Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW791343 trihydrochloride (GW791343 3HCl) 是 P2X7变构调节剂,有种属特异性,对人 P2X7的pIC50为6.9-7.2。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 848 | 6-8周 | ||
10 mg | ¥ 1,192 | 6-8周 | ||
25 mg | ¥ 2,146 | 6-8周 | ||
100 mg | ¥ 8,266 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 848 | 6-8周 |
GW791343 trihydrochloride 的其他形式现货产品:
产品描述 | GW791343 trihydrochloride (GW791343 3HCl) is aHCl salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7. |
靶点活性 | P2X7:7(pIC50) |
体外活性 | Synephrine (0.1-30 μM) displays potent vasoconstrictive effects on isolated rat aorta in a dose dependent manner, which can be significantly inhibited by pretreatment with prazosin, BRL15572, and ketanserin but not by pretreatment with SB216641 and propranolol, indicating that Synephrine exerts the constrictive effects via adrenergic alpha(1)-receptors, serotonergic 5-HT(1D) receptors, and 5-HT(2A) receptors. [2] Although the Ki values of Synephrine, 1R,2S-norephedrine, and β-phenethylamine are same for all three subtypes, only Synephrine is a partial agonist of α1A-AR subtype stably expressed in HEK 293 cells with EC50 of 4 μM, giving a maximal response at 100 μM that is equal to 55.3 % of the L-phenylephrine maximum. Functional studies on the α2A- and α2C-AR subtypes stably expressed in CHO cells indicate that Synephrine may act as an antagonist rather than an agonist of the pre-synaptic α(2A)- and α(2C)-AR subtypes present in nerve terminals, although antagonist activity of synephrine is lower than its partial agonist potency. [3] Synephrine (~100 μM) treatment increases basal glucose consumption up to 50% over the control in a dose-dependent manner, without affecting the viability of L6 skeletal muscle cells. Synephrine significantly stimulates the basal- or insulin-stimulated lactic acid production as well as glucose consumption. Synephrine treatment stimulates the phosphorylation of AMPK but not Akt, and Synephrine-induced glucose consumption and the translocation of Glut4 from the cytoplasm to the plasma membrane are sensitive to the inhibition of AMPK but not to the inhibition of PI3 kinase. [4] |
别名 | GW791343 3HCl |
分子量 | 483.81 |
分子式 | C20H24F2N4O·3HCl |
CAS No. | 309712-55-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 48.4 mg/mL(100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0669 mL | 10.3346 mL | 20.6693 mL | 51.6732 mL |
5 mM | 0.4134 mL | 2.0669 mL | 4.1339 mL | 10.3346 mL | |
10 mM | 0.2067 mL | 1.0335 mL | 2.0669 mL | 5.1673 mL | |
20 mM | 0.1033 mL | 0.5167 mL | 1.0335 mL | 2.5837 mL | |
50 mM | 0.0413 mL | 0.2067 mL | 0.4134 mL | 1.0335 mL | |
100 mM | 0.0207 mL | 0.1033 mL | 0.2067 mL | 0.5167 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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