A cell-permeable non-steroidal antagonist of the estrogen receptor GPER (Ki = 20 nM); displays low affinity cross-reactivity with the classical estrogen receptor

G-15 – 25 mg

Brand:
Cayman
CAS:
1161002-05-6
Storage:
-20
UN-No:
Non-Hazardous - /

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-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).{23444} It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ERα, so that at doses greater than 1 µM it is capable of mediating limited ER-dependent transcriptional activity.{23443} G-15 antagonizes the anti-depressive effects of estrogen in vivo.{23444}  

 

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Description

A cell-permeable non-steroidal antagonist of the estrogen receptor GPER (Ki = 20 nM); displays low affinity cross-reactivity with the classical estrogen receptor, ERα, so that at doses greater than 1 µM it is capable of mediating limited ER-dependent transcriptional activity

Formal name: (3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline

Synonyms: 

Molecular weight: 370.2

CAS: 1161002-05-6

Purity: ≥95%

Formulation: A crystalline solid

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

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