| Cas No.: | 956274-94-5 |
| Chemical Name: | 2-[2-[2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol |
| Synonyms: | 2-[2-[2-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-3H-benzimidazol-5-yl]phenyl]propan-2-ol;Mavatrep |
| SMILES: | OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2 |
| Formula: | C25N2OF3H21 |
| M.Wt: | 422.4423 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | 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.IC50 value: 6.5 nM (Ki, for TRPV1)Target: TRPV1in 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. |
| References: | [1]. Parsons WH, 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 May |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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