CAS 9087-70-1|Aprotinin acetate salt
| Common Name | Aprotinin acetate salt | ||
|---|---|---|---|
| CAS Number | 9087-70-1 | Molecular Weight | 6511.83000 |
| Density | / | Boiling Point | / |
| Molecular Formula | C284H432N84O79S7 | Melting Point | / |
| MSDS | USA | Flash Point | / |
Names
| Name | Aprotinin |
|---|---|
| Synonym | More Synonyms |
Aprotinin acetate salt BiologicalActivity
| Description | Aprotinin is a bovine pancreatic trypsin inhibitor (BPTI) inhibitor which inhibits trypsin and chymotrypsin with Kis of 0.06 pM and 9 nM, respectively. |
|---|---|
| Related Catalog | Signaling Pathways >>Anti-infection >>Influenza VirusResearch Areas >>Cardiovascular DiseasePeptidesPeptides |
| Target | Ki: 0.06 pM (Trypsin), 9 nM (Chymotrypsin)[1] |
| In Vitro | Aprotinin, a serine protease inhibitor isolated from bovine lung, is a complex protease inhibitor that is an antifibrinolytic, inhibits contact activation, and decreases the inflammatory response to cardiopulmonary bypass[2]. Aprotinin inhibits trypsin (bovine, Ki= 0.06 pM), chymotrypsin (bovine, Ki= 9 nM), plasmin (human, 0.23 nM)[1]. Aprotinin is also a competitive protein inhibitor of NOS activity. It inhibits NOS-I and NOS-II with Ki values of 50 μM and 78 μM, respectively[3]. Aprotinin significantly inhibits fibrinolysis with an IC50 of 0.16±0.05 μM[4]. |
| In Vivo | High dose aprotinin can reduce blood loss and transfusion requirements associated with primary cardiac procedures such as coronary artery bypass graft (CABG) or heart valve replacement surgery[5]. Aprotinin inhibits thrombus formation in a dose-dependent manner. Aprotinin at a dose of 1.5 mg kg-1 (bolus) and 3 mg kg-1 h-1 infusion (maintenance infusion) causes a tendency towards a reduction in bleeding time. Aprotinin significantly reduces the bleeding time starting at a dose of 3 mg kg-1 bolus plus 6 mg kg-1 h-1 showing a reduction of approximately 84%±2.9%. At the highest dose of 5 mg kg-1 and 10 mg kg-1 h-1, the strongest effects are observed[4]. Aprotinin may affect tumor necrosis factor-alpha (TNF) levels. Soluble TNFRI levels are significantly increased following I/R in the aprotinin treated wild type mice and not detected in all TNFRInull mice[6]. |
| Animal Admin | 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]. |
| References | [1]. Fritz H, et al. Biochemistry and applications of aprotinin, the kallikrein inhibitor from bovine organs. Arzneimittelforschung. 1983;33(4):479-94. [2]. Levy JH, et al. Efficacy and safety of aprotinin in cardiac surgery. Orthopedics. 2004 Jun;27(6 Suppl):s659-62. [3]. Venturini G, et al. Aprotinin, the first competitive protein inhibitor of NOS activity.Biochem Biophys Res Commun. 1998 Aug 10;249(1):263-5 [4]. 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. [5]. 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. [6]. 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. |
Chemical & Physical Properties
| Molecular Formula | C284H432N84O79S7 |
|---|---|
| Molecular Weight | 6511.83000 |
| Exact Mass | 6507.00000 |
| Appearance of Characters | lyophilized powder | white |
| InChIKey | ZPNFWUPYTFPOJU-YSFZTAPISA-N |
| SMILES | CCC(C)C1NC(=O)C(CCCNC(=N)N)NC(=O)C(C)NC(=O)C(CCCCN)NC(=O)C2CSSCC3NC(=O)CNC(=O)CNC(=O)C(Cc4ccc(O)cc4)NC(=O)C(C(C)C)NC(=O)C(Cc4ccccc4)NC(=O)C(C(C)O)NC(=O)C(CCC(N)=O)NC(=O)C(CSSCC(NC(=O)C(CC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C(CO)NC(=O)C(CCCCN)NC(=O)C(Cc4ccccc4)NC(=O)C(CC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCCN)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC3=O)C(=O)NC(CCSC)C(=O)NC(CCCNC(=N)N)C(=O)NC(C(C)O)C(=O)NC(C(=O)NCC(=O)NCC(=O)NC(C)C(=O)O)CSSCC(NC(=O)C(Cc3ccccc3)NC(=O)C(CC(=O)O)NC(=O)C3CCCN3C(=O)C(N)CCCNC(=N)N)C(=O)NC(CC(C)C)C(=O)NC(CCC(=O)O)C(=O)N3CCCC3C(=O)N3CCCC3C(=O)NC(Cc3ccc(O)cc3)C(=O)NC(C(C)O)C(=O)NCC(=O)N3CCCC3C(=O)N2)NC(=O)C(CC(C)C)NC(=O)CNC(=O)C(C)NC(=O)C(CCCCN)NC(=O)C(C)NC(=O)C(CC(N)=O)NC(=O)C(Cc2ccc(O)cc2)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccc(O)cc2)NC(=O)C(CCCNC(=N)N)NC(=O)C(C(C)CC)NC1=O |
| Storage condition | 2-8°C |
| Stability | Stable. Incompatible with strong oxidizing agents. |
| Water Solubility | glycerol: soluble3mg/mL, clear, colorless (equilibration buffer containing 5% glycerol) | Freely soluble in water and in aqueous buffers of low ionic strength. |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Hazard Codes | Xn,Xi |
| Risk Phrases | 42/43-36/37/38-20/21/22 |
| Safety Phrases | 22-45-36/37-36-26 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 1 |
| RTECS | YN5080000 |
| HS Code | 35040000 |
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Synonyms
| cas9004-04-0 |
| Trypsin Inhibitor |
| MFCD00130541 |
