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G36

Catalog No. T22794   CAS 1392487-51-2
Synonyms: G-36

G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 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 ERα and ERβ in complex biological systems.

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G36 Chemical Structure
G36, CAS 1392487-51-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 80.00
10 mg In stock $ 139.00
25 mg In stock $ 253.00
50 mg In stock $ 427.00
100 mg In stock $ 632.00
500 mg In stock $ 1,350.00
1 mL * 10 mM (in DMSO) In stock $ 89.00
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Purity: 99.86%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description G36 is a cell-permeable non-steroidal antagonist of GPER. G36 inhibits activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC50 = 112 and 165 nM, respectively). G36 has no detectable binding activity to either ERα or ERβ. G36 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 ERα and ERβ in complex biological systems.
Targets&IC50 GPER:165 nM
Synonyms G-36
Molecular Weight 412.32
Formula C22H22BrNO2
CAS No. 1392487-51-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (109.1 mM), Sonification and heating to 80℃ are recommended.

TargetMolReferences and Literature

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. Journal of Steroid Biochemistry and Molecular Biology 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. Experimental Physiology 98(3), 679-691 (2013).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Bioactive Compounds Library Max Nuclear Receptor Compound Library Bioactive Compound Library

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Keywords

G36 1392487-51-2 Endocrinology/Hormones Estrogen Receptor/ERR G 36 G-36 inhibitor inhibit

 

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