MedChemExpress - Model Muvalaplin -2565656-70-2

Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys[1][2][3][4][5].

Muvalaplin

MCE China：Muvalaplin

Brand：MedChemExpress (MCE)

Cat. No.HY-152857

CAS：2565656-70-2

Synonyms：LY3473329

Purity：99.96%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys.

In Vivo：Muvalaplin (1-30 mg/kg, p.o., daily for 5 days) reduces the levels of Lp(a) in the Lp (a) transgenic mouse model[3]. Muvalaplin (1-100 mg/kg, p.o., daily for 15 days) reduces the levels of Lp (a) levels in cynomolgus monkeys[3].

IC50 & Target：Lipoprotein(a) (Lp(a))[1] In Vivo Muvalaplin (1-30 mg/kg, p.o., daily for 5 days) reduces the levels of Lp(a) in the Lp (a) transgenic mouse model[3]. Muvalaplin (1-100 mg/kg, p.o., daily for 15 days) reduces the levels of Lp (a) levels in cynomolgus monkeys[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Lp (a) transgenic mouse model[3]

References：

[1]. Bhatia HS, et al. Lipoprotein(a): Evidence for Role as a Causal Risk Factor in Cardiovascular Disease and Emerging Therapies. J Clin Med. 2022 Oct 13;11(20):6040. [Content Brief]

[2]. Nicholls SJ, et al. Muvalaplin, an Oral Small Molecule Inhibitor of Lipoprotein(a) Formation: A Randomized Clinical Trial. JAMA. 2023 Sep 19;330(11):1042-1053. [Content Brief]

[3]. Diaz N, et al. Discovery of potent small-molecule inhibitors of lipoprotein(a) formation. Nature. 2024 May;629(8013):945-950. [Content Brief]

[4]. Hooper AJ, et al. Potential of muvalaplin as a lipoprotein(a) inhibitor. Expert Opin Investig Drugs. 2024 Jan;33(1):5-7. [Content Brief]

[5]. Norata GD, et al. Oral strategies to target proprotein convertase subtilisin/kexin type 9 and lipoprotein(a): the new frontier of lipid lowering. Eur Heart J. 2023 Dec 21;44(48):5018-5020. [Content Brief]

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MedChemExpress - Model Muvalaplin -2565656-70-2

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Muvalaplin