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GW311616 hydrochloride HNE inhibitor

Catalog No.B4676
Size Price Stock Qty
5mg
$332.00
In stock
10mg
$475.00
In stock
50mg
$1,425.00
In stock
100mg
$1,995.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

GW311616 hydrochloride

GW311616 hydrochloride Dilution Calculator

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Chemical Properties

Cas No. 197890-44-1 SDF Download SDF
Chemical Name (3S,3aS,6aR)-3-isopropyl-1-(methylsulfonyl)-4-((E)-4-(piperidin-1-yl)but-2-enoyl)hexahydropyrrolo[3,2-b]pyrrol-2(1H)-one hydrochloride
Canonical SMILES CC([[email protected]@](C1=O)([H])[[email protected]@]2([H])[[email protected]@](N1S(C)(=O)=O)([H])CCN2C(/C([H])=C([H])/CN3CCCCC3)=O)C.Cl
Formula C19H32ClN3O4S M.Wt 433.99
Solubility >21.7mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

GW311616 hydrochloride is a potent, selective, intracellular, orally bioavailable and long duration inhibitor of human neutrophil elastase (HNE) with an IC50 value of 22nM [1].

GW311616 hydrochloride has been found to be selevtive over other human serine proteases with IC50 values of 22nM for HNE, >100μM for trypsin, cathepsin G, and plasmin, >3μM for chymotrypsin and tissue plasminogen activator. In HNE enzyme kinetic tests, GW311616 has been reported to inhibit HNE with a Ki value of 0.13nM. In addition, GW311616 has been revealed to inhibit HWB with an IC50 values of 0.67μM in HWB assay. Moreover, by measurement of intraneutrophil elastase activity, GW311616 hydrochloride has been suggested to have a dose-response and duration of action in blood samples of dog [1].

References:
[1] Macdonald SJ1, Dowle MD, Harrison LA, Shah P, Johnson MR, Inglis GG, Clarke GD, Smith RA, Humphreys D, Molloy CR, Amour A, Dixon M, Murkitt G, Godward RE, Padfield T, Skarzynski T, Singh OM, Kumar KA, Fleetwood G, Hodgson ST, Hardy GW, Finch H. The discovery of a potent, intracellular, orally bioavailable,long duration inhibitor of human neutrophil elastase-GW311616A a development candidate. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8.