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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1233353-74-6
- Formel: C25H26NO5S+
- Molecular Weight:452.54
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hamsters fed with HFHCD developed hyperlipidemia[1]
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Dosage:40 mg/kg; 80 mg/kg; 160 mg/kg
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Administration:oral gavage; once daily; 4 weeks
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Result:Compared with vehicle, at 40 mg/kg, serum TC was reduced by 31.0%, serum LDL-C by 22.2%, serum TG by 52.2%, liver TC by 15.0%, and liver TG by 48%.
Compared with vehicle, at 80 mg/kg, serum TC was reduced by 34.4%, serum LDL-C by 27.6%, serum TG by 52.1%, liver TC by 13.4%, and liver TG by 37%.
Compared with vehicle, at 160 mg/kg, serum TC was reduced by 43.9%, serum LDL-C by 42.6%, serum TG by 52.1%, liver TC by 20.3%, and liver TG by 49%.
At 160 mg/kg, liver LDLR protein levels increased up to 3.5-fold and circulating PCSK9 levels decreased to 10% of control.
Serum PCSK9 immunoprecipitation/Western blot analysis showed dose-dependent lowering of PCSK9 at 40, 80, and 160 mg/kg.
Chemical Information
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CAS. Nr. 1233353-74-6
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Molecular Weight 452.54
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Formel C25H26NO5S+
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)