SSR 69071

Name: SSR 69071
Brand: Tocris Bioscience
SKU: 2506

Tocris Bioscience, part of Bio-Techne | Catalog # 2506

Citations (6)

COA / SDS

Potent, orally active human leukocyte elastase inhibitor

Key Product Details

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)
Molecular Weight:	556.63

View Full Technical Details for SSR 69071

Technical Data
Citations

Biological Activity for SSR 69071

SSR 69071 is a 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.

Compound Libraries for SSR 69071

SSR 69071 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SSR 69071

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for SSR 69071

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

Preparing Stock Solutions for SSR 69071

The following data is based on the product molecular weight 556.63.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.25 mM	7.19 mL	35.93 mL	71.86 mL
1.25 mM	1.44 mL	7.19 mL	14.37 mL
2.5 mM	0.72 mL	3.59 mL	7.19 mL
12.5 mM	0.14 mL	0.72 mL	1.44 mL

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References for SSR 69071

References are publications that support the biological activity of the product.

Varga A novel orally active inhibitor of HLE. Eur.J.Med.Chem. 2003 PMID: 12750030
Kapui 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. 2003 PMID: 12606659
Bidouard SSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia-reperfusion injury. Eur.J.Pharmacol. 2003 PMID: 12568915