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Gabexate mesylate Sale

(Synonyms: 甲磺酸加贝酯; FOY) 目录号 : GC13711

A serine protease inhibitor

Gabexate mesylate Chemical Structure

Cas No.:56974-61-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥483.00
现货
5mg
¥378.00
现货
50mg
¥1,439.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases with Ki values of 3.4nM and 180nM, respectively for human tryptase and bovine tryptase [1].

Gabexate mesylate is a drug used in the treatment of pancreatitis, disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Gabexate mesylate is reported to bind to the primary specificity site S1 of human and bovine tryptases. The carbonyl group of gabexate mesylate interacts with the oxyanion binding hole of the enzyme. The tighter binding of gabexate mesylate to human tryptase results in a higher affinity than to bovine tryptase [1].

Gabexate mesylate is also found to inhibit cNOS and iNOS, with Ki values of 150μM and 5mM. It up-regulates iNOS gene expression. In addition, gabexate mesylate inhibits the LPS/IFNγ-induced NO production with EC50 value of 250μM [2].

References:
[1] Erba F, Fiorucci L, Pascarella S, Menegatti E, Ascenzi P, Ascoli F. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61(3):271-6.
[2] Colasanti M, Persichini T, Venturini G, Menegatti E, Lauro GM, Ascenzi P. Effect of gabexate mesylate (FOY), a drug for serine proteinase-mediated diseases, on the nitric oxide pathway. Biochem Biophys Res Commun. 1998 May 19;246(2):453-6.

Chemical Properties

Cas No. 56974-61-9 SDF
别名 甲磺酸加贝酯; FOY
化学名 ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid
Canonical SMILES CCOC(=O)C1=CC=C(C=C1)OC(=O)CCCCCN=C(N)N.CS(=O)(=O)O
分子式 C16H23N3O4.CH4O3S 分子量 417.48
溶解度 ≥ 18.2 mg/mL in DMSO, ≥ 99.8 mg/mL in EtOH, ≥ 102.4 mg/mL in Water 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3953 mL 11.9766 mL 23.9532 mL
5 mM 0.4791 mL 2.3953 mL 4.7906 mL
10 mM 0.2395 mL 1.1977 mL 2.3953 mL
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