PF-07853578
Based on 1 Customer Validation
PF-07853578 is an orally active PNPLA3 modulator. PF-07853578 significantly reduces human PNPLA3-I148M protein levels and effectively decreases hepatic triglyceride content by reducing this mutant protein. PNPLA3 degrader-1 can be used in the research of liver cirrhosis and hepatocellular carcinoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.08%
- CAS. Nr.: 3036158-98-9
- Formel: C16H19ClF2N2O4S
- Molecular Weight:408.85
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Speicherung:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
PF-07853578 (Example 11) exhibits EC50 values of 5 nM (lipid droplet localization assay) and 8 nM (Western blot assay) against hPNPLA3-I148M in human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BAC-TG transgenic mice fed a high-sucrose diet[1]
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Dosage:30 mg/kg
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Administration:diet administration; 14 days
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Result:Reduced human PNPLA3 protein levels by 86.1%. The reduction in hPNPLA3-I148M led to a 61.6% decrease in hepatic triglycerides.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 3036158-98-9
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Appearance Solid
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Molecular Weight 408.85
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Formel C16H19ClF2N2O4S
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Color White to off-white
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SMILES
O=S1(N(CC[C@H]1C)[C@H]2CN(CC(F)(C2)F)C(OC3=CC=C(C=C3)Cl)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (244.59 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4459 mL | 12.2294 mL | 24.4588 mL | 61.1471 mL |
| 5 mM | 0.4892 mL | 2.4459 mL | 4.8918 mL | 12.2294 mL | |
| 10 mM | 0.2446 mL | 1.2229 mL | 2.4459 mL | 6.1147 mL | |
| 15 mM | 0.1631 mL | 0.8153 mL | 1.6306 mL | 4.0765 mL | |
| 20 mM | 0.1223 mL | 0.6115 mL | 1.2229 mL | 3.0574 mL | |
| 25 mM | 0.0978 mL | 0.4892 mL | 0.9784 mL | 2.4459 mL | |
| 30 mM | 0.0815 mL | 0.4076 mL | 0.8153 mL | 2.0382 mL | |
| 40 mM | 0.0611 mL | 0.3057 mL | 0.6115 mL | 1.5287 mL | |
| 50 mM | 0.0489 mL | 0.2446 mL | 0.4892 mL | 1.2229 mL | |
| 60 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0191 mL | |
| 80 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 100 mM | 0.0245 mL | 0.1223 mL | 0.2446 mL | 0.6115 mL |
PF-07853578 Related Classifications
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