Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BI-749327是高选择性、口服有效的TRPC6拮抗剂,对小鼠、人、豚鼠 TRPC6 作用的IC50值分别为 13 nM、19 nM 和 15 nM。BI-749327对小鼠 TRPC6 选择性比 TRPC3 高出 85 倍, 比TRPC7高出42 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 995 | 现货 | ||
5 mg | ¥ 2,880 | 现货 | ||
10 mg | ¥ 4,280 | 现货 | ||
25 mg | ¥ 6,220 | 现货 | ||
50 mg | ¥ 7,630 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,180 | 现货 |
产品描述 | BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6). |
靶点活性 | guinea pig TRPC6:15 nM (IC50), human TRPC6:19 nM (IC50), mouse TRPC6:13 nM (IC50) |
体外活性 | BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7. BI-749327 suppresses NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants and blocks associated signaling and expression of prohypertrophic genes in isolated myocytes. |
体内活性 | BI-749327 (30 mg/kg/day; i.g.) improves left heart function, reduces volume/mass ratio, and blunts expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload. BI-749327 dose-dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction. BI-749327 (3-30 mg/kg; p.o.) has a long terminal half-life (t1/2 8.5-13.5 hours) for mice. |
分子量 | 442.43 |
分子式 | C23H21F3N4O2 |
CAS No. | 2361241-23-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 31.25 mg/mL (70.63 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2602 mL | 11.3012 mL | 22.6024 mL | 56.5061 mL |
5 mM | 0.452 mL | 2.2602 mL | 4.5205 mL | 11.3012 mL | |
10 mM | 0.226 mL | 1.1301 mL | 2.2602 mL | 5.6506 mL | |
20 mM | 0.113 mL | 0.5651 mL | 1.1301 mL | 2.8253 mL | |
50 mM | 0.0452 mL | 0.226 mL | 0.452 mL | 1.1301 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。
BI-749327 2361241-23-6 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor inhibit Transient receptor potential channels BI749327 TRP Channel BI 749327 inhibitor