Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Mavatrep (JNJ-39439335) 是一种特异性的 TRPV1 拮抗剂,Ki 为 6.5 nM,可用于炎症性疼痛的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 597 | 现货 | ||
5 mg | ¥ 1,490 | 现货 | ||
10 mg | ¥ 2,390 | 现货 | ||
25 mg | ¥ 4,820 | 现货 | ||
50 mg | ¥ 7,730 | 现货 | ||
100 mg | ¥ 9,870 | 现货 | ||
500 mg | ¥ 19,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,630 | 现货 |
产品描述 | Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain. |
体外活性 | In cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca2+ influx with an IC50 of 4.6 nM. Mavatrep blocked the activation of hTRPV1 channels by Capsaicin (1 μM, pH 5.0) in a concentration-dependent fashion[1]. |
体内活性 | In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of Mavatrep superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain[1]. |
别名 | JNJ-39439335 |
分子量 | 422.44 |
分子式 | C25H21F3N2O |
CAS No. | 956274-94-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16 mg/mL (37.88 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3672 mL | 11.836 mL | 23.672 mL | 59.18 mL |
5 mM | 0.4734 mL | 2.3672 mL | 4.7344 mL | 11.836 mL | |
10 mM | 0.2367 mL | 1.1836 mL | 2.3672 mL | 5.918 mL | |
20 mM | 0.1184 mL | 0.5918 mL | 1.1836 mL | 2.959 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。
Mavatrep 956274-94-5 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor capsaicin TRP Channel neuropathic pain calcium ions JNJ-39439335 JNJ 39439335 inhibit Transient receptor potential channels hTRPV1 channel JNJ39439335 HEK293 inhibitor