1. Immunology/Inflammation
  2. PGE synthase
  3. PF-4693627

PF-4693627 

Cat. No.: HY-125415
Handling Instructions

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.

PF-4693627 Chemical Structure

PF-4693627 Chemical Structure

CAS No. : 1312815-93-2

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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].

IC50 & 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.
Molecular Weight

502.43

Formula

C₂₆H₂₉Cl₂N₃O₃

CAS No.

1312815-93-2

SMILES

O=C(C1CCN(C2=NC3=CC(Cl)=C(C4=CC=C(Cl)C=C4)C=C3O2)CC1)N[[email protected]@H]5C[[email protected]@H](CO)CCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PF-4693627PF4693627PF 4693627PGE synthaseProstaglandin E synthasemPGES-1orallybioavailableinflammationosteoarthritisrheumatoidarthritisInhibitorinhibitorinhibit

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