| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml; Ethanol: 5 mg/ml | [form ]
A crystalline solid | [pka]
15.05±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
PF-4693627 is a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. | [Uses]
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]. | [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. |
| [storage]
Store at -20°C | [References]
[1] Arhancet GB, et al. Discovery and SAR of PF-4693627, a potent, selective and orally bioavailable mPGES-1 inhibitor for the potential treatment of inflammation. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1114-9. DOI:10.1016/j.bmcl.2012.11.109 |
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| Company Name: |
cjbscvictory
|
| Telephone: |
13348960310 13348960310 |
| Website: |
www.weikeqi-biotech.com/ |
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