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GW311616 hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
GW311616 hydrochloride图片
CAS NO:197890-44-1
包装与价格：
包装价格(元)
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GW-311616 是一种有效的、可口服的、长效的、选择性的人中性粒细胞弹性蛋白酶 (HNE) 抑制剂，IC50 值为 22 nM，Ki 值为 0.31 nM。
Cas No.197890-44-1
别名GW311616A
化学名(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 SMILESCC([C@@](C1=O)([H])[C@@]2([H])[C@@](N1S(C)(=O)=O)([H])CCN2C(/C([H])=C([H])/CN3CCCCC3)=O)C.Cl
分子式C19H32ClN3O4S
分子量433.99
溶解度≥ 21.7 mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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