化合物MDR-652 T22360

Product Introduction
Bioactivity


英文名: MDR-652

描述: 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。

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.

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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 249 mg/mL (555.86 mM)


关键字: Inhibitor | Transient receptor potential channels | MDR 652 | neuropathic | MDR-652 | MDR652 | analgesic | TRP Channel | TRPV1 | activity | pain | hTRPV1 | inhibit | ligand

相关产品: HC-070 | TC-I 2014 | beta-Eudesmol | RN9893 | Optovin | RQ-00203078 | ML329 | TRPV3 antagonist 74a | AMTB hydrochloride | Englerin A

相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Covalent Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

化合物MDR-652 T22360信息由TargetMol中国为您提供，如您想了解更多关于化合物MDR-652 T22360报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途