A potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme); selective for human neutrophil elastase over rat

SSR 69071 – 10 mg

Brand:
Cayman
CAS:
344930-95-6
Storage:
-20
UN-No:
Non-Hazardous - /

SSR 69071 is a potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme).{35315} It is selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively). It inhibits human neutrophil elastase ex vivo in mouse bronchoalveolar lavage (BAL) fluid (ED50 = 10.5 mg/kg, p.o.). In vivo, SSR 69071 (2.8 mg/kg, p.o.) reduces acute lung hemorrhage induced by human neutrophil elastase in mice. It reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively). SSR 69071 also reduces cardiac infarct size when administered prior to ischemia or reperfusion in a rabbit model of ischemia-reperfusion injury.{35314}  

 

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Description

A potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme); selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively); inhibits human neutrophil elastase ex vivo in mouse BAL fluid (ED50 = 10.5 mg/kg, p.o.); reduces acute lung hemorrhage induced by human neutrophil elastase in mice (2.8 mg/kg, p.o.); reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively); reduces cardiac infarct size in a rabbit model of ischemia-reperfusion injury,

Formal name: 2-[[6-methoxy-4-(1-methylethyl)-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl]methoxy]-9-[2-(1-piperidinyl)ethoxy]-4H-pyrido[1,2-a]pyrimidin-4-one

Synonyms: 

Molecular weight: 556.6

CAS: 344930-95-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Immunology & Inflammation|Innate Immunity

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