G36

G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM) . G-36 is promising for research in the field of cancer[1][2].

Product Specifications

CAS Number

[1392487-51-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/g36.html

Purity

99.35

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 80°C)

Smiles

CC(C1=CC2=C(N[C@@H](C3=C(Br)C=C(OCO4)C4=C3)[C@]5([H])[C@@]2([H])C=CC5)C=C1)C

Molecular Formula

C22H22BrNO2

Molecular Weight

412.32

Precautions

H302, H315, H319

References & Citations

[1]Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, Bologa CG, Oprea TI, Yamaguchi Y, Hayashi S, Sklar LA, Hathaway HJ, Arterburn JB, Prossnitz ER. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol. 2011 Nov;127 (3-5) :358-66.|[2]Yu X, et al. The activation of G protein-coupled estrogen receptor induces relaxation via cAMP as well as potentiates contraction via EGFR transactivation in porcine coronary arteries. PLoS One. 2018 Jan 23;13 (1) :e0191418.