A cell-permeable non-steroidal antagonist of GPER

G-36 – 1 mg

Brand:
Cayman
CAS:
1392487-51-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.{23445} It is thought to be involved in estrogen-sensitive cancers.{23445,23446} GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.{23445} G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol (Item No. 10006315) or the GPER-selective agonist G-1 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).{23443} It has no detectable binding activity to either ERα or ERβ.{23443} 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.{23443} G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.{23443,24423}  

 

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Description

A cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively); has no detectable binding activity to either ERα or ERβ

Formal name: (4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline

Synonyms: 

Molecular weight: 412.3

CAS: 1392487-51-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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