PF-9184 - CAS:1221971-47-6

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PF-9184

目录号 : KCM10727 CAS No. : 1221971-47-6 纯度 : ≥98%

Data Sheet 产品使用指南

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H (PGH; ) into the biologically active PGE . 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 (IC = 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 PGE in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (ICs = 0.4-5 µM).

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.

体外研究

PF-9184 (0.015-100 μM; 24 hours) inhibits IL-1β-stimulated prostaglandin E2 (PGE2) synthesis in rheumatoid arthritis (RASF) in synovial fibroblasts derived from patients and has no apparent cytotoxic effects up to 100 μM.

PF-9184 (0.015-100 μM) potently blocks mPGES-1 ability to synthesize PGE2 from PGH2, and with no apparent inhibitory effects on COX-2 and prostacyclin synthase in cells.

PF-9184 (0.015-100 μM) inhibits PGE2 weakly but has no effect on TXB2 synthesis except at 100 μM in human whole blood and modified blood assays.

PF-9184 is a poor inhibitor of recombinant rat mPGES-1 (IC50=1080±398 nM).

体内研究

PF-9184 (oral administration or even local delivery) has no effect on PGE2 synthesis in recombinant rats.

分子式

C₂₁H₁₄Cl₂N₂O₄S

分子量

461.32

CAS号

1221971-47-6

中文名称

N-(3',4'-二氯[1,1'-联苯]-4-基)-4-羟基-2H-1,2-苯并噻嗪-3-甲酰胺 1,1-二氧化物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据

In Vitro:

DMSO: ≥ 100 mg/mL (216.77 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1677 mL	10.8385 mL	21.6769 mL
5 mM	0.4335 mL	2.1677 mL	4.3354 mL
10 mM	0.2168 mL	1.0838 mL	2.1677 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

纯度： ≥98%