PF-4693627
Based on 1 Customer Validation
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
For research use only. We do not sell to patients.
- Purity: 99.63%
- CAS No.: 1312815-93-2
- Formula: C26H29Cl2N3O3
- Molecular Weight:502.43
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Storage: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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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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Targeted Diversity Library
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Chemokine Compound Library
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Heterocyclic Compound Library
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Anti-Rheumatic Arthritis Compound Library
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Immunology/Inflammation Compound Library
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Biological Activity
IC50: 3 nM (mPGES-1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Fibroblast | IC50 |
>10 μM
Compound: 26, PF-4693627
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Inhibition of COX2 in human fetal fibroblast cells assessed as PGF2alpha level after 50 mins by ELISA
Inhibition of COX2 in human fetal fibroblast cells assessed as PGF2alpha level after 50 mins by ELISA
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[PMID: 23260349] |
| Fibroblast | IC50 |
0.006 μM
Compound: 26, PF-4693627
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Inhibition of mPGES-1 in human fetal fibroblast cells assessed as PGF2alpha level after 50 mins by ELISA
Inhibition of mPGES-1 in human fetal fibroblast cells assessed as PGF2alpha level after 50 mins by ELISA
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[PMID: 23260349] |
PF-4693627 also inhibits mPGES-1 with IC50s of 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively[1].
PF-4693627 shows high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-4693627 (1.0 mg/kg; i.v.) shows good bioavailability (59%) and modest half life (t1/2=3.7 h) in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Guinea pig with carrageenan stimulated air pouch inflammation model[1]
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Dosage:10 mg/kg
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Administration:Administered orally
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Result:63% PGE2 inhibition.
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Animal Model:Sprague-Dawley rats[1].
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Dosage:1.0 mg/kg (Pharmacokinetic Analysis)
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Administration:Administered i.v.
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Result:Clearance (CL), volume of distribution (Vdss), t1/2, mean residence time (MRT) and bioavailability (F) is 12 mL/min/kg, 3.0 L/kg, 3.7 h, 4.42 h, 59%, respectively.
Chemical Information
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CAS No. 1312815-93-2
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Appearance Solid
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Molecular Weight 502.43
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Formula C26H29Cl2N3O3
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Color White to off-white
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SMILES
O=C(C1CCN(C2=NC3=CC(Cl)=C(C4=CC=C(Cl)C=C4)C=C3O2)CC1)N[C@@H]5C[C@@H](CO)CCC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (199.03 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)
Purity & Documentation
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Data Sheet (281 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
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 | 1.9903 mL | 9.9516 mL | 19.9033 mL | 49.7582 mL |
| 5 mM | 0.3981 mL | 1.9903 mL | 3.9807 mL | 9.9516 mL | |
| 10 mM | 0.1990 mL | 0.9952 mL | 1.9903 mL | 4.9758 mL | |
| 15 mM | 0.1327 mL | 0.6634 mL | 1.3269 mL | 3.3172 mL | |
| 20 mM | 0.0995 mL | 0.4976 mL | 0.9952 mL | 2.4879 mL | |
| 25 mM | 0.0796 mL | 0.3981 mL | 0.7961 mL | 1.9903 mL | |
| 30 mM | 0.0663 mL | 0.3317 mL | 0.6634 mL | 1.6586 mL | |
| 40 mM | 0.0498 mL | 0.2488 mL | 0.4976 mL | 1.2440 mL | |
| 50 mM | 0.0398 mL | 0.1990 mL | 0.3981 mL | 0.9952 mL | |
| 60 mM | 0.0332 mL | 0.1659 mL | 0.3317 mL | 0.8293 mL | |
| 80 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6220 mL | |
| 100 mM | 0.0199 mL | 0.0995 mL | 0.1990 mL | 0.4976 mL |
PF-4693627 Related Classifications
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