R&D Systems Inc. Tocris Bioscience Boston Biochem

SSR 69071

Cat. No. 2506

SSR 69071 C27H32N4O7S [344930-95-6]

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Chemical 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

Biological Activity

High affinity, potent inhibitor of human leukocyte elastase (HLE) (IC50 = 3.9 nM). Displays species-selectivity (Ki values are 0.017, 1.70, 3.01, 58 and > 100 nM  for human, mouse, rat, rabbit and porcine elastase respectively). Inhibits HLE-induced lung hemorrhage in mice (ID50 = 2.8 mg/kg) and reduces infarct size in an in vivo acute model of coronary ischemia-reperfusion injury. Orally active.

Technical Data

M.Wt:
556.63
Formula:
C27H32N4O7S
Solubility:
Soluble to 10 mM in ethanol and to 25 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
344930-95-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Bidouard et al (2003) SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury. Eur.J.Pharmacol. 461 49. PMID: 12568915.

Kapui et al (2003) Biochemical and pharmacological characterization of 2-(9-(2-Piperidinoethoxy)-4-oxo-4H-pyrido[1,2-α]pyrimidin-2-yloxymethyl)-4-(1-methylethyl)-6-methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (SSR69071), a novel, orally active elastase inhibitor. J.Pharmacol.Exp.Ther. 305 451. PMID: 12606659.

Varga et al (2003) A novel orally active inhibitor of HLE. Eur.J.Med.Chem. 38 421. PMID: 12750030.

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Keywords: SSR 69071, supplier, Potent, orally, active, human, leukocyte, elastase, inhibitors, Neutrophil, Proteinases, Proteases, SSR69071, HLE, inhibitor

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