Muvalaplin

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].

Product Specifications

CAS Number

[2565656-70-2]

Product Name Alternative

LY3473329

UNSPSC

12352005

Target

LDLR

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/muvalaplin.html

Purity

99.96

Solubility

DMSO : 22.22 mg/mL (ultrasonic; adjust pH to 7 with 1 M HCl)

Smiles

OC([C@H]([C@H]1CCNC1)CC2=CC(CN(CC3=CC(C[C@@H]([C@H]4CCNC4)C(O)=O)=CC=C3)CC5=CC(C[C@@H]([C@H]6CCNC6)C(O)=O)=CC=C5)=CC=C2)=O

Molecular Formula

C42H54N4O6

Molecular Weight

710.90

References & Citations

[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.|[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.|[3]Diaz N, et al. Discovery of potent small-molecule inhibitors of lipoprotein (a) formation. Nature. 2024 May;629 (8013) :945-950.|[4]Hooper AJ, et al. Potential of muvalaplin as a lipoprotein (a) inhibitor. Expert Opin Investig Drugs. 2024 Jan;33 (1) :5-7.|[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.