G15

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Chemical Structure| 1161002-05-6 同义名 : GRB-G15
CAS号 : 1161002-05-6
货号 : A1176585
分子式 : C19H16BrNO2
纯度 : 99%+
分子量 : 370.24
MDL号 : MFCD16618401
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 G15 is a high-affinity and selective GPER receptor antagonist with Ki value of 20nM[1]. It exhibits low-affinity cross-reactivity with the canonical estrogen receptor (ER) ERα, such that it mediates limited ER-dependent transcriptional activity at doses greater than 1 µM[2]. G-15 antagonizes the anti-depressive effects of estrogen in vivo at dose of 10mg/kg, i.p.[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.01mL

5.40mL

2.70mL
参考文献

[1]Dennis MK, Burai R, Ramesh C, Petrie WK, Alcon SN, Nayak TK, Bologa CG, Leitao A, Brailoiu E, Deliu E, Dun NJ, Sklar LA, Hathaway HJ, Arterburn JB, Oprea TI, Prossnitz ER. In vivo effects of a GPR30 antagonist. Nat Chem Biol. 2009 Jun;5(6):421-7. doi: 10.1038/nchembio.168. PMID: 19430488; PMCID: PMC2864230.

[2]Dennis MK, Field AS, Burai R, Ramesh C, Petrie WK, Bologa CG, Oprea TI, Yamaguchi Y, Hayashi S, Sklar LA, Hathaway HJ, Arterburn JB, Prossnitz ER. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J Steroid Biochem Mol Biol. 2011 Nov;127(3-5):358-66. doi: 10.1016/j.jsbmb.2011.07.002. Epub 2011 Jul 14. PMID: 21782022; PMCID: PMC3220788.