莫伐倍林 T77695

Product Introduction
Bioactivity


英文名: Muvalaplin

描述: Muvalaplin (LY3473329) 是一种具有口服活性的脂蛋白 (a) Lp (a) 抑制剂，可阻断 apo(a)-apo B100 相互作用来抑制 Lp(a) 的形成。

体内活性: The single ascending dose treatment evaluated the effect of a single dose of Muvalaplin ranging from 1 mg to 800 mg or placebo taken by healthy participants with any Lp(a) level. The multiple ascending dose treatment evaluated the effect of taking daily doses of Muvalaplin (30 mg to 800 mg) or placebo for 14 days in patients with Lp(a) levels of 30 mg/dL or higher. Oral doses of 30 mg to 800 mg for 14 days resulted in increasing Muvalaplin plasma concentrations and half-life ranging from 70 to 414 hours. Muvalaplin lowered Lp(a) plasma levels within 24 hours after the first dose, with further Lp(a) reduction on repeated dosing. Maximum placebo-adjusted Lp(a) reduction was 63% to 65%, resulting in Lp(a) plasma levels less than 50 mg/dL in 93% of participants, with similar effects at daily doses of 100 mg or more. No clinically significant changes in plasminogen levels or activity were observed. Conclusion: Muvalaplin, a selective small molecule inhibitor of Lp(a) formation, was not associated with tolerability concerns and lowered Lp(a) levels up to 65% following daily administration for 14 days.[2]

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

溶解度: DMSO : 10 mg/mL (14.07 mM)
H2O : <0.1 mg/mL


关键字: Muvalaplin | LY-3473329 | LY 3473329

相关库: Drug Repurposing Compound Library | Bioactive Compounds Library Max | Inhibitor 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