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PF-9184

Catalog No.
C3475
microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor
Grouped product items
SizePriceStock Qty
5mg
$117.00
Ship with 5-10 days
10mg
$163.00
Ship with 5-10 days
25mg
$348.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

PF-9184 is a novel mPGES-1 inhibitor [1]. Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal isomerase expressed in cytokine-sensitive brain endothelial cells. mPGES-1 functions as the central switch during immune-induced pyresis and as a target for treatment of fever and other PGE2-dependent acute phase reactions elicited by the brain [2]. mPGES-1 has been incolved in the formation of PGE2 essential for pain hypersensitivity and inflammation. Microsomal prostaglandin E synthase-1 (mPGES-1) has been involved in converting the COX product prostaglandin H2 (PGH2) into the biologically active PGE2[3].

In vitro: PF-9184 potently inhibited recombinant human mPGES-1 with an IC50 value of 16.5 ± 3.8 nM. PF-9184 showed no effect on rhCOX-1 and rhCOX-2 with >6500-fold selectivity. In rationally designed cell systems, PF-9184 inhibited PGE2 synthesis with IC50 in the range of 0.5–5 μM in serum-free cell and human whole blood cultures, while sparing the synthesis of 6-keto-PGF1α (PGF1α) and PGF2α[1]. PF-9184 showed no apparent cytotoxic effects up to 100 μM [1].

References:
[1] Mbalaviele G, Pauley A M, Shaffer A F, et al.  Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor[J]. Biochemical pharmacology, 2010, 79(10): 1445-1454.
[2] Engblom D, Saha S, Engstrm L, et al.  Microsomal prostaglandin E synthase-1 is the central switch during immune-induced pyresis[J]. Nature neuroscience, 2003, 6(11): 1137-1138.
[3] Jakobsson P J, Thorén S, Morgenstern R, et al.  Identification of human prostaglandin E synthase: a microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target[J]. Proceedings of the National Academy of Sciences, 1999, 96(13): 7220-7225.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt461.3
Cas No.1221971-47-6
FormulaC21H14Cl2N2O4S
Solubility≤15mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical NameN-​(3',​4'-​dichloro[1,​1'-​​biphenyl]​-​4-​​yl)​-​4-​​hydroxy-​2H-​1,​2-​​benzothiazine-​​3-​carboxamide 1,​1-​​dioxide
SDFDownload SDF
Canonical SMILESOC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

PF-9184