产品名称

PF-03549184

一般描述

PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1).

别 称

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

纯 度

≥98.0%(HPLC)

CAS NO.

1221971-47-6

分子式

C²¹H¹⁴Cl²N²O⁴S

分子量

461.32

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至米色固体

溶解性(25℃)

DMSO

~5mg/mL(warmed)

l  生物学信息

生物活性/药理作用

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  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.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.  https://www.ncbi.nlm.nih.gov