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/ Gabexate Mesylate

甲磺酸加贝酯 /Gabexate Mesylate {[allProObj[0].p_purity_real_show]}

货号：A113053 同义名： FOY;Gabexate (mesylate)

Gabexate mesylate could inhibit trypsin, plasmin, plasma kallikrein and thrombin with IC50s of 9.4 μM, 30 μM, 41 μM and 110 μM. It has certain anticoagulant effect.

Gabexate Mesylate 化学结构 CAS号：56974-61-9
Gabexate Mesylate 化学结构
CAS号：56974-61-9
Gabexate Mesylate 3D分子结构
CAS号：56974-61-9
Gabexate Mesylate 化学结构 CAS号：56974-61-9
Gabexate Mesylate 3D分子结构 CAS号：56974-61-9
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Gabexate Mesylate 纯度/质量文件 产品仅供科研

货号：A113053 标准纯度： {[allProObj[0].p_purity_real_show]}
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全球学术期刊中引用的产品

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Gabexate Mesylate 生物活性

描述 Gabexate mesylate is a non-antigenic synthetic inhibitor of trypsin-like serine proteinases that is therapeutically used in the treatment of pancreatitis and disseminated intravascular coagulation and as a regional anticoagulant for hemodialysis. Values of the inhibition constant (K(i)) for gabexate mesylate binding to human and bovine tryptase were 3.4 x 10(-9) M and 1.8 x 10(-7) M (at pH 7.4 and 37.0 degrees), respectively. Furthermore, gabexate mesylate inhibited the fibrinogenolytic activity of human tryptase[3]. Gabexate mesylate inhibits competitively constitutive and inducible NO synthase (cNOS and iNOS, respectively), with Ki values of 1.0 x 10(-4) M and 5.0 x 10(-3) M, respectively, at pH 7.4 and 37.0 degrees C. Moreover, like other NOS inhibitors, gabexate mesylate increases iNOS mRNA expression in rat C6 glioma cells, as induced by E. coli lipopolysaccharide plus interferon-gamma. And gabexate mesylate inhibits dose-dependently nitrite production (i.e. NO release) in rat C6 glioma cells, as induced by E. coli lipopolysaccharide plus interferon-gamma[4]. Gabexate Mesylate decreased the TNFalpha production of LPS-stimulated monocytes as shown by the inhibition of mRNA expression and increased the IL-10 production of LPS-stimulated monocytes. Gabexate Mesylate also suppressed the NFkappaB activity of LPS-stimulated monocytes. Inhibitory effect of Gabexate Mesylate on the TNFalpha production of activated human monocytes is mediated by the suppression of NFkappaB activation[5]. The administration of gabexate mesylate after ERCP protects against the development of pancreatitis similarly to the preprocedure administration[6].

Gabexate Mesylate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00835705 - Completed - -
NCT00703755 Patients With Metabolic Syndro... 展开 >>me 收起 << Phase 2 Completed - -
NCT00035256 Osteoporosis, Postmenopausal Phase 4 Completed - United States, Illinois ... 展开 >> For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Maywood, Illinois, United States United States, Oregon For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Portland, Oregon, United States Canada, Ontario For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Kitchener, Ontario, Canada For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician London, Ontario, Canada Canada, Quebec For additional information regarding investigative sites for this trial, contact 1-877-CTLILLY (1-877-285-4559, 1-317-615-4559) Monday-Friday from 9:00 AM to 5:00 PM Eastern Time (UTC/GMT - 5 hours, EST), or speak with your personal physician Sainte -Foy, Quebec, Canada 收起 <<

Gabexate Mesylate 参考文献

[1]Erba F, Fiorucci L, et al. Selective inhibition of human mast cell tryptase by gabexate mesylate, an antiproteinase drug. Biochem Pharmacol. 2001 Feb 1;61(3):271-6.

[2]Aosasa S, Ono S, et al. Mechanism of the inhibitory effect of protease inhibitor on tumor necrosis factor alpha production of monocytes. Shock. 2001 Feb;15(2):101-5.

[3]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

[4]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

[5]Aosasa S, Ono S, Mochizuki H, Tsujimoto H, Ueno C, Matsumoto A. Mechanism of the inhibitory effect of protease inhibitor on tumor necrosis factor alpha production of monocytes. Shock. 2001 Feb;15(2):101-5

[6]Manes G, Ardizzone S, Lombardi G, Uomo G, Pieramico O, Porro GB. Efficacy of postprocedure administration of gabexate mesylate in the prevention of post-ERCP pancreatitis: a randomized, controlled, multicenter study. Gastrointest Endosc. 2007 Jun;65(7):982-7

Gabexate Mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.98mL

2.40mL

1.20mL

23.95mL

4.79mL

2.40mL

Gabexate Mesylate 技术信息

CAS号56974-61-9
分子式C17H27N3O7S
分子量 417.477
别名 FOY;Gabexate (mesylate)
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(251.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 7 mg/mL(16.77 mM)，配合低频超声助溶
动物实验配方

PO 0.5% CMC-Na 50 mg/mL suspension

Tags: Gabexate | 56974-61-9 | FOY | Proteasome | Proteasome Inhibitor | Metabolic Enzyme/Protease | Proteasome | Factor Xa | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Gabexate Mesylate 纯度/质量文件 | Gabexate Mesylate 生物活性 | Gabexate Mesylate 临床数据 | Gabexate Mesylate 参考文献 | Gabexate Mesylate 实验方案 | Gabexate Mesylate 技术信息

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