| CAS NO: | 824982-41-4 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 824982-41-4 |
| 化学名 | 3'-(trifluoromethyl)-N-(4-((trifluoromethyl)sulfonyl)phenyl)-3,6-dihydro-2H-[1,2'-bipyridine]-4-carboxamide |
| Canonical SMILES | FC(F)(C1=CC=CN=C1N2CCC(C(NC(C=C3)=CC=C3S(=O)(C(F)(F)F)=O)=O)=CC2)F |
| 分子式 | C19H15F6N3O3S |
| 分子量 | 479.4 |
| 溶解度 | <47.94mg/ml in DMSO;<23.97mg/ml in ethanol |
| 储存条件 | Store at RT |
| 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 | A 784168 is a potent antagonist of TRPV1 receptor with pKi value of 7.15 [1]. The transient receptor potential cation channel subfamily V member 1 (TrpV1) receptor is a nonselective cation channel and distributes throughout the nervous system. TrpV1 receptor is activated by a wide variety of physical and chemical stimuli [1]. A 784168 is a potent TRPV1 receptor antagonist with pKi value of 7.15 for recombinant hTRPV1 receptor. In the Ca2+ flux assay, A 784168 inhibited 50 nM CAP-induced calcium flux with pIC50 value of 7.13 of the recombinant hTRPV1 receptor [1]. A 784168 inhibited TRPV1 activation by 50 nM capsaicin, pH 5.5, 3 μM NADA and 10 μM anandamide with IC50 values of 25, 14, 33.7, 35.1 nM, respectively. In rat dorsal root ganglion neurons, A 784168 inhibited 1 μM capsaicin-induced currents with IC50 value of 10 nM [2]. In CFA-induced thermal hyperalgesia, A-784168 (30 μM/kg) reduced capsaicin-induced nocifensive behaviors with ED50 value of 10 μM/kg [2]. In rats, A 784168 inhibited 1% formalin-induced secondary mechanical hyperalgesia and allodynia in the contralateral and ipsilateral paws [3]. References: |
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