Aprotinin (Synonyms: 抑肽酶)

目录号: HY-P0017 纯度: 99.01%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Aprotinin是分离自牛肺的丝氨酸蛋白酶 (BPTI) 抑制剂，对胰蛋白酶和胰凝乳蛋白酶 的 K_i 值分别为0.06 pM和9 nM。

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Aprotinin Chemical Structure

CAS No. : 9087-70-1

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Customer Review

MCE 顾客使用本产品发表的 14 篇科研文献

: Aprotinin purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2017 Dec 1;313(6):C632-C643. [Abstract]; Effects of protease inhibitor PIC, a serine protease inhibitor AEBSF and trypsin and chymotrypsin inhibitors Aprotinin (Aprot, 0.1 mM) on PRR cleavage induced by BSA in HK-2 cells.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with K_is of 0.06 pM and 9 nM, respectively.

IC₅₀ & Target

Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)^[1]

体外研究
(In Vitro)

Aprotinin 是一种从牛肺中分离出来的丝氨酸蛋白酶抑制剂，是一种复合蛋白酶抑制剂，具有抗纤维蛋白溶解作用，可抑制接触激活，并降低体外循环的炎症反应^[2]。
Aprotinin 抑制胰蛋白酶 (牛，K_i=0.06 pM)、胰凝乳蛋白酶 (牛，K_i=9 nM)、纤溶酶 (人，0.23 nM)^[1]。
Aprotinin 也是一种 NOS 活性的竞争性蛋白抑制剂。它抑制 NOS-I 和 NOS-II 的 K_i 值分别为 50 μM 和 78 μM^[3]。
Aprotinin 显著抑制纤维蛋白溶解，IC₅₀ 为 0.16±0.05 μM^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Aprotinin 高剂量可以减少与主要心脏手术相关的失血和输血需求，例如冠状动脉旁路移植术 (CABG) 或心脏瓣膜置换手术^[5]。
Aprotinin 以剂量依赖性方式抑制血栓形成，Aprotinin 剂量为 1.5 mg/kg 和 3 mg/kg/h 输注 (维持输注) 有减少出血时间的趋势。Aprotinin 以 3 mg/kg/h 剂量加 6 mg/kg/h 显著减少出血时间约 84%±2.9%。在 5 mg/kg/h 和 10 mg/kg/h 的最高剂量下，观察到最强的效果^[4]。Aprotinin 可能影响肿瘤坏死因子-α (TNF) 水平。在经 Aprotinin 处理的野生型小鼠中，I/R 后可溶性 TNFRI 水平显著增加，但在所有 TNFRInuLl 小鼠中均未检测到^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

6511.44

Formula

C₂₈₄H₄₃₂N₈₄O₇₉S₇

CAS 号

9087-70-1

性状

固体

颜色

Off-white to light brown

Sequence

Arg-Pro-Asp-Phe-Cys-Leu-Glu-Pro-Pro-Tyr-Thr-Gly-Pro-Cys-Lys-Ala-Arg-Ile-Ile-Arg-Tyr-Phe-Tyr-Asn-Ala-Lys-Ala-Gly-Leu-Cys-Gln-Thr-Phe-Val-Tyr-Gly-Gly-Cys-Arg-Ala-Lys-Arg-Asn-Asn-Phe-Lys-Ser-Ala-Glu-Asp-Cys-Met-Arg-Thr-Cys-Gly-Gly-Ala(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)

Sequence Shortening

RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA(Disulfide bridge: Cys5-Cys55,Cys14-Cys38,Cys30-Cys51)

中文名称

抑肽酶；抑胰肽酶；屈来密多

结构分类

Others

初始来源

动物

Bovine lung

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

细胞实验：

H₂O 中的溶解度 : 100 mg/mL (15.36 mM; 超声助溶)

DMSO 中的溶解度 : 66.67 mg/mL (10.24 mM; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈3); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.1536 mL	0.7679 mL	1.5358 mL
5 mM	0.0307 mL	0.1536 mL	0.3072 mL
10 mM	0.0154 mL	0.0768 mL	0.1536 mL

查看完整储备液配制表

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (7.68 mM); 澄清溶液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.01%

选择批次：

Data Sheet (671 KB) SDS (393 KB)

COA (264 KB) RP-HPLC (475 KB) MS (530 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62. [Content Brief]

[2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94. [Content Brief]

[3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

[4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5 [Content Brief]

[5]. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31. [Content Brief]

[6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83. [Content Brief]

[7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62. [Content Brief]

Animal Administration ^[4]^[6]	Rats: Male Wistar rats (180-220 g) are used in the study. Aprotinin is dissolved in physiological saline. Aprotinin is administered by bolus injection followed by a maintenance infusion. The doses given are 1.5 mg kg^-1 and 3 mg kg^-1 h^-1, 3mg kg^-1 and 6 mg kg^-1 h^-1 up to 5 mg kg^-1 and 10 mg kg^-1 h^-1. Plasma concentrations for the two agents are assessed by pharmacokinetic studies in rats^[4]. Mice: An intact mouse model of ischemia/reperfusion (30 min-I/60 min-R) is used and left ventricular peak + dP/dt is measured in wild type mice (WT, C57BL/6; n=10), WT mice with aprotinin (4mL/kg; n=10), transgenic mice devoid of the TNFRI (TNFRInull; n=10), and TNFRInull with aprotinin (n=10)^[6]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62. [Content Brief] [2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94. [Content Brief] [3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62. [4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5 [Content Brief] [5]. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31. [Content Brief] [6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83. [Content Brief] [7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62. [Content Brief]

Animal Administration
^[4]^[6]

Rats: Male Wistar rats (180-220 g) are used in the study. Aprotinin is dissolved in physiological saline. Aprotinin is administered by bolus injection followed by a maintenance infusion. The doses given are 1.5 mg kg^-1 and 3 mg kg^-1 h^-1, 3mg kg^-1 and 6 mg kg^-1 h^-1 up to 5 mg kg^-1 and 10 mg kg^-1 h^-1. Plasma concentrations for the two agents are assessed by pharmacokinetic studies in rats^[4].

Mice: An intact mouse model of ischemia/reperfusion (30 min-I/60 min-R) is used and left ventricular peak + dP/dt is measured in wild type mice (WT, C57BL/6; n=10), WT mice with aprotinin (4mL/kg; n=10), transgenic mice devoid of the TNFRI (TNFRInull; n=10), and TNFRInull with aprotinin (n=10)^[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62. [Content Brief]

[2]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94. [Content Brief]

[3]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62.

[4]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity. Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5 [Content Brief]

[5]. Sperzel M, et al. Evaluation of aprotinin and tranexamic acid in different in vitro and in vivo models of fibrinolysis, coagulation and thrombus formation. J Thromb Haemost. 2007 Oct;5(10):2113-8. Epub 2007 Jul 31. [Content Brief]

[6]. Davis R, et al. Aprotinin. A review of its pharmacology and therapeutic efficacy in reducing blood loss associated withcardiac surgery. Drugs. 1995 Jun;49(6):954-83. [Content Brief]

[7]. Sabbagh MJ, et al. Aprotinin exacerbates left ventricular dysfunction after ischemia/reperfusion in mice lacking tumor necrosis factor receptor I. J Cardiovasc Pharmacol. 2008 Oct;52(4):355-62. [Content Brief]

Aprotinin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	0.1536 mL	0.7679 mL	1.5358 mL	3.8394 mL
	5 mM	0.0307 mL	0.1536 mL	0.3072 mL	0.7679 mL
	10 mM	0.0154 mL	0.0768 mL	0.1536 mL	0.3839 mL
H₂O	15 mM	0.0102 mL	0.0512 mL	0.1024 mL	0.2560 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aprotinin9087-70-1抑肽酶抑胰肽酶屈来密多Influenza VirusSer/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Aprotinin (Synonyms: 抑肽酶)

Customer Review

MCE 顾客使用本产品发表的 14 篇科研文献