization after 90 secs by calcein-4 AAM dye-based FLIPR assay, EC50=0.586μM | 30077609 | ||
| HEK293 | Function assay | 30 mins | Inverse agonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by HTRF assay, EC50=0.0041μM | 30339387 | ||
| CHO | Function assay | Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in CHO cells by radioligand binding assay, Ki=0.143μM | 31609608 | |||
| CHO | Function assay | Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=2.01μM | ChEMBL | |||
| CHO | Function assay | Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method, EC50=10.1μM | ChEMBL | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성
| 분자량 | 463.79 | 화학식 | C22H21Cl3N4O |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 168273-06-1 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | N/A | Smiles | CC1=C(N(N=C1C(=O)NN2CCCCC2)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)Cl | ||
용해도
|
In vitro |
DMSO
: 92 mg/mL
(198.36 mM)
Ethanol : 50 mg/mL Water : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘
| 특징 |
Efficacious to induce weight reduction and improvements in cardiometabolic risk factors, however was withdrawn in 2009 due to severe depressive disorder and anxiety.
|
|---|---|
| Targets/IC50/Ki |
ACAT1
ACAT2
MmpL3
hCB1
(Cell-free assay) 13.6 nM
hCB2
(Cell-free assay) 1.64 μM
|
| 시험관 내(In vitro) |
Rimonabant (SR141716)는 Raw264.7 대식세포에서 IC50 2.9 μM 및 분리된 복막 대식세포에서 ACAT 활성을 용량 의존적으로 감소시킵니다. 이는 온전한 CHO-ACAT1 및 CHO-ACAT2 세포와 무세포 분석에서 거의 동일한 효율로 ACAT 활성을 억제하며, CHO-ACAT1 및 CHO-ACAT2에 대해 각각 1.5 μM 및 2.2 μM의 IC50을 갖습니다. ACAT 억제와 일치하게, 이 화합물 처리는 대식세포에서 ACAT 의존성 과정, 옥시스테롤 유도 세포 사멸 및 아세틸화-LDL 유도 거품 세포 형성을 차단합니다. 이는 마우스 정관 수축 및 쥐 뇌막의 아데닐산 고리화효소 활성 모두에 대한 Cannabinoid Receptor 작용제의 억제 효과를 농도 의존적으로 길항합니다. 이 화합물은 인간 대장암 세포(DLD-1, CaCo-2 및 SW620)의 세포 성장을 유의하게 감소시키고 세포 사멸을 유도합니다. 이는 테스트된 모든 세포주에서 세포 주기 분포를 변경할 수 있습니다. 특히, Rimonabant는 세포 사멸 또는 괴사를 유도하지 않고 DLD-1 세포에서 G2/M 세포 주기 정지를 유발합니다. |
| 키나아제 분석 |
방사성 리간드 결합 분석
|
|
인간 CB1 및 CB2가 안정적으로 형질감염된 HEK 293 세포와 세포막이 정제됩니다. 정제된 막 0.2-8 μg를 배양 버퍼(50 mM Tris-HCl, 5 mM MgCl2, 1 mM EDTA, 0.3% BSA, pH 7.4)에서 0.75 nM [3H] CP55,940 및 Rimonabant (SR141716)와 함께 배양합니다. 비특이적 결합은 1 μM CP55,940 존재하에 정의됩니다. 반응은 Multiscreen에서 30 °C에서 1시간 30분 동안 배양됩니다. 반응은 매니폴드 여과로 종료되고 얼음처럼 차가운 세척 버퍼(50mM Tris, pH 7.4, 0.25% BSA)로 4회 세척됩니다. 필터에 결합된 방사능은 Topcount로 측정됩니다. IC50은 [3H] CP55,940의 결합을 50% 억제하는 데 필요한 이 화합물의 농도로 결정되며 비선형 회귀 분석으로 계산됩니다.
|
|
| 생체 내(In vivo) |
Rimonabant (SR141716)는 복강 내 또는 경구 투여되며 Cannabinoid Receptor 작용제의 고전적인 약리학적 및 행동적 효과를 강력하고 용량 의존적으로 길항합니다. 아족시메탄 유발 결장 발암의 마우스 모델에서, 이는 대장암에 선행하는 비정상적인 선와 초점(ACF) 형성을 유의하게 감소시켰습니다. 이 화합물(10 mg/kg 경구 투여)은 포도당 내성 손상 모델로서 3개월령 수컷 비만 Zucker 쥐에게 2주 동안 투여되었고, 대사 증후군 모델로서 6개월령 수컷 비만 Zucker 쥐에게 10주 동안 투여되었습니다. RANTES (Regulated upon Activation, Normal T cell Expressed, and Secreted) 및 MCP-1 (monocyte chemotactic protein-1) 혈청 수치는 마른 쥐에 비해 비만 Zucker 쥐에서 증가했으며, 장기 치료에 의해 유의하게 감소하여 대사 증후군 쥐의 체중 증가를 늦춥니다. 호중구와 단핵구는 마른 쥐에 비해 어린 및 늙은 비만 Zucker 쥐에서 유의하게 증가했으며 이 화합물에 의해 감소했습니다. 혈소판 결합 피브리노겐은 양쪽 연령의 마른 쥐에 비해 비만 Zucker 쥐에서 유의하게 증가했으며 이 화합물에 의해 감소했습니다. 비만 쥐의 혈소판은 트롬빈 유발 응집 및 피브리노겐에 대한 부착에 더 민감하며, 이들 모두는 Rimonabant 요법에 의해 약화되었습니다. |
참조 |
|
적용 분야
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | CD44 / Lgr5 / CD133 / EpCAM β-catenin p-LRP6 / LRP6 / Lgr5 |
|
29354056 |
| Immunofluorescence | β-catenin Lgr5 |
|
29354056 |
임상시험 정보
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT00750347 | Completed | Pain |
University Hospital Clermont-Ferrand |
September 2008 | Phase 1 |
| NCT00656487 | Completed | Cannabis Dependence|Cannabis Withdrawal |
The Scripps Research Institute|National Institute on Drug Abuse (NIDA) |
April 30 2008 | Phase 2 |
| NCT00546325 | Completed | Diabetes Mellitus Type 2 |
Sanofi |
October 2007 | Phase 3 |
| NCT00525681 | Completed | Renal Transplantation |
University of Oslo School of Pharmacy |
September 2007 | Phase 4 |
| NCT00584389 | Terminated | Obesity |
University of Surrey|European Foundation for the Study of Diabetes|Royal Surrey County Hospital NHS Foundation Trust |
July 2007 | Phase 4 |
| NCT01041170 | Completed | Cannabis|Dependence |
National Institute on Drug Abuse (NIDA)|National Institutes of Health Clinical Center (CC) |
April 16 2006 | Phase 1 |
기술 지원
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