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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 the detailed information of Mavatrep(JNJ-39439335), the solubility of Mavatrep(JNJ-39439335) in water, the solubility of Mavatrep(JNJ-39439335) in DMSO, the solubility of Mavatrep(JNJ-39439335) in PBS buffer, the animal experiment (test) of Mavatrep(JNJ-39439335), the cell expriment (test) of Mavatrep(JNJ-39439335), the in vivo, in vitro and clinical trial test of Mavatrep(JNJ-39439335), the EC50, IC50,and affinity,of Mavatrep(JNJ-39439335), For the detailed information of Mavatrep(JNJ-39439335), the solubility of Mavatrep(JNJ-39439335) in water, the solubility of Mavatrep(JNJ-39439335) in DMSO, the solubility of Mavatrep(JNJ-39439335) in PBS buffer, the animal experiment (test) of Mavatrep(JNJ-39439335), the cell expriment (test) of Mavatrep(JNJ-39439335), the in vivo, in vitro and clinical trial test of Mavatrep(JNJ-39439335), the EC50, IC50,and affinity,of Mavatrep(JNJ-39439335), Please contact DC Chemicals. |