Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pyr10 是吡唑衍生物,是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 549 | 现货 | ||
10 mg | ¥ 892 | 现货 | ||
50 mg | ¥ 3,216 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 598 | 现货 |
产品描述 | Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor. Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells (IC50: 0.72 μM) (IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells) . |
靶点活性 | TRPC3:0.72 μM |
体外活性 | The novel pyrazole Pyr10 displayed substantial selectivity for TRPC3-mediated responses (18-fold) and the selective block of TRPC3 channels by Pyr10 barely affected mast cell activation[1]. |
体内活性 |
Pyr10 blunted ventricular CF activation and MF in l-NAME hypertensive mice.?Finally, TRPC3 was present in human ventricular CFs and upregulated in MF, whereas pharmacological modulation of TRPC3-NFATc3 decreased proliferation and collagen secretion.?TRPC3-NFATc3 signaling is modulated by P.E. and critically regulates ventricular CF phenotype and MF.?These findings strongly argue for P.E., through TRPC3 targeting, as potential and interesting therapeutics for MF management[2]. |
分子量 | 449.37 |
分子式 | C18H13F6N3O2S |
CAS No. | 1315323-00-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (211.4 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2253 mL | 11.1267 mL | 22.2534 mL | 55.6334 mL |
5 mM | 0.4451 mL | 2.2253 mL | 4.4507 mL | 11.1267 mL | |
10 mM | 0.2225 mL | 1.1127 mL | 2.2253 mL | 5.5633 mL | |
20 mM | 0.1113 mL | 0.5563 mL | 1.1127 mL | 2.7817 mL | |
50 mM | 0.0445 mL | 0.2225 mL | 0.4451 mL | 1.1127 mL | |
100 mM | 0.0223 mL | 0.1113 mL | 0.2225 mL | 0.5563 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。
Pyr10 1315323-00-2 Membrane transporter/Ion channel TRP/TRPV Channel l-NAME pyrazole SOCE Inhibitor TRPC3 fibroblast cardiac ROCE inhibit Orai STIM1 Pyr 10 Transient receptor potential channels Ca2+ TRP Channel Pyr-10 inhibitor