Chemical Structure : GPER antagonist G36
CAS No.: 1392487-51-2
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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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.
M.Wt | 412.3 | |
Formula | C22H22BrNO2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
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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