DC371739
Based on 1 Customer Validation
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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- Purity: 95.56%
- CAS No.: 2135765-21-6
- 화학식: C29H30N2O4
- 분자량:470.56
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:HepG2 cells
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Concentration:0-5 µM
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Incubation Time:4, 24, 48 h
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Result:Decreased the mRNA expression of PCSK9 and ANGPTL3 in a dose and time dependent manner.
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Cell Line:HepG2, LO2 cells
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Concentration:0.5, 1, 2.5, 5, 10 µM
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Incubation Time:24 h
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Result:Decreased the protein expression of PCSK9 and increased the protein expression of LDLR in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old healthy male Syrian golden hamsters (HFD-fed) [2]
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Dosage:10, 30, 100 mg/kg
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Administration:P.o.; daily for 21 days
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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%.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2135765-21-6
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Appearance Solid
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분자량 470.56
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화학식 C29H30N2O4
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Color Light yellow to light brown
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SMILES
OCN1C2=C(C3=C1CN4CCC5=CC(OCC6=CC=CC=C6)=C(C=C5C4C3)OC)C=C(OC)C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Bao X, et al. Targeting proprotein convertase subtilisin/kexin type 9 (PCSK9): from bench to bedside. Signal Transduct Target Ther. 2024 Jan 8;9(1):13. [Content Brief]
[2]. Wang J, et al. Identification and evaluation of a lipid-lowering small compound in preclinical models and in a Phase I trial. Cell Metab. 2022 May 3;34(5):667-680.e6. [Content Brief]
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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