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Merck
CN
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主要文件

安全信息

PZ0326

Sigma-Aldrich

PF-03549184

≥98% (HPLC)

别名:

N-(3′,4′-dichloro[1,1′-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide, PF-9184

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About This Item

经验公式（希尔记法）:
C21H14Cl2N2O4S
CAS号:
1221971-47-6
分子量:
461.32
UNSPSC代码:
12352202
NACRES:
NA.77

质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear (warmed)

储存温度

2-8°C

InChI

1S/C21H14Cl2N2O4S/c22-16-10-7-13(11-17(16)23)12-5-8-14(9-6-12)25-19(21(24)27)20(26)15-3-1-2-4-18(15)30(25,28)29/h1-11,26H,(H2,24,27)

InChI key

YGTUCAUHSJOJCQ-UHFFFAOYSA-N

生化/生理作用

PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its expression is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC50 ranges from 0.5 to 5 μM. IC50 concentrations for rhCOX1 and rHCOX2 are 118 μM and 236 μM, respectively.
PGE2 is involved in inflammation and is one of the most abundant prostanoid.

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H315,H319,H335

危险分类

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

靶器官

Respiratory system

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
066M4713V

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Gabriel Mbalaviele et al.
Biochemical pharmacology, 79(10), 1445-1454 (2010-01-14)
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
Hui-Hua Chang et al.
Future medicinal chemistry, 3(15), 1909-1934 (2011-10-26)
Microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal synthase responsible for the synthesis of the pro-tumorigenic prostaglandin E(2) (PGE(2)). mPGES-1 is overexpressed in a wide variety of cancers. Since its discovery in 1997 by Bengt Samuelsson and collaborators, the enzyme

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