1. Metabolic Enzyme/Protease
  2. Elastase
  3. SSR69071

SSR69071 

Cat. No.: HY-103445
Handling Instructions

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases.

For research use only. We do not sell to patients.

SSR69071 Chemical Structure

SSR69071 Chemical Structure

CAS No. : 344930-95-6

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Description

SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury[1]. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases[2].

In Vitro

SSR69071 is a potent inhibitor of human leukocyte elastase (HLE), with the inhibition constant (Ki) and the constant for inactivation process (kon) being 0.0168±0.0014 nM and 0.183±0.013 106/mol sr, respectively[2].
SSR69071 is a potent, competitive and slow tight binding inhibitor of HLE in vitro with a Ki value of 16.8 pM[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SSR69071 (3 mg/kg i.v.) reduces cardiac infarct size when administered before ischemia or just prior to reperfusion[1].

Treatment with SSR69071 (3 mg/kg i.v.) just prior to reperfusion significantly reduces cardiac elastase activity[1].
Bronchoalveolar lavage fluid from mice orally treated with SSR69071 inhibits HLE (ex vivo), and in this model, SSR69071 has a dose-dependent efficacy with an ED50=10.5 mg/kg p.o. SSR69071 decreases significantly the acute lung hemorrhage induced by HLE (ED50=2.8 mg/kg p.o.) in mice[2]. SSR69071 prevents carrageenan- (ED30=2.2 mg/kg) and HLE-induced (ED30=2.7 mg/kg) paw edema in rats after p.o. administration[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male New Zealand white rabbits weighing 2-3 kg[1]
Dosage: 3 mg/kg (dissolved in methane sulphonic acid before being diluted in 0.9% saline)
Administration: Administered i.v.
Result: Treatment just prior to reperfusion significantly reduced cardiac elastase activity.
Molecular Weight

556.63

Formula

C27H32N4O7S

CAS No.
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SSR69071
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HY-103445
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