ChemicalBook CAS DataBase List 150374-95-1

150374-95-1

Name	N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt
CAS	150374-95-1
Molecular Formula	C20H21N2NaO7S
Molecular Weight	456.44
MOL File	150374-95-1.mol

Chemical Properties

Melting point	104-108 °C(Solv: water (7732-18-5))
storage temp.	Desiccate at RT
solubility	DMSO (Slightly), Methanol (Slightly)
form	Solid
color	White to Off-White

Hazard Information

Uses

Treatment of acute lung injury; acute respiratory distress syndrome (elastase inhibitor).

Biological Activity

Selective leukocyte elastase inhibitor (IC 50 = 44 nM) that displays no activity at a range of other proteases. Inhibits NF- κ B activation and LTB 4 -induced neutrophil transmigration in vitro . Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo .

in vivo

Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID₅₀ = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID₅₀ = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase^[1].
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats^[2].
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder^[3].

Animal Model:	Male Golden hamsters, weighing 90 to 110 g^[1].
Dosage:	0.021-2.1 mg/kg.
Administration:	Intratracheally five min before HNE injection.
Result:	Significantly and dosedependently suppressed the lung hemorrhage.

Animal Model:	Male Sprague-Dawley rats weighing 350-400 g^[2].
Dosage:	10 mg/kg.
Administration:	Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
Result:	Greatly suppressed lung injury, as revealed by the reduced histological damage. Significantly ameliorated HSR-induced lung injury. Markedly decreased the levels of TNF-α and iNOS gene.

Animal Model:	Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g^[3].
Dosage:	15 mg/kg or 60 mg/kg.
Administration:	IP.
Result:	Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.

storage

Desiccate at RT

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