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.
For research use only. We do not sell to patients.
- Purity: 99.08%
- CAS No.: 3036158-98-9
- Formula: C16H19ClF2N2O4S
- Molecular Weight:408.85
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Storage:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
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Orally Active Compound Library
HY-L061
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Anti-Liver Cancer Compound Library
HY-L101
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 3036158-98-9
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Appearance Solid
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Molecular Weight 408.85
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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, 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 |
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