ELN441958

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更新时间： 2026-01-15 11:07:17

CAS号：913064-47-8

常用名： ELN-441958

价格：
￥需询单/1kg ￥需询单/1g ￥需询单/1mg

纯度： 98.0%

备货期： 需询单

库存： 询单

其他详情（用途，包装）：
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

供应商信息：

公司名：上海楼岚生物科技有限公司

认证状态： 未认证供应商

商品数： 2474件

电话： 52996696

地址： 沪南路2729弄1310号

地区： 上海市浦东新区

联系人： 孙先生

联系人电话： 021-52996696

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网址：http://www.bioll.com

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2025-02-05 价格：￥3825.9 ELN-441958

2024-07-15 价格：需询单 ELN-441958

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ELN-441958价格

ELN441958

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