2. Metabolic Enzyme/Protease
  3. ANGPTL PCSK9
  4. DC371739

DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia.

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DC371739 Chemical Structure

DC371739 Chemical Structure

CAS No. : 2135765-21-6

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Description

DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia[1][2].

In Vitro

DC371739 (0-10 µM, 0-24 h) increases the ratio of DiI-LDL uptake in a dose- and time-dependent manner in HepG2 cells[2].
DC371739 (0-5 µM; 4, 24, 48 h) decreases the mRNA expression of PCSK9 and ANGPTL3 in HepG2 cells[2].
DC371739 (0-10 µM;24 h) decreases the protein expression of PCSK9 and increases the protein expression of LDLR[2].
DC371739 (5µM; 24 h) inhibits ANGPTL3 transcription and expression by targeting HNF-1α[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DC371739 Related Antibodies

RT-PCR[2]

Cell Line: HepG2 cells
Concentration: 0-5 µM
Incubation Time: 4, 24, 48 h
Result: Decreased the mRNA expression of PCSK9 and ANGPTL3 in a dose and time dependent manner.

Western Blot Analysis[2]

Cell Line: HepG2, LO2 cells
Concentration: 0.5, 1, 2.5, 5, 10 µM
Incubation Time: 24 h
Result: Decreased the protein expression of PCSK9 and increased the protein expression of LDLR in a dose-dependent manner.
In Vivo

DC371739 (10, 30, 100 mg/kg; p.o.; daily for 21 days) decreases the plasma levels of total cholesterol (TC), LDL-cholesterol (LDL-C) and triglyceride in hamsters[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old healthy male Syrian golden hamsters (HFD-fed) [2]
Dosage: 10, 30, 100 mg/kg
Administration: P.o.; daily for 21 days
Result: Decreased the serum TC levels of the hamsters treated with 10, 30, or 100 mg/kg by 29.46%, 35.65%, and 38.69%, the serum LDL-C levels were significantly lower by 23.25%, 31.04%, and 35.03%, respectively, led to significantly lower serum TG levels by 49.57%, 57.52%, and 78.16%.
Molecular Weight

470.56

Formula

C29H30N2O4
CAS No.
SMILES

OCN1C2=C(C3=C1CN4CCC5=CC(OCC6=CC=CC=C6)=C(C=C5C4C3)OC)C=C(OC)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DC371739 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DC3717392135765-21-6DC 371739DC-371739ANGPTLPCSK9Angiopoietin-like proteinProprotein convertase subtilisin/kexin type 9ANGPTL3LDLRHepG2 cellstotal cholesterolLDL-cholesterotriglyceridehyperlipidemiaInhibitorinhibitorinhibit

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