产品说明
生化/生理作用
SLV320 is an orally active, high-affinity adenosine receptor A1 antagonist (pKi = 9.0 against 3H-DPCPX for binding human A1R and 8.6 against 3H-CCPA for binding rat A1R) that exhibits higher A1R-selectivity than DPCPX over other adenosine receptor subtypes (Fold-selectivity/subtypes = 200/hA3, 398/hA2a, 3981/hA2b). SLV320 displays much reduced or little affinity toward a panel of 94 other receptors and no inhibitory activity against PDE1-6 (IC50 ≥1 μM). SLV320 selectively reduces A1R-mediated bradycardia (ED50 = 0.49 mg/kg via p.o. or 0.25 mg/kg via i.v. 10 min prior to 100 μg/kg adenosine i.v. challenge), but not A2R-dependent hypotension (up to 2 mg/kg) among adenosin-challenged rats. When administered via food intake, SLV320 efficacy is demonstrated in experimental models of chronic renal failure (CRF; 10 mg/kg/day) and liver cirrhosis (5.1 mg/kg/day p.o.) in rats in vivo.
基本信息
| 经验(实验)分子式 | C18H20N4O |
| 分子量 | 308.38 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
| SMILES string | O[C@H]1CC[C@@H](CC1)NC2=NC(C3=CC=CC=C3)=NC4=C2C=CN4 |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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