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LY2444296
产品别名
1346133-11-6
LY2444296
(S)-3-Fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
4-[4-[[(2S)-2-(3-Fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]-3-fluorobenzamide
LY 2444296
LY-2444296
FP3FBZ
3-Fluoro-4-[4-[[(2S)-2-(3-fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]benzamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C24H22F2N2O2 |
| Molecular weight | 408.44 |
| Biochem/physiol Actions【生化/生理作用】 | LY2444296 is a brain-penetrant, orally active, short-acting, high-affinity, potent and selective κ (kappa) opioid receptor (KOR) antagonist (human κ/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/κ, 21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses κ agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by rat formalin test), decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| 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 | NC(C1=CC=C(OC2=CC=C(CN3CCC[C@H]3C4=CC=CC(F)=C4)C=C2)C(F)=C1)=O |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
