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SSR 69071

Cat. No. 2506

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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 (K_i 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 40 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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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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Elastase

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