G36
Cat. No.：YN470049
CAS No. ：1392487-51-2
| 产品名称: | G36 |
| CAS No.: | 1392487-51-2 |
| Chemical Name: | (4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline |
| Synonyms: | (3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-8-isopropyl-3a,4,5, 9b-tetrahydro-3H-cyclopenta[c]quinoline;G-36 |
| 分子量: | 412.3 |
| 分子式: | C22H22BrNO2 |
| SMILES: | BrC1=CC2=C(OCO2)C=C1[C@@H]3NC(C=CC(C(C)C)=C4)=C4[C@@]5([H])[C@]3([H])CC=C5 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | G-36 是细胞膜通透的G 蛋白偶联雌激素受体(GPER/GPR30)的非甾体拮抗剂，通过 GPER 而不是Erα选择性地抑制雌激素介导的PI3K激活。G-36 还抑制雌激素介导的钙动员 (IC50=112 nM)。 |
| IC50和靶点: | |
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Filardo, E.J., and Thomas, P.Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiologyEndocrinology153(7),2953-2962(2012)
Chevalier, N., Vega, A., Bouskine, A., et al.GPR30, the non-classical membrane G protein related estrogen receptor, is overexpressed in human seminoma and promotes seminoma cell proliferationPLoS One7(4),34672(2012)
Dennis, M.K., Field, A.S., Burai, R., et al.Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivityJ. Steroid Biochem. Mol. Biol.127(3-5),358-366(2011)
Brailoiu, G.C., Arterburn, J.B., Oprea, T.I., et al.Bradycardic effects mediated by activation of G protein-coupled estrogen receptor in rat nucleus ambiguusExp. Physiol.98(3),679-691(2013)
