344930-95-6
344930-95-6 structure
- Name: SSR 69071
- Chemical Name: 6-methoxy-1,1-dioxo-2-[[4-oxo-9-(2-piperidin-1-ylethoxy)pyrido[1,2-a]pyrimidin-2-yl]oxymethyl]-4-propan-2-yl-1,2-benzothiazol-3-one
- CAS Number: 344930-95-6
- Molecular Formula: C27H32N4O7S
- Molecular Weight: 556.63100
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Elastase
- Create Date: 2019-01-03 01:56:22
- Modify Date: 2025-08-23 11:16:39
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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].
| Name | 6-methoxy-1,1-dioxo-2-[[4-oxo-9-(2-piperidin-1-ylethoxy)pyrido[1,2-a]pyrimidin-2-yl]oxymethyl]-4-propan-2-yl-1,2-benzothiazol-3-one |
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| Synonyms | hms3269m07 |
| 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]. |
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| Related Catalog | |
| 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]. |
| 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]. 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. |
| References |
[3]. Márton Varga, et al. A novel orally active inhibitor of HLE. Eur J Med Chem. 2003 Apr;38(4):421-5. |
| Molecular Formula | C27H32N4O7S |
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| Molecular Weight | 556.63100 |
| Exact Mass | 556.19900 |
| PSA | 128.13000 |
| LogP | 3.82880 |