计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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%.
IC50& Target:K i : 0.26 nM (native human bradykinin B 1 receptor)
规格
规格或纯度
10mM in DMSO
英文名称
ELN-441958
生化机理
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。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
C1CN(CCC12CCN(CC2)C(=O)C3=CC(=CC=C3)N4CC5=C(C4=O)C(=CC=C5)Cl)C6=CC=NC=C6
关联CAS
MeSH Entry Terms
7-chloro-2-(3-(9-pyridin-4-yl-3,9-diazaspiro(5.5)undecanecarbonyl)phenyl)-2,3-dihydro-isoindol-1-one;ELN441958
分子量
501.02
技术文档
高级数据
关联靶点（人）
BDKRB1
Tchem
B1缓激肽受体(B1 bradykinin receptor)
(1 活性数据)
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）