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G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17beta-estradiol (Cay-10006315) or the GPER-selective agonist G-1 (Cay-10008933) (IC50 = 112 and 165 nM, respectively). It has no detectable binding activity to either ERalpha or ERbeta. G-36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERalpha and ERbeta in complex biological systems.Formal Name: (4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline. CAS Number: 1392487-51-2. Molecular Formula: C22H22BrNO2. Formula Weight: 412.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 206, 243, 293 nm. 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. InChi Code: InChI=1S/C22H22BrNO2/c1-12(2)13-6-7-19-16(8-13)14-4-3-5-15(14)22(24-19)17-9-20-21(10-18(17)23)26-11-25-20/h3-4,6-10,12,14-15,22,24H,5,11H2,1-2H3/t14-,15+,22-/m1/s1. InChi Key: QTOCPACSSHFGOY-ZCCHDVMBSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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