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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Based on 1 publication(s) in Google Scholar

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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.
Appearance

Solid

Color

Light yellow to light brown

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1251 mL 10.6256 mL 21.2513 mL
5 mM 0.4250 mL 2.1251 mL 4.2503 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1251 mL 10.6256 mL 21.2513 mL 53.1282 mL
5 mM 0.4250 mL 2.1251 mL 4.2503 mL 10.6256 mL
10 mM 0.2125 mL 1.0626 mL 2.1251 mL 5.3128 mL
15 mM 0.1417 mL 0.7084 mL 1.4168 mL 3.5419 mL
20 mM 0.1063 mL 0.5313 mL 1.0626 mL 2.6564 mL
25 mM 0.0850 mL 0.4250 mL 0.8501 mL 2.1251 mL
30 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 mL
40 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3282 mL
50 mM 0.0425 mL 0.2125 mL 0.4250 mL 1.0626 mL
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DC371739 Related Classifications

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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