2015年10月26日星期一

Mavatrep(JNJ-39439335)|TRPV1 inhibitor|DC Chemicals

Mavatrep(JNJ-39439335)|TRPV1 inhibitor|DC Chemicals

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

Product Name: Mavatrep(JNJ-39439335) |Catalog Number:  DC8378 | cas: 956274-94-5 | Other names: JNJ-39439335,JNJ 39439335,JNJ39439335 | Chemical name: | Molecule Formula: C25H21F3N2O | MW: 422.44

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
in vitro: Mavatrep exhibits superior pharmacodynamic properties. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM. Mavatrep blocks the activation of hTRPV1 channels by Capsaicin (1 μM) and by pH (5.0) in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM, respectively.
in vivo: Mavatrep exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain.

For research and scientific purpose only, not for human use.

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