PF 9184

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Cat.No. 5917 - PF 9184 | C21H14Cl2N2O4S | CAS No. 1221971-47-6
Description: Potent microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor
Chemical Name: N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor (IC50 values are 16.5 and 1080 nM for human and rat mPGES-1, respectively). Exhibits >6500-fold selectivity for mPGES-1 over COX-1 and COX-2. Inhibits IL-1β-induced PGE2 synthesis in vitro.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 461.32
Formula C21H14Cl2N2O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1221971-47-6
PubChem ID 54728414
InChI Key VGACSWBJQLLJFB-UHFFFAOYSA-N
Smiles OC2=C(C(NC3=CC=C(C4=CC=C(Cl)C(Cl)=C4)C=C3)=O)NS(C1=CC=CC=C12)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.13 100

Preparing Stock Solutions

The following data is based on the product molecular weight 461.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.17 mL 10.84 mL 21.68 mL
5 mM 0.43 mL 2.17 mL 4.34 mL
10 mM 0.22 mL 1.08 mL 2.17 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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References

References are publications that support the biological activity of the product.

Mbalaviele et al (2010) Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor. Biochem.Pharmacol. 79 1445 PMID: 20067770


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