| CAS NO: | 956274-94-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 956274-94-5 |
| 别名 | JNJ-39439335 |
| 化学名 | (E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol |
| Canonical SMILES | CC(C1=CC=CC=C1C2=CC(N3)=C(N=C3/C([H])=C([H])/C4=CC=C(C(F)(F)F)C=C4)C=C2)(O)C |
| 分子式 | C25H21F3N2O |
| 分子量 | 422.44 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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]. Reference: |
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