G-1
产品说明书
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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 |
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| 溶解度 : | - | |
| 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 | |
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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 |
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