Description
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
Product information
CAS Number: 1221971-47-6
Molecular Weight: 461.32
Formula: C21H14Cl2N2O4S
Chemical Name: N-{3',4'-dichloro-[1,1'-biphenyl]-4-yl}-4-hydroxy-1,1-dioxo-2H-1λ⁶,2-benzothiazine-3-carboxamide
Smiles: OC1=C(NS(=O)(=O)C2=CC=CC=C21)C(=O)NC1=CC=C(C=C1)C1=CC=C(Cl)C(Cl)=C1
InChiKey: VGACSWBJQLLJFB-UHFFFAOYSA-N
InChi: InChI=1S/C21H14Cl2N2O4S/c22-16-10-7-13(11-17(16)23)12-5-8-14(9-6-12)24-21(27)19-20(26)15-3-1-2-4-18(15)30(28,29)25-19/h1-11,25-26H,(H,24,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects up to 100 μM. PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells. PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays. PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM).
In Vivo:
PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.