SSR 69071

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Cat.No. 2506 - SSR 69071 | C27H32N4O7S | CAS No. 344930-95-6
Description: Potent, orally active human leukocyte elastase inhibitor
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
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

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
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 344930-95-6
PubChem ID 9872438
InChI Key DRZXDZYWZSKFDL-UHFFFAOYSA-N
Smiles COC1=CC(C(C)C)=C2C(=O)N(COC3=CC(=O)N4C=CC=C(OCCN5CCCCC5)C4=N3)S(=O)(=O)C2=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 13.92 25
ethanol 5.57 10

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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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

2 Citations for SSR 69071

Citations are publications that use Tocris products. Selected citations for SSR 69071 include:

Hoffmann et al (2011) Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem 286 28889 PMID: 21693707

Li et al (2013) Solar ultraviolet irradiation induces decorin degradation in human skin likely via neutrophil elastase. PLoS One 8 e72563 PMID: 24023624


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