ELN-441958
规格
| Cas Number | 913064-47-8 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 100 mg/mL (199.59 mM; Need ultrasonic) |
| 过滤标签 | Bradykinin Receptor,GPCR/G Protein |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | ELN-441958 是一种强效、中性、竞争性和选择性缓激肽 B 1 受体拮抗剂，对本地人缓激肽 B 1 受体的 K i 为 0.26 nM。ELN-441958 的口服生物利用度高，在小鼠中枢神经系统的暴露量低。 |
| 英文描述 |
ELN-441958 is a potent, neutral, competitive and selective bradykinin B 1 receptor antagonist with a K i of 0.26 nM against native human bradykinin B 1 receptor. ELN-441958 has high oral bioavailability, and has low CNS exposure in the mouse In Vitro ELN-441958 is selective for primate over rodent B 1 receptors with a rank order potency (K B , nanomolar) of human (0.12 ± 0.02) ~ rhesus monkey (0.24 ± 0.01) > rat (1.5 ± 0.4) > mouse (14 ± 4). ELN-441958 has good permeability and metabolic stability. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo ELN-441958 (1-10 mg/kg; s.c.; once) dose-dependently reduces carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model . ELN-441958 (0-10 mg/kg; i.v. or p.o.) exhibits a favorable pharmacokinetic profile in the rat and rhesus monkey . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult male and female rhesus monkeys Dosage: 1, 3, or 10 mg/kg Administration: Subcutaneous injection, 30 min before carrageenan injection Result: Increased the tail-withdrawal latencies in a dose-dependent manner. Animal Model: Rhesus monkeys or Sprague-Dawley rats Dosage: 2.5 or 10 mg/kg for rats, 1 mg/kg or 5 mg/kg for rhesus monkeys Administration: Intravenous injection (2.5 mg/kg and 1 mg/kg) or oral administration (10 mg/kg and 5 mg/kg) (Pharmacokinetic Analysis) Result: In rats: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg, approximately four times total body water) and a moderate clearance (0.96 L/h/kg, approximately 24% of hepatic blood flow). The terminal plasma half-life of this compound in rats was 1.7 h. When dosed orally, the concentrations increased to a maximum of 1.2 g/mL at 2 h after dosing. The oral availability was 57%. In rhesus monkeys: When dosed intravenously, showed a moderate volume of distribution (2.7 L/kg) and a moderate clearance (0.49 L/h/kg, approximately 32% of hepatic blood flow). The terminal plasma half-life was 3.9 h. When dosed orally, the concentrations increased to a maximum of 3.6 g/mL at 3.3 h after dosing. The calculated oral bioavailability was greater than 100%. Form:Solid IC50& Target:K i : 0.26 nM (native human bradykinin B 1 receptor) |