MDR-652 是一种高效的特异性瞬时受体电位香草酸亚型 1 (TRPV1) 配体，具有激动剂活性。对 hTRPV1 和 rTRPV1 的 K_i 分别为 11.4 和 23.8 nM。对 hTRPV1 和 rTRPV1 的 EC₅₀ 分别为 5.05 和 93 nM。MDR-652 可用于缓解疼痛的研究。

MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The K i s are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC 50 s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.

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hTRPV1 11.4 nM (Ki) rTRPV1 23.8 nM (Ki)

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.
MDR-652 (5-10 mg/kg; i.p. and s.c.) blocks the neuropathic pain completely, indicating 100% maximum possible effect (MPE) .
MDR-652 has a promising topical pharmacokinetic profile.
MDR-652 has no significant toxicity. In a single-dose toxicity study, the LD 50 of MDR-652 is higher than 200 and 2000 mg/kg in i.p. and p.o. administration, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Jihyae Ann, et al. Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic. J Med Chem. 2020 Jan 9;63(1):418-424.

In Vitro: DMSO : 250 mg/mL (558.10 mM; Need ultrasonic)配制储备液