Pirinixic Acid Aminothiazole is a dual inhibitor of 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase 1 (mPGES-1) with IC50 values of 0.3 and 0.4 μM, respectively . 5-lipoxygenase (5-LO) and microsomal prostaglandin E2 synthase-1 (mPGES-1) are critical enzymes involved in the metabolism of arachidonic acid (AA). They are key enzymes in the synthesis of leukotrienes (LTs) and PGE2, respectively . Dual inhibition of 5-LO and mPGES-1 is currently pursued as potential pharmacological strategy for treatment of inflammation and cancer . Pirinixic Acid Aminothiazole is a dual inhibitor of 5-LO and mPGES-1. Pirinixic Acid Aminothiazole hardly inhibited cyclooxygenase (COX)-1/2 activities and failed to inhibit 12/15-LOs. In cell-free assay, Pirinixic Acid Aminothiazole was highly potent against both 5-LO and mPGES-1 with IC50 values of 0.3 and 0.4 μM, respectively. In the cell-based assay, Pirinixic Acid Aminothiazole inhibited 5-LO directly with IC50 value of 0.2 μM . In zymosan-induced peritonitis in mice, Pirinixic Acid Aminothiazole (10 mg/kg) reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%, accompanied by significantly impaired levels of cysLTs (84% reduction) and PGE2 (46% reduction). These results suggested that Pirinixic Acid Aminothiazole dually inhibited LT and PGE2 synthesis in vivo connected to anti-inflammatory effectiveness .

Product information

CAS Number: 1492060-44-2

Molecular Weight: 513.07

Formula: C25H25ClN4O2S2

Chemical Name: 2-[(4-chloro-6-{[4-(naphthalen-2-yl)-1,3-thiazol-2-yl]amino}pyrimidin-2-yl)sulfanyl]octanoic acid

Smiles: CCCCCCC(SC1N=C(Cl)C=C(NC2=NC(=CS2)C2C=C3C=CC=CC3=CC=2)N=1)C(O)=O

InChiKey: BADFIDKPYNKNRT-UHFFFAOYSA-N

InChi: InChI=1S/C25H25ClN4O2S2/c1-2-3-4-5-10-20(23(31)32)34-25-28-21(26)14-22(30-25)29-24-27-19(15-33-24)18-12-11-16-8-6-7-9-17(16)13-18/h6-9,11-15,20H,2-5,10H2,1H3,(H,31,32)(H,27,28,29,30)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.