추천 제품
Quality Level
분석
≥98% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 5 mg/mL, clear (warmed)
저장 온도
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
생화학적/생리학적 작용
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.
신호어
Warning
유해 및 위험 성명서
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
표적 기관
Respiratory system
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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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