1233353-74-6
Chemical Structure
CVI-LM001
- CAS No.: 1233353-74-6
- Formula:C25H26NO5S+
- Molecular Weight:452.54
IUPAC Name: (7S,13aR)-3,10-dimethoxy-9-((phenylsulfonyl)oxy)-5,6,7,8,13,13a-hexahydroisoquinolino[3,2-a]isoquinolin-7-ium
InChIKey: VMEXZUKCHMJHJC-HSZRJFAPSA-O
SMILES: O=S(OC1=C(C=CC2=C1C[N@+]3([C@@]([H])(C4=CC=C(C=C4CC3)OC)C2)[H])OC)(C5=CC=CC=C5)=O
Biological Activity: CVI-LM001 is an orally active PCSK9 inhibitor. CVI-LM001 inhibits PCSK9 transcription and suppresses PCSK9 mRNA expression, reducing circulating PCSK9. CVI-LM001 stabilizes LDLR mRNA and increases hepatic LDLR expression. CVI-LM001 induces hepatic AMPK phosphorylation, alleviates hepatic steatosis, reduces triglyceride synthesis, promotes fatty acid oxidation, and lowers serum and hepatic lipid levels. CVI-LM001 can be used for research on hypercholesterolemia and metabolic dysfunction-associated steatotic liver disease[1][2][3][4][5].
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CVI-LM001 | CVI-LM001 is an orally active PCSK9 inhibitor. CVI-LM001 inhibits PCSK9 transcription and suppresses PCSK9 mRNA expression, reducing circulating PCSK9. CVI-LM001 stabilizes LDLR mRNA and increases hepatic LDLR expression. CVI-LM001 induces hepatic AMPK phosphorylation, alleviates hepatic steatosis, reduces triglyceride synthesis, promotes fatty acid oxidation, and lowers serum and hepatic lipid levels. CVI-LM001 can be used for research on hypercholesterolemia and metabolic dysfunction-associated steatotic liver disease. | |||||||||||||||||||||
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References
- [1]. Liu J, et al. CVI-LM001, a first-in-class novel oral PCSK9 modulator, lowers plasma Ldl-c and reduces circulating PCSK9 in preclinical animal models and in hyperlipidemic human subjects[J]. Circulation, 2020, 142(Suppl_3): A12579.
- [2]. Arnaboldi L, et al. New frontiers in the treatment of hypercholesterolaemia: oral inhibition of PCSK9. European heart journal supplements : journal of the European Society of Cardiology. 2026 May;28(Suppl 5):v95-v99.
- [3]. Kosmas CE, et al. PCSK9 Targeting in the Management of Hypercholesterolaemia. EMJ Cardiol. 2023;11(1):87-97.
- [4]. Qiao MQ, et al. Structure-activity relationship and biological evaluation of xanthine derivatives as PCSK9 inhibitors for the treatment of atherosclerosis. European journal of medicinal chemistry. 2023 Feb 05;247:115047. [Content Brief]
- [5]. Tokgözoğlu L, et al. Oral PCSK9 Inhibitors: Will They Work?. Current atherosclerosis reports. 2025 Apr 30;27(1):53.
