연구용

GSK269962A HCl ROCK 억제제

제품 번호S7687

GSK269962A HCl은 ROCK1과 ROCK2에 대해 각각 1.6 및 4 nM의 IC50 값을 갖는 선택적 ROCK(Rho-associated protein kinase) 억제제입니다.
GSK269962A HCl ROCK 억제제 Chemical Structure

화학 구조

분자량: 607.06

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품질 관리

배치: 순도: 99.59%
99.59

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=18.8477 μM
NCI-H1694 Growth inhibition assay Inhibition of human NCI-H1694 cell growth in a cell viability assay, IC50=24.8749 μM
NCI-H1963 Growth inhibition assay Inhibition of human NCI-H1963 cell growth in a cell viability assay, IC50=1.27839 μM
NCI-H2081 Growth inhibition assay Inhibition of human NCI-H2081 cell growth in a cell viability assay, IC50=34.6044 μM
NCI-H209 Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=22.6272 μM
NCI-H2107 Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=25.6561 μM
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=6.50426 μM
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=0.95937 μM
NCI-H2227 Growth inhibition assay Inhibition of human NCI-H2227 cell growth in a cell viability assay, IC50=7.88616 μM
NCI-H524 Growth inhibition assay Inhibition of human NCI-H524 cell growth in a cell viability assay, IC50=22.8763 μM
NCI-H526 Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=18.5431 μM
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=2.45161 μM
NMC-G1 Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50=15.0578 μM
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.82294 μM
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=10.9496 μM
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=17.201 μM
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=13.9191 μM
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=46.195 μM
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50=8.71808 μM
P30-OHK cell Growth inhibition assay Inhibition of human P30-OHK cell growth in a cell viability assay, IC50=7.62877 μM
P30-OHK cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=7.04954 μM
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=6.22126 μM
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=0.49004 μM
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50=18.9036 μM
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=10.5662 μM
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=10.67 μM
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=18.5236 μM
RPMI-8402 cell Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=4.5856 μM
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay, IC50=0.393 μM
Ramos-2G6-4C10 cell Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=1.357 μM
SCLC-21H cell Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=7.61149 μM
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=11.8321μM
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=6.23183 μM
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=1.28661 μM
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=5.75508 μM
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=11.7259 μM
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.04526 μM
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay, IC50=32.5965 μM
SK-MM-2 cell Growth inhibition assay Inhibition of human SK-MM-2 cell growth in a cell viability assay, IC50=42.3405 μM
SK-N-DZ cell Growth inhibition assay Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.48314 μM
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=17.5456 μM
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=24.9736 μM
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay, IC50=8.07737 μM
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=0.000137 μM
SU-DHL-1 cell Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=12.7336 μM
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay, IC50=39.011 μM
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.88656 μM
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay, IC50=12.7521 μM
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.2991 μM
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=23.0793 μM
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=1.87034 μM
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=21.4387 μM
AM-38 cell Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=7.26327 μM
ATN-1 cell Growth inhibition assay Inhibition of human ATN-1 cell growth in a cell viability assay, IC50=24.7555 μM
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=22.2532 μM
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.00789 μM
human BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=3.97107 μM
BE-13 cell Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.14081μM
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=3.40703 μM
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=18.8859 μM
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=13.9545 μM
CAL-148 cell Growth inhibition assay Inhibition of human CAL-148 cell growth in a cell viability assay, IC50=35.6557 μM
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay, IC50=22.8423 μM
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=32.4114 μM
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=11.6089 μM
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=36.6381 μM
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50=23.3577 μM
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=8.70625 μM
WSU-NHL cell Growth inhibition assay Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=27.1907 μM
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=0.66846 μM
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay, IC50=47.0263 μM
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=0.847 μM
CCRF-CEM cell Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=8.65392 μM
CMK cell Growth inhibition assay Inhibition of human CMK cell growth in a cell viability assay, IC50=1.01323 μM
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=3.24226 μM
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=2.0738 μM
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=36.5497 μM
CRO-AP2 cell Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=2.36088 μM
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=23.9145 μM
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=47.586 μM
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=0.62814 μM
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=0.08509 μM
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=0.62854 μM
D-392MG cell Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=1.43039 μM
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=8.53492 μM
D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=12.3152 μM
DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=47.1417 μM
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=7.01898 μM
DMS-114 cell Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=49.8468 μM
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay, IC50=42.9923 μM
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=4.22764 μM
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=8.43623 μM
Daudi cell Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=2.09802 μM
EC-GI-10 cell Growth inhibition assay Inhibition of human EC-GI-10 cell growth in a cell viability assay, IC50=44.2589 μM
ECC4 cell Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=32.1896 μM
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=2.45594 μM
ES1 cell Growth inhibition assay Inhibition of human ES1 cell growth in a cell viability assay, IC50=5.54087 μM
ES3 cell Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=42.4729 μM
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay, IC50=35.195 μM
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=0.24733 μM
ES7 cell Growth inhibition assay Inhibition of human ES7 cell growth in a cell viability assay, IC50=5.23124 μM
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=0.81924 μM
EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=13.6759 μM
EW-22 cell Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=47.7947 μM
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay, IC50=9.80389 μM
GDM-1 cell Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=8.39196 μM
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=0.00523 μM
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=0.04951 μM
GR-ST cell Growth inhibition assay Inhibition of human GR-ST cell growth in a cell viability assay, IC50=13.7902 μM
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay, IC50=1.60389 μM
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=6.69712 μM
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=37.6011 μM
HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=13.3834 μM
HD-MY-Z cell Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=25.2146 μM
HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=12.2114 μM
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=23.9527 μM
HT cell Growth inhibition assay Inhibition of human HT cell growth in a cell viability assay, IC50=4.44321 μM
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=4.90686 μM
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=3.78986 μM
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=32.9086 μM
IST-SL1 cell Growth inhibition assay Inhibition of human IST-SL1 cell growth in a cell viability assay, IC50=2.17079 μM
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=3.26608 μM
K052 cell Growth inhibition assay Inhibition of human K052 cell growth in a cell viability assay, IC50=0.75301 μM
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=33.5915 μM
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=29.3969 μM
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=42.9142 μM
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=4.11247 μM
KE-37 cell Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.835 μM
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=23.9757 μM
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=0.56742 μM
KM12 cell Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=3.52964 μM
KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=30.4549 μM
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay, IC50=8.81915 μM
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=37.426 μM
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.0046 μM
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=23.484 μM
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=20.7445 μM
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=13.6742 μM
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=28.3883 μM
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=10.5536 μM
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=1.71496μM
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay, IC50=11.1726 μM
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=12.7431 μM
LC4-1 cell Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=32.8341 μM
LOUCY cell Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50=1.15276 μM
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=30.2122 μM
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=39.2258 μM
LU-134-A cell Growth inhibition assay Inhibition of human LU-134-A cell growth in a cell viability assay, IC50=7.14068 μM
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=22.218 μM
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=17.4351μM
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay, IC50=45.0841 μM
MDA-MB-134-VI cell Growth inhibition assay Inhibition of human MDA-MB-134-VI cell growth in a cell viability assay, IC50=39.2486 μM
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=0.64383 μM
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=0.0669 μM
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=3.40304 μM
MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=4.43653 μM
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=4.11163 μM
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=14.4124 μM
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=1.25922 μM
MRK-nu-1 cell Growth inhibition assay Inhibition of human MRK-nu-1 cell growth in a cell viability assay, IC50=0.57572 μM
MSTO-211H cell Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=12.869 μM
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=0.13915 μM
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=1.56109 μM
NB1 cell Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=3.84369 μM
NB10 cell Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50=0.13915 μM
NB12 cell Growth inhibition assay Inhibition of human NB12 cell growth in a cell viability assay, IC50=16.5656 μM
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay, IC50=2.31278 μM
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay, IC50=3.58051 μM
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=0.59114 μM
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay, IC50=41.8453 μM
NCI-H1155 cell Growth inhibition assay Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50=14.3408 μM
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay, IC50=11.8982 μM
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=4.9411 μM
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay, IC50=22.8795 μM
NCI-H1417 cell Growth inhibition assay Inhibition of human NCI-H1417 cell growth in a cell viability assay, IC50=5.67522 μM
NCI-H1436 cell Growth inhibition assay Inhibition of human NCI-H1436 cell growth in a cell viability assay, IC50=3.84101 μM
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=12.8935 μM
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=36.6284 μM
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화학 정보, 보관 및 안정성

분자량 607.06 화학식

C29H30N8O5.HCl

보관 (수령일로부터)
CAS 번호 2095432-71-4 SDF 다운로드 원액 보관

동의어 GSK269962B, GSK269962 Smiles CCN1C2=CC(=NC=C2N=C1C3=NON=C3N)OC4=CC=CC(=C4)NC(=O)C5=CC=C(C=C5)OCCN6CCOCC6.Cl

용해도

In vitro
배치:

DMSO : 100 mg/mL (164.72 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 28 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

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

Targets/IC50/Ki
ROCK1
(Cell-free assay)
1.6 nM
ROCK2
(Cell-free assay)
4 nM
MSK1
(Cell-free assay)
49 nM
RSK1
(Cell-free assay)
132 nM
시험관 내(In vitro)
GSK269962A는 사람 평활근에서 안지오텐신 II에 의해 유도된 액틴 스트레스 섬유 형성을 완전히 억제했습니다. 액틴 섬유 형성 억제 효과는 약 1 μM GSK269962A에서부터 관찰되었습니다. GSK269962A는 IC50 35 nM으로 전수축된 쥐 대동맥(조직 배양액)에서 혈관 이완을 유도했습니다. GSK269962A에 의해 유도된 이완은 가역적입니다. GSK269962A는 대식세포에서 IL-6 mRNA 전사를 억제하고 LPS 유도 IL-6 및 TNF-α 단백질 생성을 감소시켰습니다.
생체 내(In vivo)
GSK269962A의 경구 투여는 자발성 고혈압 쥐에서 전신 혈압의 현저한 용량 의존적 감소를 유도했습니다. 혈압 감소는 급성적이고 상당했습니다. 혈압에 대한 최대 효과는 경구 위관 영양 후 약 2시간 후에 관찰되었습니다. 혈압 감소는 아마도 압력 반사 기전의 활성화로 인해 심박수의 급성, 용량 의존적 증가를 동반했습니다. 10 mg/kg 용량의 GSK 269962를 사용한 ROCK 억제는 결과적으로 VV(배뇨량), PVR(잔뇨), VT(부피 역치), VE(배뇨 효율), ICI(수축 간격), BC(방광 순응도) 및 VTNVC(비배뇨성 수축 유발 부피 역치)의 증가를 유발했습니다. GSK 269962를 통한 ROCK 경로의 억제는 HR(심박수), SBP(수축기 혈압), MBP(평균 동맥압) 또는 DBP(확장기 혈압)에는 영향을 미치지 않는 것으로 보였습니다. NVC:nonvoiding contractions.
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