| Identification | Back Directory | [Name]
mavatrep | [CAS]
956274-94-5 | [Synonyms]
CS-1660
mavatrep
Mavatrep(JNJ-39439335)
JNJ 39439335;JNJ39439335
(trans)-2-(2-{2-[2-(4-trifluoromethylphenyl)vinyl]-1H-benzimidazol-5-yl}phenyl)propan-2-ol
Benzenemethanol, α,α-dimethyl-2-[2-[(1E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-1H-benzimidazol-6-yl]- | [Molecular Formula]
C25H21F3N2O | [MOL File]
956274-94-5.mol | [Molecular Weight]
422.45 |
| Chemical Properties | Back Directory | [Boiling point ]
612.1±65.0 °C(Predicted) | [density ]
1.300±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
10.73±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
mavatrep is a potent and orally bioavailable antagonist of trpv1 with ic50 value of 4.6 nm [1][2].transient receptor potential vanilloid-1 (trpv1) is a thermosensitive and nonselective cation channel, and is a member of the trp channel superfamily. the channel is activated by acidic ph (<6.8), thermal stimuli (>43℃), and endogenous lipidic mediators (anandamide and oxidative metabolites of linoleic acid) [1].mavatrep is a potent and orally bioavailable trpv1 antagonist. in hek293 cells that stably express human or rat trpv1 (rtrpv1) channels, mavatrep (1 μm) inhibited capsaicin-induced ca2+ influx with ic50 values of 4.6 nm and 21 nm. in whole-cell patch clamp electrophysiology assay, mavatrep concentration-dependently inhibited the activation of htrpv1 channels by ph (5.0) and capsaicin (1 μm) with ic50 values of 6.8 and 23 nm, respectively. mavatrep (0.1 μm) also inhibited 74 ± 8.1% heat-evoked currents mediated by htrpv1 [1].in the cfa model of inflammatory of pain, mavatrep (10 mg/kg po) significantly reversed cfa-induced thermal hypersensitivity with ed50 and ed80 values of 1.8 and 7.8 mg/kg, respectively [1]. | [storage]
Store at -20°C | [References]
[1]. parsons wh, calvo rr, cheung w, et al. benzo[d]imidazole transient receptor potential vanilloid 1 antagonists for the treatment of pain: discovery of trans-2-(2-{2-[2-(4-trifluoromethyl-phenyl)-vinyl]-1h-benzimidazol-5-yl}-phenyl)-propan-2-ol (mavatrep). j med chem, 2015, 58(9): 3859-3874. |
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