PF-4693627

Name: PF-4693627
Brand: TargetMol
SKU: T16504
Rating: 4.5 (1 reviews)

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Catalog No. T16504Cas No. 1312815-93-2

PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).

PF-4693627

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Catalog No. T16504Cas No. 1312815-93-2

Pack Size	Price	USA Warehouse	Global Warehouse
500 μg	$133	35 days	35 days
1 mg	$246	35 days	35 days
5 mg	$1,150	35 days	35 days
10 mg	$2,160	35 days	35 days

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
Targets&IC50	mPGES-1:3 nM
In vitro	PF-4693627 displays high activity in lipopolysaccharide (LPS) stimulated human whole blood (HWB) cell assay (IC50=109 nM). PF-4693627 also inhibits mPGES-1 (IC50s: 180 and 6 nM in HWB-1483 and human fetal fibroblast, respectively).
In vivo	PF-4693627 (1.0 mg/kg; i.v.) displays good bioavailability (59%) and modest half-life (t1/2=3.7 h) in Sprague-Dawley rats. PF-4693627 (10 mg/kg; orally) suppresses 63% of PGE2 production relative to vehicle control in the Guinea pig carrageenan stimulated air pouch model[1].

Chemical Properties

Molecular Weight	502.43
Formula	C₂₆H₂₉Cl₂N₃O₃
Cas No.	1312815-93-2
Smiles	ClC=1C=C2C(OC(=N2)N3CCC(C(N[C@@H]4C[C@@H](CO)CCC4)=O)CC3)=CC1C5=CC=C(Cl)C=C5
Relative Density.	1.38 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc