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KPR-2579
产品别名
1801742-41-5
KPR-2579
N-((R)-Carbamoylphenylmethyl)-N-[(R)-1-(3,5-difluorophenyl)ethyl]benzamide
(αR)-α-[Benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-benzeneacetamide
N-((R)-2-Amino-2-oxo-1-phenylethyl)-N-((R)-1-(3,5-difluorophenyl)ethyl)benzamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C23H20F2N2O2 |
| Molecular weight | 394.41 |
| Biochem/physiol Actions【生化/生理作用】 | KPR-2579 does not distress temperature of the body at any given dose. It helps to block the activation of C-fiber single-unit afferent activities (SAAs), stimulated by acetic acid (AA). KPR-2579 is a potent and selective transient receptor potential melastatin 8 (TRPM8; CRM1) antagonist (IC50 = 80/89 nM against EC80 MeOH-induced Ca2+ response in human/rat CRM1 HEK293T transfectants) with good selectivity (IC50 >30 μM against ligand-induced Ca2+ influx using hTRPA1, hTRPV1, or hTRPV4 transfectants) and oral availability (59% post 10 mg/kg p.o.; rats). KPR-2579 exhibits in vivo efficacy against icilin-induced wet-dog shakes (WDS; by 31/73/100% with 1/3/10 mg/kg p.o. 1h prior to icilin i.p.; female rats) and distension-induced rhythmic bladder contraction (by 70/89% with 0.1/0.3 mg/kg i.v.; male rats) without negative cardiovascular effects. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| optical activity【旋光性】 | [α]/D +124 to +136°, c = c=1 in chloroform-d |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=C(C1=CC=CC=C1)N([C@H](C)C2=CC(F)=CC(F)=C2)[C@H](C3=CC=CC=C3)C(N)=O |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
