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首页-小分子抑制剂&激动剂-GPCR-GPER (GPR30)-GPER agonist G-1
GPER agonist G-1

Chemical Structure : GPER agonist G-1

CAS No.: 881639-98-1

GPER agonist G-1 (Tespria)

货号: PC-60270Not For Human Use, Lab Use Only.

GPER agonist G-1 (Tespria) is potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GPER agonist G-1 (Tespria) is potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.
GPER agonist G-1 displays no activity at ERα and ERβ at concentrations up to 10 uM.
GPER agonist G-1 increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with IC50 of 0.7 and 1.6 nM respectively.
GPER agonist G-1 induces cell cycle arrest, DNA damage and cell death by the activation of the intrinsic apoptotic mechanism in H295R cells.

物理化学性质&存储条件

分子量 412.28
分子式 C21H18BrNO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone

参考文献

1. Wang C, et al. Mol Endocrinol. 2008 Mar;22(3):636-48.

2. Chimento A, et al. Oncotarget. 2015 Aug 7;6(22):19190-203.

3. Ahola TM, et al. Endocrinology. 2002 Sep;143(9):3376-84.

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