Mavatrep 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。

Mavatrep is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.

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].

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].

956274-94-5

C25H21F3N2O

422.44

JNJ-39439335

DMSO:28 mg/mL (66.28 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years