Mavatrep(JNJ-39439335)

产品编号: DC8378 Featured
Mavatrep(JNJ-39439335)
结构式
956274-94-5
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中国地区超过5000个高品质化合物库存
应用领域
Mavatrep是一种口服生物有效的TRPV1拮抗剂, 对hTRPV1通道具有高亲和力, 抑制TRPV1激动剂与[3H]-Resiniferatoxin结合(Ki=6.5 nM), 对CYP亚型 3A4, 1A2, 和 2D6的酶活性作用效果较低。
Cas No.: 956274-94-5
名称:
别名: JNJ-39439335,JNJ 39439335,JNJ39439335
SMILES: CC(C)(C1=CC=CC=C1C2=CC3=C(C=C2)N=C(N3)/C=C/C4=CC=C(C=C4)C(F)(F)F)O
分子式: C25H21F3N2O
分子量: 422.44
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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