WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522526
Description: PF-9184 is a potent and selective mPGES-1 inhibitor. PF-9184 potently inhibited recombinant human (rh) mPGES-1 (IC(50)=16.5+/-3.8nM), and had no effect against rhCOX-1 and rhCOX-2 (>6500-fold selectivity). PF-9184 inhibited PGE(2) synthesis (IC(50) in the range of 0.5-5 microM in serum-free cell and human whole blood cultures, respectively) while sparing the synthesis of 6-keto-PGF(1alpha) (PGF(1alpha)) and PGF(2alpha).
MedKoo Cat#: 522526
Chemical Formula: C21H14Cl2N2O4S
Exact Mass: 460.0051
Molecular Weight: 461.31
Elemental Analysis: C, 54.68; H, 3.06; Cl, 15.37; N, 6.07; O, 13.87; S, 6.95
Synonym: PF-9184; PF9184; PF 9184.
IUPAC/Chemical Name: N-(3',4'-Dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide
InChi Key: VGACSWBJQLLJFB-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(C1=C(O)C2=CC=CC=C2S(N1)(=O)=O)NC3=CC=C(C4=CC=C(Cl)C(Cl)=C4)C=C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 461.31 Batch specific molecular weights may vary from batch to batch due to the degree 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||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Mbalaviele G, Pauley AM, Shaffer AF, Zweifel BS, Mathialagan S, Mnich SJ,
Nemirovskiy OV, Carter J, Gierse JK, Wang JL, Vazquez ML, Moore WM, Masferrer JL.
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. 2010 May 15;79(10):1445-54. doi: 10.1016/j.bcp.2010.01.003.
Epub 2010 Jan 11. PubMed PMID: 20067770.
Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheumatoid arthritis and inflammatory pain, largely attributed to the inhibition of PGE(2) synthesis, provides a rationale for exploring mPGES-1 inhibition as a potential novel therapy for these diseases.