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GPER antagonist G36

Chemical Structure : GPER antagonist G36

CAS No.: 1392487-51-2

GPER antagonist G36 (G36, G-36)

Catalog No.: PC-60269Not For Human Use, Lab Use Only.

GPER antagonist G36 is a potent, selective, cell-permeable GPER/GPR30 antagonist that inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 with IC50 of 112 nM and 165 nM, respectively.

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Biological Activity

GPER antagonist G36 is a potent, selective, cell-permeable GPER/GPR30 antagonist that inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 with IC50 of 112 nM and 165 nM, respectively.
GPER antagonist G36 has no detectable binding activity to either ERα or ERβ.
GPER antagonist G36 inhibits estrogen- and G-1-mediated calcium mobilization as well as ERK1/2 activation, with no effect on EGF-mediated ERK1/2 activation.

Physicochemical Properties

M.Wt 412.3
Formula C22H22BrNO2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(±)-(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline

References

1. Dennis MK, et al. J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66.

2. Ashton AW, et al. Mol Endocrinol. 2015 Aug;29(8):1144-55.

3. Evans NJ, et al. PLoS One. 2016 Mar 21;11(3):e0152138.

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