Catalog Number: 2506
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.
Background References
  1. SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury.
    Bidouard et al.
    Eur.J.Pharmacol., 2003;461:49
  2. A novel orally active inhibitor of HLE.
    Varga et al.
    Eur.J.Med.Chem., 2003;38:421
  3. 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 ela
    Kapui et al.
    J.Pharmacol.Exp.Ther., 2003;305:451
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SSR 69071 include:

2 Citations: Showing 1 - 2
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  1. Solar ultraviolet irradiation induces decorin degradation in human skin likely via neutrophil elastase.
    Authors: Li Et al.
    PLoS One 2013;8:e72563
  2. Pivotal role for alpha1-antichymotrypsin in skin repair.
    Authors: Hoffmann Et al.
    J Biol Chem 2011;286:28889

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