ELN-441958
更新时间：2025-09-12 19:48:45
采购访问：21次
| 常用名 | ELN-441958 | CAS号 | 913064-47-8 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor.IC50 value: 0.26 nM (Ki)Target: B1 Receptorin vitro: ELN-441958 is a novel small molecule bradykinin B1 receptor antagonist, based on the inhibition of agonist-induced increases in intracellular calcium in native and recombinant cells. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. ELN-441958 also displays good selectivity for B1 over other receptors examined in a broad screening panel. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptor, the most potent off-target activity identified. In IMR-90 cells expressing the native human B1 receptor, ELN-441958 produced a concentration-dependent antagonism of the DAKD-induced calcium mobilization with a KB of 0.12 nM. [1]in vivo: ELN-441958 is essentially completely absorbed and produces high plasma levels after oral administration in rhesus monkeys.ELN-441958 has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes. ELN-441958 has high oral exposure and moderate plasma half-lives in rats and rhesus monkeys. The oral availability of ELN441958 in rats was 57%. ELN-441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 3 mg/kg s.c. [1] 物理化学性质： CAS号：913064-47-8 常用中文名：ELN-441958 常用英文名：ELN-441958 分子式：C29H29ClN4O2 分子量：501.01900 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：-20°C，密闭，干燥 |
上海化源世纪贸易有限公司
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- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：ELN-441958
- 价格： ￥3825.9/10mg ￥2380.9/5mg ￥7650.9/25mg ￥12240.9/50mg
- 纯度：99.0%
- 备货期：10天
- 联系人：阿拉丁
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：ELN-441958
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：$463/10mM*1mLinDMSO