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.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 556.63. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.8 mL||8.98 mL||17.97 mL|
|5 mM||0.36 mL||1.8 mL||3.59 mL|
|10 mM||0.18 mL||0.9 mL||1.8 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
References are publications that support the products' biological activity.
Bidouard et al (2003) SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury. Eur.J.Pharmacol. 461 49 PMID: 12568915
Varga et al (2003) A novel orally active inhibitor of HLE. Eur.J.Med.Chem. 38 421 PMID: 12750030
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 ela J.Pharmacol.Exp.Ther. 305 451 PMID: 12606659
If you know of a relevant reference for SSR 69071, please let us know.
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Keywords: SSR 69071, supplier, Potent, orally, active, human, leukocyte, elastase, inhibitors, inhibits, Neutrophil, Proteinases, Proteases, SSR69071, HLE, inhibitor, Elastase, Elastase, Tocris Bioscience
3 Citations for SSR 69071
Citations are publications that use Tocris products. Selected citations for SSR 69071 include:
Li et al (2013) Solar ultraviolet irradiation induces decorin degradation in human skin likely via neutrophil elastase. PLoS One 8 e72563 PMID: 24023624
Hoffmann et al (2011) Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem 286 28889 PMID: 21693707
Reardon et al (2011) Thymic stromal lymphopoetin-induced expression of the endogenous inhibitory enzyme SLPI mediates recovery from colonic inflammation. Immunity 35 223 PMID: 21820333
Do you know of a great paper that uses SSR 69071 from Tocris? If so please let us know.
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