PF-9184

Product Name: PF-9184
CAS No.: 1221971-47-6
Chemical Name: PF-9184
Synonyms: PF-9184;PF-03549184;PF9184,PF 9184;N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide;2H-1,2-Benzothiazine-3-carboxamide, N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-, 1,1-dioxide;N-(3',4'-dichloro-[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-benzo[e][1,2]thiazine-3-carboxamide 1,1-dioxide
CBNumber: CB43067570
Molecular Formula: C21H14Cl2N2O4S
Formula Weight: 461.32
MOL File: 1221971-47-6.mol

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PF-9184 Property

Melting point:: 285.5-289.3 °C
Density: 1.574±0.06 g/cm3(Predicted)
storage temp.: 2-8°C
solubility: ≤15mg/ml in DMSO;20mg/ml in dimethyl formamide
pka: 4.50±1.00(Predicted)
form: powder
color: white to beige

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: PZ0326
Product name: PF-03549184
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $108
Updated: 2024/03/01

Sigma-Aldrich

Product number: PZ0326
Product name: PF-03549184
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $348
Updated: 2024/03/01

Cayman Chemical

Product number: 18904
Product name: PF-9184
Purity: ≥98%
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 18904
Product name: PF-9184
Purity: ≥98%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 18904
Product name: PF-9184
Purity: ≥98%
Packaging: 10mg
Price: $151
Updated: 2024/03/01

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PF-9184 Chemical Properties,Usage,Production

Description

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H₂ (PGH₂; ) into the biologically active PGE₂ . Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. PF-9184 is a potent inhibitor of mPGES-1 (IC₅₀ = 16.5 nM for recombinant human enzyme). It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE₂ in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC₅₀s = 0.4-5 μM).

Uses

PF 9184 is a?microsomal prostaglandin E?synthase-1(mPGES-1) inhibitor. mPGES-1is an enzyme induced during the inflammatory response and it is an attractive target for developing anti-inflammatory drugs.

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].

Enzyme inhibitor

This potent mPGES-1 inhibitor (FW = 461.32 g/mol; CAS 1221971-47-6; Solubility: 100 mM in DMSO), also named N-[3',4'-dichloro(1,1'- biphenyl)yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide), targets human and rat microsomal prostaglandin E synthase 1, with respective IC50 values of 16.5 nM and 1.08 μM, exhibiting >6500x selectivity toward mPGES-1 versus COX1 and COX2. PF-9184 inhibits IL- 1β-induced PGE2 synthesis in vitro. In inflammation and clinically relevant biological systems, mPGES-1 expression, like COX-2 expression is induced in cell context- and time-dependent manner, a behavior that is fully consistent with the kinetics of PGE2 synthesis

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.

PF-9184 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-9184 Suppliers

China 20 India 2 United Kingdom 2 United States 6 Global 30

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1221971-47-6, PF-9184Related Search:

PF-9184

N-[3',4'-Dichloro(1,1'-biphenyl)-yl]-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide

PF-03549184

2H-1,2-Benzothiazine-3-carboxamide, N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-, 1,1-dioxide

PF9184,PF 9184

N-(3',4'-dichloro-[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-benzo[e][1,2]thiazine-3-carboxamide 1,1-dioxide

1221971-47-6