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G-36 (CAS 1392487-51-2) LS-H96

GPER antagonist
LS-H96-1 / 1 mg / $175
LS-H96-5 / 5 mg / $225
LS-H96-10 / 10 mg / $265
LS-H96-50 / 50 mg / $725
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Description: G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17 beta -estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). It has no detectable binding activity to either ER alpha or ER beta . 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. G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ER alpha and ER beta in complex biological systems. H96_ChemicalStructureImage.png
(4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline
 
biochemical, chemical, antagonist
LS-H96
1392487-51-2
C22H22BrNO2
≥98%
A crystalline solid
 
BrC1=CC2=C(OCO2)C=C1[C@@H]3NC(C=CC(C(C)C)=C4)=C4[C@@]5([H])[C@]3([H])CC=C5
InChI=1S/C22H22BrNO2/c1-12(2)13-6-7-19-16(8-13)14-4-3-5-15(14)22(24-19)17-9-20-21(10-18(17)23)26-11-25-20/h3-4,6-10,12,14-15,22,24H,5,11H2,1-2H3/t14-,15+,22-/m1/s1
QTOCPACSSHFGOY-ZCCHDVMBSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: GPER1 / GPR30 related products

Usage Information

G-36 is supplied as a crystalline solid. A stock solution may be made by dissolving the G-36 in the solvent of choice. G-36 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of G-36 in these solvents is approximately 1, 20, and 30 mg/ml, respectively. G-36 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, G-36 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. G-36 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Filardo, E.J. and Thomas, P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 153(7), 2953-2962 (2012).
  2. Chevalier, N., Vega, A., Bouskine, A., et al. GPR30, the non-classical membrane G protein related estrogen receptor, is overexpressed in human seminoma and promotes seminoma cell proliferation. PLoS One 7(4), 34672 (2012).
  3. Dennis, M.K., Field, A.S., Burai, R., et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J. Steroid Biochem. Mol. Biol. 127(3-5), 358-366 (2011).
  4. Brailoiu, G.C., Arterburn, J.B., Oprea, T.I., et al. Bradycardic effects mediated by activation of G protein-coupled estrogen receptor in rat nucleus ambiguus. Exp. Physiol. 98(3), 679-691 (2013).

 


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