G-1

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Chemical Structure| 881639-98-1 同义名 : LNS 8801
CAS号 : 881639-98-1
货号 : A287698
分子式 : C21H18BrNO3
纯度 : 99%+
分子量 : 412.28
MDL号 : MFCD16618392
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(121.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 GPR30 is a G protein–coupled receptor identified as a novel 17β-estradiol (E2)–binding protein structurally distinct from the classic estrogen receptors α and β. GPR30 can mediate rapid E2-induced nongenomic signaling events, including stimulation of adenylyl cyclase, and, via transactivation of epidermal growth factor receptors, induces mobilization of intracellular Ca2+ stores and activation of MAPK and PI3K signaling pathways. G-1 is a GPR30-specific agonist. G-1 did not alter GPR30 mRNA expression. G-1 induced [Ca2+]i by 511nM in ER-positive MCF-7 cells, but by 1517nM in ER-negative SKBr3 cells. G-1–activated GPR30 blocked growth of ER-positive breast cancer cells but did so independently of ligand-activated ER. Activation of GPR30 by G-1 at 1μM blocked cell cycle progression at G1 phase, with up-regulation of p53, p21 and cyclin D1 observed. Pretreatment with G-1 at 1nM for 15min reduced neuronal loss through inhibiting excessive autophagy induced by glutamate exposure.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.13mL

2.43mL

1.21mL

24.26mL

4.85mL

2.43mL
参考文献

[1]Gonzalez de Valdivia E, et al. G protein-coupled estrogen receptor 1 (GPER1)/GPR30 increases ERK1/2 activity through PDZ motif-dependent and -independent mechanisms. J Biol Chem. 2017 Jun 16;292(24):9932-9943.

[2]Lu Y, Jiang Q, et al. 17β-estradiol rapidly attenuates P2X3 receptor-mediated peripheral pain signal transduction via ERα and GPR30. Endocrinology. 2013 Jul;154(7):2421-33.