產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg 25mg
CAS	1161002-05-6
別名	N/A
化學(xué)名	(3aR,4R,9bS)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
分子式	C19H16BrNO2
分子量	370.24
溶解度	≥ 37mg/mL in DMSO
儲(chǔ)存條件	-20°C, protect from light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

G-15 is a selective antagonist of GPR30 with Ki value of 20 nM [1].

G protein-coupled receptor 30 (GPR30) is an integral membrane protein that localizes to the endoplasmic reticulum and with high affinity for estradiol and aldosterone. GPR30 participates in multiple intracellular signaling pathways [1].

G-15 is a selective GPR30 antagonist with Ki value of 20 nM, While displayed little binding to ERα or ERβ up to 10 μM. In SKBr3 breast cancer cells that expressed only GPR30, G-1 or estrogen significantly increased intracellular calcium concentrations, while G15 inhibited the response to G-1 or estrogen with IC50 value of 185 and 190 nM respectively in a dose-dependent way. In GPR30-transfected COS7 cells, G-15 inhibited both estrogen and G-1 activation of PI3K and accumulation of PIP3 [1]. In endometriotic cells, G-1 increased cell proliferation and Akt phosphorylation, while G-15 reversed this stimulation and inhibited cell proliferation and induced Akt dephosphorylation [2].

In intact rats and ovariectomized (OVX) rats treated with estradiol, G-15 impaired acquisition of delayed matching-to-position (DMP) T-maze task with a persistent turn. The result suggested that GPR30 played an crucial role in mediating the effects of estradiol on spatial learning [3].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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