A dual inhibitor of mPGES-1 (IC50 = 3.9 μM ) and 5-LO (IC50 = 4.1 μM); blocks PGE2 and LT synthesis in cell free and intact cell assays

YS-121 – 10 mg

Brand:
Cayman
CAS:
916482-17-2
Storage:
-20
UN-No:
De Minimis - 1231 / 3

Microsomal prostaglandin E2 synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever, and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. YS-121 is a dual inhibitor of mPGES-1 (IC50 = 3.9 μM){16667} and 5-LO (IC50 = 4.1 μM).{17994} It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. Moreover, YS-121 (1.5 mg/kg, intraperitoneal) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy.{17751} YS-121 has minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively, at 10 μM.{16667}  

 

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Description

A dual inhibitor of mPGES-1 (IC50 = 3.9 μM ) and 5-LO (IC50 = 4.1 μM); blocks PGE2 and LT synthesis in cell free and intact cell assays, and also in an animal model of inflammation

Formal name: 2-[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-octanoic acid

Synonyms: 

Molecular weight: 408

CAS: 916482-17-2

Purity: ≥98%

Formulation: A solution in methyl acetate

Product Type|Biochemicals|Small Molecule Inhibitors|Cyclooxygenases||Product Type|Biochemicals|Small Molecule Inhibitors|Lipoxygenases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Leukotrienes||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Immunology & Inflammation|Innate Immunity

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