PF-07202954
Based on 1 Customer Validation
PF-07202954 is an orally active, highly selective DGAT2 inhibitor with an IC50 of 10 nM against human DGAT2 and an IC50 of 17 nM against rat DGAT2. PF-07202954 reduces triglyceride synthesis, decreases hepatic triglyceride content and plasma triglyceride levels, inhibits de novo lipogenesis, and suppresses the hepatic SREBP signaling pathway as well as the expression of SREBP target genes. PF-07202954 is applicable to research related to non-alcoholic steatohepatitis.
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- Pureté : 98.82%
- CAS No.: 2639372-47-5
- Formule: C22H23FN6O3
- Masse moléculaire:438.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
PF-07202954 inhibits DGAT2-mediated triglyceride synthesis in cryopreserved human hepatocytes with an IC50 of 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Western-diet-fed rats
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; twice daily; 8 days
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Result:Reduced plasma triglycerides.
Reduced liver triglycerides.
Achieved a 71% reduction in plasma triglycerides at 100 mg/kg dose.
Achieved a 48% reduction in liver triglycerides at 100 mg/kg dose.
Reduced multiple SREBP target genes in a dose-dependent manner.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2639372-47-5
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Appearance Solid
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Masse moléculaire 438.45
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Formule C22H23FN6O3
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Color Light yellow to yellow
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SMILES
O=C(C1=CN=C(C2=CC(OC3=NC=CC=C3OCC)=CN=C2)N=C1)N[C@@H]4CNC[C@@H](F)C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 3.33 mg/mL (7.59 mM; ultrasonic and warming and heat to 60°C; 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)
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 | 2.2808 mL | 11.4038 mL | 22.8076 mL | 57.0190 mL |
| 5 mM | 0.4562 mL | 2.2808 mL | 4.5615 mL | 11.4038 mL |
PF-07202954 Related Classifications
HY-156259 Related Classifications
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Keywords
- PF-07202954
- 2639372-47-5
- PF07202954
- PF 07202954
- Acyltransferase
- Diacylglycerol acyltransferase
- Diglyceride acyltransferase
- acyl-CoA:cholesterol acyltransferase
- mono- acylglycerol acyltransferase
- DGAT2
- rat DGAT2
- non-alcoholic steatohepatitis
- plasma triglyceride levels
- cryopreserved human hepatocytes
- human DGAT2
- triglyceride synthesis
- de novo lipogenesis
- hepatic SREBP signaling
- liver triglyceride content
- Inhibitor
- inhibitor
- inhibit