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Forskolin (Colforsin) cAMP 활성제

Name: Forskolin (Colforsin)
Brand: Selleck Chemicals
SKU: S2449
Rating: 5 (190 reviews)

제품 번호S2449

Forskolin (Colforsin)은 다양한 세포 유형에서 진핵 아데닐릴 고리화효소(AC)의 보편적인 활성제이며, 세포 생리학 연구에서 cAMP 수치를 높이는 데 일반적으로 사용됩니다. Forskolin은 또한 PXR 및 FXR 활성을 활성화합니다. Forskolin은 autophagy를 자극합니다.

Forskolin (Colforsin) cAMP 활성제 Chemical Structure

화학 구조

분자량: 410.5

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품질 관리

배치: 순도: 99.20%

99.20

함께 자주 사용되는 제품 Forskolin (Colforsin)

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EPZ004777

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관련 타겟	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
기타 cAMP 억제제	PACAP 1-38 ESI-09 Bithionol HJC0350 PACAP 6-38 acetate Lysipressin Acetate PACAP 1-27 Fipexide hydrochloride ST034307 HJC0197

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
HT-29	Apoptosis Assay	40 μM	48 h	DMSO	induces changes in the phosphorylation status of PP2A targets	24997451
SW480	Apoptosis Assay	40 μM	48 h	DMSO	induces changes in the phosphorylation status of PP2A targets	24997451
HT-29	Apoptosis Assay	40 μM	48 h	DMSO	induces an activation of caspase 3/7	24997451
SW480	Apoptosis Assay	40 μM	48 h	DMSO	induces an activation of caspase 3/7	24997451
HT-29	Function Assay	40 μM	7 d	DMSO	reduces colonosphere formation capability	24997451
SW480	Function Assay	40 μM	7 d	DMSO	reduces colonosphere formation capability	24997451
HT-29	Growth Inhibition Assay	40 μM	0-72 h	DMSO	inhibits cell growth time dependently	24997451
SW480	Growth Inhibition Assay	40 μM	0-72 h	DMSO	inhibits cell growth time dependently	24997451
HT-29	Function Assay	40 μM	48 h	DMSO	activates PP2A	24997451
SW480	Function Assay	40 μM	48 h	DMSO	activates PP2A	24997451
C6	Function Assay	10 μM	20 min		increases cAMP accumulation	25069417
Huh-7	Function Assay	0-20 μM	2 h		results in a dose-dependent increase in c-Myc expression at the protein and mRNA levels	25109834
THP-1	Function Assay	1/10 μM	2 h	DMSO	suppresses MCP-1 production	25154882
BeWo	Function Assay	20 µM	48 h	DMSO	induces cell fusion	25184477
ventricular cardiomyocytes	Function Assay	0.01-10 μM			evokes an inotropic response 120±15% above basal with an EC50 of 2.2 µM	25203113
ventricular cardiomyocytes	Function Assay	0.01-10 μM			increases cAMP accumulation	25203113
MIN6	Function Assay	10 μM	3 h		increases D3 mRNA expression	25241124
L6	Function Assay	40 µM	24 h		inhibits DMH1-induced Akt activation	25247550
HEK‐CFTR	Function Assay	2–50 μM	0-12 min	DMSO	induces a dose‐dependent iodide efflux	25263207
SK-N-SH	Cell Viability Assay	10 μM	48 h		enhances SK-N-SH neuroblastoma cell viability	25266063
SK-N-AS	Function Assay	10 μM	10/30/60 min		increases levels of p-β-catenin (ser675) and induces accumulation of p-β-catenin (ser675) in (peri)nuclear regions	25266063
SK-N-AS	Function Assay	10 μM	30 min		induces phosphorylation of β-catenin (ser675), p-GSK3β (ser9) and concomitant higher levels of active, unphosphorylated, β-catenin	25266063
SK-N-AS	Function Assay	10 μM	24 h		increases the expression of cyclin D1	25266063
SK-N-AS	Function Assay	10 μM	24 h		increases the cAMP levels	25266063
SK-N-AS	Cell Viability Assay	10 μM	24/48 h		enhances time-dependently cellular viability	25266063
granulosa cells	Function Assay	10 μM	24 h		increases the levels of RGS2 promoter activity	25339105
granulosa cells	Function Assay	10 μM	24 h		increases the intensity of DNA/protein complex	25339105
granulosa cells	Function Assay	10 μM	12/24 h		increases the levels of reporter activity for the longest fragment (−854/+18RGS2.LUC)	25339105
granulosa cells	Function Assay	10 μM	12/24 h		increases the levels of RGS2 mRNA	25339105
BeWo	Function Assay	20 µM	48 h	DMSO	downregulates the level of GCM-1	25362260
BeWo	Function Assay	20 µM	48 h	DMSO	downregulates the level of TMEMF16	25362260
BeWo	Function Assay	20 µM	48 h	DMSO	increases the beta-hCG release	25362260
EM1	Function Assay	15 μM	48 h		reduces the expression of LIF or PTGS2 in CALR- or EPAC2-silenced EM1 cells	25378661
Primary bovine chondrocytes	Growth Inhibition Assay	5μM	48 h		reverses the inhibitory effect of celecoxib on proliferation in growth plate chondrocytes	25406016
RBMECs	Function Assay	5 μM	1 h		blocks the actin cytoskeleton rearrangement seen with EMAP-II treatment	25416651
RBMECs	Function Assay	5 μM	1 h		blocks the EMAP-II-induced change in MLC phosphorylation	25416651
RBMECs	Function Assay	5 μM	1 h		reverses the changes in ZO-1 distribution seen with EMAP-II treatment	25416651
RBMECs	Function Assay	5 μM	1 h		inhibits the decreased of amount of ZO-1 in MFs induced by EMAP-II	25416651
RBMECs	Function Assay	5 μM	1 h		prevents the increase in HRP flux across the BTB induced by EMAP-II	25416651
RBMECs	Function Assay	5 μM	1 h		prevents the EMAP-II-induced TEER value decrease	25416651
RBMECs	Function Assay	5 μM	1 h		blocks the activation of RhoA/ROCK induced by EMAP-II	25416651
RBMECs	Function Assay	0.05/0.5/5 μM	0.25 h		increases cAMP concentration	25416651
ThGCs	Function Assay	10 μM	3 h		inhibits the effect of H2O2 on EDN2 mRNA	25433027
ThGCs	Function Assay	10 μM	4 h		increases CoCl2-induced EDN2 gene expression	25433027
ThGCs	Function Assay	10 μM	4 h		augments HIF1A levels that were stimulated by CoCl2	25433027
LNCaP	Function Assay	10 μM	12 h	DMSO	induces a dramatic increase of CREB1 activity	25548099
BeWo	Function Assay	20 µM	48 h	DMSO	increases the adhesion of THP-1 monocytes	25566740
BeWo	Function Assay	20 µM	48 h	DMSO	increases the differentiation of BeWo cells	25566740
OCI-Ly18	Function Assay	40 μM	1 h	DMSO	induces the increment of cAMP concentrations	25576220
OCI-Ly1	Function Assay	40 μM	1 h	DMSO	induces the increment of cAMP concentrations	25576220
3T3-L1	Function Assay	2.5/5 μM	24 h		significantly decreases ATGL protein expression at all doses tested	25590597
HEK293	Function Assay	5 µM	30 min		increases cAMP levels	25591908
hADSCs	Function Assay	5 µM	30 min		increases cAMP levels	25591908
SH-SY5Y	Function Assay	10 μM	1 h		increases AGC1 mRNA level	25597433
SH-SY5Y	Function Assay	10 μM	1 h		increases LUC activity	25597433
UACC-647	Function Assay	10 μM	15 min	DMSO	increases eEF2 phosphorylation levels	25703025
UACC-647	Function Assay	10 μM	15 min	DMSO	inhibits ERK phosphorylation	25703025
UACC-647	Function Assay			DMSO	leads to a rise in cAMP levels (EC50 = 20.39 μM)	25703025
SC	Function Assay	0.5 μM	72 h		increases both Krox-20 and O1 expression in axon-related SCs but only Krox-20	25705874
SC	Function Assay	0.5 μM	24 h		mimicks the effect of cAMP analogs on O1 and MBP expression	25705874
oocytes	Function Assay	5 μM	24 h		attenuates rh-insulin action on oocyte GVBD significantly	25707854
BeWo	Function Assay	10 μM	72 h	DMSO	mediates BeWo cell differentiation	25713425
GH3	Function Assay	1 μM	6-h		induces PRL and Bmal1, but not Clock, mRNA expression	25727018
GH3	Function Assay	1 μM	6-h		attenuates the correlation between PRL and Bmal1 expression	25727018
PC12	Function Assay	25 μM	48 h		activates cAMP	25769305
BAECs	Function Assay	25 μM	24 h		enhances the activation of PPARα by 5 μM resveratrol, T4HS, or 4-PAP	25798826
GLUTag	Function Assay	10 µM	4 h		increases the pCREB levels with the IBMX	25832631
GLUTag	Function Assay	10 µM	0/2/4 h		stimulates GLP-1 secretion cotreated with IBMX	25832631
PBMC	Function Assay	50 μM	24 h		inhibits the increased secretion of TNF induced by the DPE	25866079
H295R	Function Assay	10 μM	48 h		increases steroid metabolites in the androgen, mineralo- and glucocorticoid pathways	25869556
3T3-L1 preadipocytes	Function Assay	10 μM	12 h		induces CREB phosphorylation and C/EBPβ expression	25928058
PCCL3	Function Assay	10 µM	24 h		enhances DuOx2 promoter transcription activity	25960956
SCG	Function Assay	100 μM		DMSO	reduces the excitability of SCG neurons	25962132
HEK-293	Function Assay	35 μM		DMSO	induces a conspicuous “inactivation” of the Kv2.1 current	25962132
SCG	Function Assay	20 μM		DMSO	reversibly suppresses IKV with a IC50 of 24.4 μM	25962132
PC-3	Cell Viability Assay	40 µM	24/48/72 h	DMSO	decreases cell viability time dependently	26023836
PC-3	Function Assay	40 µM	2 h	DMSO	leads to PP2A activation	26023836
SH-SY5Y	Function Assay	30 μM	30 min	DMSO	significantly increases the activation of PKA	26025137
EndoC-βH1	Function Assay	5 μM	1 h		leads to a strong cAMP increase	26028562
EndoC-βH1	Function Assay	5 μM	1 h		potentiates glucose-induced insulin secretion in the presence of glucose	26028562
RBMECs	Function Assay	5 μM	1 h		inhibits EMAP-II-induced inactivation of Rap1	26044663
AML-12	Function Assay	20 μM	3 h		induces the dephosphorylation of CRTC2	26048985
AML-12	Function Assay	20 μM	3 h		up-regulates Pgc1a, Pepck, and G6pc mRNA levels	26048985
AML-12	Function Assay	20 μM	1-8 h		increases glucose production	26048985
AML-12	Function Assay	20 μM	3 h		upregulates the phosphorylation levels at Thr-411 and Ser-493	26048985
Caco-2	Function Assay	0.1/1/10 μM	24 h		increases MRP2 protein level	26049102
Caco-2	Function Assay	0.1/1/10 μM	20 min		induces a dose-dependent increase in intracellular cAMP levels	26049102
bovine oocytes	Function Assay	100 μM	12 h		inhibits the effect of NPPA and/or NPPC to stimulate resumption of meiosis	26051611
BeWo	Function Assay	25 μM	24/48/72 h		leads to an increase in the expression of other fusion markers	26053549
Spinal cords	Function Assay	1 μM	30 min		stimulates cAMP levels	26126926
MDCK	Function Assay	10 µM	24 h	DMSO	inhibits the increased expression of FN caused by TGF-β1	26202352
MDCK	Function Assay	10 µM	24 h	DMSO	upregulates the expression of TGF-β1 and CTGF	26202352
RPMI 8226	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
H929	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
U266	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
OPM-2	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
INA-6	Cell Viability Assay	0-100 μM	72 h		induces cell death dose dependently	26306624
RBMECs	Function Assay	5 μM	1 h		blocks the Rac1 inactivation induced by EMAP-II	26358039
Mo-DCs	Function Assay	50 μM	24 h		promotes IL-23 production in the supernatant of zymosan stimulated Mo-DCs	26412948
HEK293	Function Assay	10 μM	6 h		increases phosphorylation of overexpressed KLHL3 at S433	26435498
ASK	Function assay		1 hr			2849641
Vero E6	Antiviral assay					17663539
epithelial cells	Function assay	1 uM	4, 6, and 8 days			19966789
HepG2 (DPX-2)	Function assay		24 hrs			20966043
HepG2	Function assay		24 hrs			20966043
HepG2 (DPX-2)	Function assay		24 hrs			20966043
HEK293T	Function assay	10 uM				24387325
HEK293	Function assay	10 uM	16 hrs			26435512
MCF7	Cytotoxicity assay		48 hrs			28838692
HEK293	Function assay		30 mins			30006176
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	410.5	화학식	C₂₂H₃₄O₇	보관 (수령일로부터)	3년-20°C분말
CAS 번호	66575-29-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	HL 362, Coleonol			Smiles	CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O

용해도

In vitro
배치:

DMSO : 82 mg/mL (199.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 82 mg/mL

Water : Insoluble

DMSO : 40 mg/mL (97.44 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 20 mg/mL

Water : Insoluble

DMSO : 82 mg/mL (199.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 45 mg/mL

Water : Insoluble

DMSO : 82 mg/mL (199.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 82 mg/mL

Water : Insoluble

DMSO : 82 mg/mL (199.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 82 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.050mg/ml (2.56mM)	Taking the 1 mL working solution as an example, add 50 μL 21 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

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	Adenylyl cyclase (AC) (A wide variety of cell types)
시험관 내(In vitro)	Forskolin (Colforsin)은 막, 세포 또는 조직에서 cAMP 수준을 증가시킵니다. 이는 Adenylyl Cyclase를 활성화할 뿐만 아니라 포도당 수송체 및 이온 채널을 포함한 특정 다른 단백질과 상호 작용합니다. 이 화합물은 9가지 다른 막 횡단 Adenylyl Cyclase 동형의 활성화를 촉진할 수 있으며, AC9에 대해서는 다소 낮은 효능을 보입니다. 이는 고친화성 결합 부위, 즉 G-proteins (G_s)–Adenylyl Cyclase 복합체를 식별하고 정량화하는 수단을 제공하는 데 사용될 수 있습니다. GPCRs에 의한 _s의 활성화는 _s-Forskolin에 의한 Adenylyl Cyclase 활성의 강화로 인해 세포 내 Forskolin 자극 cAMP 생성에 기여합니다. 이는 세포 표면 수용체와 상호 작용하지 않고 아데닐레이트 사이클라제 활성을 자극합니다. cAMP의 강화는 호염기구 및 비만 세포 탈과립 및 히스타민 방출을 억제하고, 혈압 및 안압을 낮추며, 혈소판 응집을 억제하고, 혈관 확장, 기관지 확장 및 갑상선 호르몬 분비를 촉진하며, 지방 세포에서 지방 분해를 자극합니다. Forskolin은 cAMP 형성과는 독립적으로 혈소판 활성화 인자(PAF)의 결합을 억제하는데, 이는 PAF에 대한 직접적인 효과 또는 PAF의 수용체 부위 결합 방해를 통해 발생할 수 있습니다. 또한 여러 막 수송 단백질에 영향을 미치는 것으로 보이며, 적혈구, 지방세포, 혈소판 및 기타 세포에서 포도당 수송을 억제합니다. 이 화합물은 녹내장 치료에 사용됩니다.
생체 내(In vivo)	Forskolin (Colforsin, HL 362, Coleonol)은 다양한 세포 유형에서 진핵생물 Adenylyl Cyclase (AC)의 유비쿼터스 활성제이며, 일반적으로 cAMP 수치를 높이는 데 사용됩니다. 또한 PXR 및 FXR 활성을 활성화하고 Autophagy를 자극합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/12825829/ [2] https://pubmed.ncbi.nlm.nih.gov/23023353/ [3] https://pubmed.ncbi.nlm.nih.gov/35286396/ [4] https://pubmed.ncbi.nlm.nih.gov/27590029/

적용 분야

방법	바이오마커	PMID
Western blot	cleaved caspase-3 / caspase-3 cleaved caspase-9 / caspase-9 β-catenin c-myc / Cyclin D1 pS6K1 / S6K1 / pCREB / CREB p-JNK / JNK / P-p38 / p38	30863177
Immunofluorescence	5hmC Fe(II) CYP17A1 / CYP21A2	29239726
Growth inhibition assay	Cell viability	30863177

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT04254705	Withdrawn	Cystic Fibrosis	Universitaire Ziekenhuizen KU Leuven\|Vertex Pharmaceuticals Incorporated\|KU Leuven\|University of Lisbon	March 1 2020	Not Applicable
NCT02807415	Completed	Cystic Fibrosis	Hannover Medical School\|Heidelberg University\|University of Giessen	June 1 2016	--
NCT02586883	Completed	Idiopathic Dilation of the Bronchi	Assistance Publique - Hôpitaux de Paris	March 29 2016	Not Applicable
NCT03652090	Completed	Cystic Fibrosis	Institut National de la Santé Et de la Recherche Médicale France\|ABCF2	September 1 2010	--

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C1=C0/X	C1:	LOG(C1):
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