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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。
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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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 358 | 现货 | |
5 mg | ¥ 893 | 现货 | |
10 mg | ¥ 1,430 | 现货 | |
25 mg | ¥ 2,890 | 现货 | |
50 mg | ¥ 4,630 | 现货 | |
100 mg | ¥ 5,920 | 现货 | |
200 mg | ¥ 7,990 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 978 | 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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 40 mg/mL (94.69 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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