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PF-9184

目录号 : GC15351

A potent mPGES-1 inhibitor

PF-9184 Chemical Structure

Cas No.:1221971-47-6

规格 价格 库存 购买数量
1mg
¥619.00
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5mg
¥1,522.00
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10mg
¥2,126.00
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25mg
¥4,521.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

PF-9184 is a novel mPGES-1 inhibitor [1]. Microsomal prostaglandin E synthase-1 (mPGES-1) is an inducible terminal isomerase expressed in cytokine-sensitive brain endothelial cells. mPGES-1 functions as the central switch during immune-induced pyresis and as a target for treatment of fever and other PGE2-dependent acute phase reactions elicited by the brain [2]. mPGES-1 has been incolved in the formation of PGE2 essential for pain hypersensitivity and inflammation. Microsomal prostaglandin E synthase-1 (mPGES-1) has been involved in converting the COX product prostaglandin H2 (PGH2) into the biologically active PGE2[3].

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].

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.

Chemical Properties

Cas No. 1221971-47-6 SDF
化学名 N-​(3',​4'-​dichloro[1,​1'-​​biphenyl]​-​4-​​yl)​-​4-​​hydroxy-​2H-​1,​2-​​benzothiazine-​​3-​carboxamide 1,​1-​​dioxide
Canonical SMILES OC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O
分子式 C21H14Cl2N2O4S 分子量 461.3
溶解度 ≤15mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
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1 mM 2.1678 mL 10.8389 mL 21.6779 mL
5 mM 0.4336 mL 2.1678 mL 4.3356 mL
10 mM 0.2168 mL 1.0839 mL 2.1678 mL
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