化合物LNP023 hydrochloride T9189

Product Introduction
Bioactivity


英文名: Iptacopan hydrochloride

描述: Iptacopan hydrochloride (LNP023 hydrochloride) 是一种可口服、高效和高选择性的因子 B 抑制剂，IC50 为 10 nM。 LNP023 显示与人因子 B 的直接、可逆和高亲和力结合，KD 为 7.9 nM。

体外活性: LNP023 demonstrates excellent selectivity over other proteases affording IC50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D (>100 μM)[3].

体内活性: LNP023 (20-180 mg/kg; oral administration) is effective upon prophylactic and therapeutic dosing in an experimental model of membranous nephropathy in rats and prevents KRN (150 μL)-induced arthritis in mice[2].After oral administration (rat 30 and, dog 10 mg/kg), LNP023 exhibits moderate half-lives (T1/2; Wistar Han rats 3.4 h, beagle dogs 5.5 h) and Cmax (Wistar Han rats 410 nM, beagle dogs 2200 nM)[3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 50 mg/mL (108.94 mM)
DMSO : 50 mg/mL (108.94 mM)


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相关产品: Lipoteichoic acid | Complement factor D-IN-2 | C3a 70-77 2TFA(63555-63-5(free base)) | ADH-503 | 3-Phenoxybenzaldehyde | CP-447697 | NDT 9513727 | JR14a | Danicopan | Avacopan

相关库: Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Highly Selective Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途