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1392487-51-2

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1392487-51-2 Usage

Uses

G-36 is a selective G protein-coupled estrogen receptor (GPER) agonist.

Check Digit Verification of cas no

The CAS Registry Mumber 1392487-51-2 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,9,2,4,8 and 7 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1392487-51:
(9*1)+(8*3)+(7*9)+(6*2)+(5*4)+(4*8)+(3*7)+(2*5)+(1*1)=192
192 % 10 = 2
So 1392487-51-2 is a valid CAS Registry Number.

1392487-51-2Downstream Products

1392487-51-2Relevant articles and documents

Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity

Dennis, Megan K.,Field, Angela S.,Burai, Ritwik,Ramesh, Chinnasamy,Petrie, Whitney K.,Bologa, Cristian G.,Oprea, Tudor I.,Yamaguchi, Yuri,Hayashi, Shin-Ichi,Sklar, Larry A.,Hathaway, Helen J.,Arterburn, Jeffrey B.,Prossnitz, Eric R.

, p. 358 - 366 (2011)

GPER/GPR30 is a seven-transmembrane G protein-coupled estrogen receptor that regulates many aspects of mammalian biology and physiology. We have previously described both a GPER-selective agonist G-1 and antagonist G15 based on a tetrahydro-3H-cyclopenta[c]quinoline scaffold. The antagonist lacks an ethanone moiety that likely forms important hydrogen bonds involved in receptor activation. Computational docking studies suggested that the lack of the ethanone substituent in G15 could minimize key steric conflicts, present in G-1, that limit binding within the ERα ligand binding pocket. In this report, we identify low-affinity cross-reactivity of the GPER antagonist G15 to the classical estrogen receptor ERα. To generate an antagonist with enhanced selectivity, we therefore synthesized an isosteric G-1 derivative, G36, containing an isopropyl moiety in place of the ethanone moiety. We demonstrate that G36 shows decreased binding and activation of ERα, while maintaining its antagonist profile towards GPER. G36 selectively inhibits estrogen-mediated activation of PI3K by GPER but not ERα. It also inhibits estrogen- and G-1-mediated calcium mobilization as well as ERK1/2 activation, with no effect on EGF-mediated ERK1/2 activation. Similar to G15, G36 inhibits estrogen- and G-1-stimulated proliferation of uterine epithelial cells in vivo. The identification of G36 as a GPER antagonist with improved ER counterselectivity represents a significant step towards the development of new highly selective therapeutics for cancer and other diseases.

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