A competitive sPLA2-IIA inhibitor with IC50 values of 80

YM-26734 – 10 mg

Brand:
Cayman
CAS:
144337-18-8
Storage:
-20
UN-No:
Non-Hazardous - /

Secreted phospholipases A2 (sPLA2s) are a diverse family of low molecular weight PLA2s with tissue-specific expression patterns and actions.{23479} The group IIA sPLA2 (sPLA2-IIA) was originally purified from platelets and exudates from patients with rheumatoid arthritis.{23479} Its expression can be induced by inflammatory mediators, and mouse studies suggest that it may play roles in colorectal polyposis, atherosclerosis, and bacterial infections.{23479,23478} YM-26734 is a derivative of a compound isolated from the fruit of H. amygdaline that competitively inhibits rabbit platelet sPLA2 with an IC50 value of 85 nM.{28705} It inhibits sPLA2-hGIIA, -mGIIA, -rGIIA, -hGV, -mGV, -hGX, and -mGX with IC50 values of 80, 30, 120, 110, 520, >1600, and >1600 nM, respectively.{28706,28707} YM-26734 displays minimal activity at cytosolic PLA2, COX and lipoxygenase.{28705} At 45 µg/ear or 11 mg/kg i.v., YM-26734 has been used to ameliorate local inflammatory responses in TPA-induced mouse ear edema.{28705}  

 

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Description

A competitive sPLA2-IIA inhibitor with IC50 values of 80, 30, 120, 110, 520, >1600, and >1600 nM for sPLA2-hGIIA, -mGIIA, -rGIIA, -hGV, -mGV, -hGX, and -mGX, respectively; ameliorates local inflammatory responses in TPA-induced mouse ear edema at 45 µg/ear or 11 mg/kg i.v.

Formal name: 1,1′-[5-[3,4-dihydro-7-hydroxy-2-(4-hydroxyphenyl)-2H-1-benzopyran-4-yl]-2,4,6-trihydroxy-1,3-phenylene]bis-1-dodecanone

Synonyms: 

Molecular weight: 731

CAS: 144337-18-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Immunology & Inflammation||Research Area|Lipid Biochemistry|Glycerophospholipids|Phospholipases

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