A potent inhibitor of neutrophil elastase
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SSR 69071

Item No. 21477

Technical Information
Formal 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
CAS Number
344930-95-6
Molecular Formula
C27H32N4O7S
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMSO: 25mMEthanol: 10mM
λmax
229, 271 nm
SMILES
O=C1N(C2=NC(OCN3S(C(C=C(OC)C=C4C(C)C)=C4C3=O)(=O)=O)=C1)C=CC=C2OCCN5CCCCC5
InChi Code
InChI=1S/C27H32N4O7S/c1-18(2)20-14-19(36-3)15-22-25(20)27(33)31(39(22,34)35)17-38-23-16-24(32)30-11-7-8-21(26(30)28-23)37-13-12-29-9-5-4-6-10-29/h7-8,11,14-16,18H,4-6,9-10,12-13,17H2,1-3H3
InChi Key
DRZXDZYWZSKFDL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    SSR 69071 is a potent inhibitor of neutrophil elastase (Ki = 0.0168 nM for the human enzyme).1 It is selective for human neutrophil elastase over rat, mouse, and rabbit elastases (Kis = 3, 1.8, 58 nM, respectively). It inhibits human neutrophil elastase ex vivo in mouse bronchoalveolar lavage (BAL) fluid (ED50 = 10.5 mg/kg, p.o.). In vivo, SSR 69071 (2.8 mg/kg, p.o.) reduces acute lung hemorrhage induced by human neutrophil elastase in mice. It reduces carrageenan- and human neutrophil elastase-induced paw edema in rats (ED30s = 2.2 and 2.7 mg/kg, respectively). SSR 69071 also reduces cardiac infarct size when administered prior to ischemia or reperfusion in a rabbit model of ischemia-reperfusion injury.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kapui, Z., Varga, M., Urban-Szabo, K., et alBiochemical and pharmacological characterization of 2-(9-(2-piperidinoethoxy)-4-oxo-4H-pyrido[1,2-a]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(2), 451-459 (2003).

    2. Bidouard, J.-P., Duval, N., Kapui, Z., et alSSR69071, an elastase inhibitor, reduces myocardial infarct size following ischemia - reperfusion injury. Eur. J. Pharm. 461(1), 49-52 (2003).