1312815-93-2
1312815-93-2 structure
- Name: PF-4693627
- Chemical Name: 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)- 3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide
- CAS Number: 1312815-93-2
- Molecular Formula: C26H29Cl2N3O3
- Molecular Weight: 502.433
- Catalog: Signaling Pathways Immunology/Inflammation PGE synthase
- Create Date: 2018-06-28 10:03:35
- Modify Date: 2025-08-26 21:35:37
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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)[1].
| Name | 1-[5-chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)- 3-(hydroxymethyl)cyclohexyl]piperidine-4-carboxamide |
|---|---|
| Synonyms |
1-[5-Chloro-6-(4-chlorophenyl)-1,3-benzoxazol-2-yl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide
4-Piperidinecarboxamide, 1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]- |
| Description | 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)[1]. |
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| Related Catalog | |
| Target |
IC50: 3 nM (mPGES-1)[1] |
| In Vitro | 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]. |
| In Vivo | PF-4693627 (10 mg/kg; orally) inhibits 63% of PGE2 production relative to vehicle control in Guinea pig carrageenan stimulated air pouch model[1]. 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]. Animal Model: Guinea pig with carrageenan stimulated air pouch inflammation model[1] Dosage: 10 mg/kg Administration: Administered orally Result: 63% PGE2 inhibition. Animal Model: Sprague-Dawley rats[1]. Dosage: 1.0 mg/kg (Pharmacokinetic Analysis) Administration: Administered i.v. 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. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C26H29Cl2N3O3 |
| Molecular Weight | 502.433 |
| Exact Mass | 501.158600 |
| PSA | 78.60000 |
| LogP | 4.84 |
| Index of Refraction | 1.659 |