Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MDR-652是瞬时受体电位香草酸亚型 1 的选择性激动剂,对 hTRPV1 和 rTRPV1 的Ki 分别为 11.4 和 23.8 nM,EC50分别为 5.05 和 93 nM。MDR-652在缓解疼痛方面有研究的价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 538 | 现货 | ||
2 mg | ¥ 789 | 现货 | ||
5 mg | ¥ 1,320 | 现货 | ||
10 mg | ¥ 1,990 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,790 | 现货 | ||
100 mg | ¥ 6,780 | 现货 | ||
500 mg | ¥ 13,600 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,450 | 现货 |
产品描述 | MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1) with Ki value of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1 respectively and EC50s for hTRPV1 and rTRPV1 are 5.05 and 93 nM respectively. MDR-652 is a potent topical analgesic. |
靶点活性 | TRPV1 (rat):23.8 nM (Ki), TRPV1 (rat):93 nM (EC50), TRPV1 (human):11.4 nM (Ki), TRPV1 (human):5.05 nM (EC50) |
体内活性 | MDR-652 (0.5 and 5 mg/kg) displays a dose-dependent decrease of body temperature, supporting that MDR-652 displays TRPV1 agonism in the intact animal[1]. Potent analgesic activity was observed in models of neuropathic pain, and MDR-652 blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) [1]. MDR-652 has a promising topical pharmacokinetic profile[1]. MDR-652 displays weak systemic toxicity and is negative in assays of genotoxicity. In a single-dose toxicity study, the LD50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively[1]. |
动物实验 | MDR-652 (0.5 and 5 mg/kg; Administered intraperitoneally; 7 hours; ICR mouse) decreased body temperature in a dose-dependent manner. MDR-652 (1, 2, 5, and 10 mg/kg; Administered intraperitoneally and subcutaneously; 24 hours; Rats with spinal nerve ligation (SNL) model)The i.p. administration exhibited an excellent and dose dependent analgesic profile with an ED50 of 0.5-2 mg/kg. The subcutaneous injection (sc) also displayed an excellent analgesic outcome with maximum effect at 30 min after administration. |
分子量 | 447.95 |
分子式 | C22H23ClFN3O2S |
CAS No. | 1933528-96-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 249 mg/mL (555.86 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 | 2.2324 mL | 11.162 mL | 22.3239 mL | 55.8098 mL |
5 mM | 0.4465 mL | 2.2324 mL | 4.4648 mL | 11.162 mL | |
10 mM | 0.2232 mL | 1.1162 mL | 2.2324 mL | 5.581 mL | |
20 mM | 0.1116 mL | 0.5581 mL | 1.1162 mL | 2.7905 mL | |
50 mM | 0.0446 mL | 0.2232 mL | 0.4465 mL | 1.1162 mL | |
100 mM | 0.0223 mL | 0.1116 mL | 0.2232 mL | 0.5581 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。
MDR-652 1933528-96-1 Membrane transporter/Ion channel TRP/TRPV Channel Inhibitor Transient receptor potential channels MDR 652 neuropathic MDR652 analgesic TRP Channel TRPV1 activity pain hTRPV1 inhibit ligand inhibitor