Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pico145 (HC-608) 是有效的瞬时受体电位通道蛋白 1/4/5 (TRPC1/TRPC4/TRPC5) 抑制剂,在细胞中,抑制 (-)-englerin A 活化TRPC4/TRPC5 通道的IC50分别为 0.349 和 1.3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,160 | 现货 | ||
5 mg | ¥ 2,890 | 现货 | ||
10 mg | ¥ 4,280 | 现货 | ||
25 mg | ¥ 6,850 | 现货 | ||
50 mg | ¥ 9,270 | 现货 | ||
100 mg | ¥ 12,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,990 | 现货 |
产品描述 | Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels. Pico145 inhibits ( )-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells) It also shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
靶点活性 | TRPC4:0.349 nM (cell assay), TRPC5:1.3 nM (cell assay), TRPC4-TRPC1:0.03 nM (cell assay), TRPC5-TRPC1:0.2 nM (cell assay) |
体外活性 | Pico145 is a remarkable small-molecule inhibitor of TRPC1/4/5 channels. Pico145 displays no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells). Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM, and 0.2 nM, respectively). Pico145 effectively inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P) and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels (IC50: 0.011 nM). The potency of Pico145 can be reduced by increased (?)-englerin A concentration. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells[1]. |
别名 | HC-608 |
分子量 | 524.88 |
分子式 | C23H20ClF3N4O5 |
CAS No. | 1628287-16-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 99 mg/mL (188.61 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.9052 mL | 9.526 mL | 19.052 mL | 47.6299 mL |
5 mM | 0.381 mL | 1.9052 mL | 3.8104 mL | 9.526 mL | |
10 mM | 0.1905 mL | 0.9526 mL | 1.9052 mL | 4.763 mL | |
20 mM | 0.0953 mL | 0.4763 mL | 0.9526 mL | 2.3815 mL | |
50 mM | 0.0381 mL | 0.1905 mL | 0.381 mL | 0.9526 mL | |
100 mM | 0.0191 mL | 0.0953 mL | 0.1905 mL | 0.4763 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。
Pico145 1628287-16-0 Membrane transporter/Ion channel TRP/TRPV Channel TRP Channel Transient receptor potential channels inhibit HC608 Pico-145 Inhibitor HC 608 Pico 145 HC-608 inhibitor