基本情報
- CAS
1219214-76-2- 標準SMILES
O=C(O)C1CC(C2CCCCC2)CN1- InChIKey
XRZWVSXEDRYQGC-UHFFFAOYSA-N- 分子式
- C11H19NO2
- 平均分子量
- 197.27 g/mol
- 単同位体質量
- 197.14157885
概要
Streptokinase, is a sterile, purified preparation of a bacterial protein elaborated by group C (beta) -hemolytic streptococci.
名称と識別子
- 優先名称
- Streptokinase
- IUPAC
- 4-cyclohexylpyrrolidine-2-carboxylic acid
- 現地名
- ストレプトキナーゼ
- 英語名
- STREPTOKINASE
- 分子式
- C11H19NO2
- 分子量
- 197.27406
名称と別名
名称をさらに表示
データベース識別子
- CAS
1219214-76-2、9002-01-1- PubChem CID
- 9815560
- DTXSID
DTXSID00864144- ChEMBL
CHEMBL2108147- EC Number
- 232-647-1
物性
構造計算による物性
- XLogP
- 0.3
- 極性表面積
- 49.3 Ų
- 水素結合供与体数
- 2
- 水素結合受容体数
- 3
- 回転可能結合数
- 2
- 重原子数
- 14
- 形式電荷
- 0
- 複雑度
- 211
実験および物理化学的性質
物理化学的性質
- 貯蔵温度
- -20 °C · -20°C
- 外見
- 凍結乾燥粉末
- 色
- White to off-white
- 由来生物
- human
- Merck
- 13 · 13,8903
- Specific Activity
- 2 · ≥2,000units/mg solid
- InChI
- 1S/C11H19NO2/c13-11(14)10-6-9(7-12-10)8-4-2-1-3-5-8/h8-10,12H,1-7H2,(H,13,14)
- InChIKey
- XRZWVSXEDRYQGC-UHFFFAOYSA-N
- SMILES
- N1C(CC(C1)C2CCCCC2)C(=O)O
安全と法規制
GHS分類
GHS Classification
Danger
H334 (100%): May cause allergy or asthma symptoms or breathing difficulties if inhaled [Danger Sensitization, respiratory]
P233, P260, P271, P284, P304+P340, P342+P316, P403, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 131 reports by companies from 1 notifications to the ECHA C&L Inventory.
危険有害性情報
毒性情報
Adverse Effects
Allergic reactions and bleeding are common adverse events related to streptokinase. The GISSI study demonstrated a 3.4% incidence of minor bleeding. The ISSI-2 study demonstrates a 0.4% incidence of significant bleeding. Patients may experience transient bradycardia or hypotension, with an incidence of 10%. Streptokinase is derived from bacterial proteins and thus can result in allergic reactions. Allergic reactions have been noted in up to 4.4% of patients and may present with fever, shivering, or rash. In rare cases, anaphylaxis may occur, which appears to be IgE mediated. Patients who develop anaphylactic signs and symptoms should promptly discontinue treatment and receive epinephrine.
Toxicity Summary
Streptokinase can precipitate an allergic reaction. Symptoms include fever, shivering, and rash. Patients in rare instances have developed nonfatal anaphylactic reactions. In cases of anaphylaxis, patients should be administered epinephrine immediately and discontinue streptokinase therapy. The toxicity of streptokinase is believed to be because it is a polypeptide derivative of beta-hemolytic streptococci bacteria.
Plasminogen is an inactive molecule that becomes activated to plasmin when the Arg/Val bond is cleaved. Plasmin breaks down fibrin clots created by the blood clotting cascade. Streptokinase forms a highly specific 1:1 enzymatic complex with plasminogen which converts inactive plasminogen molecules into active plasmin. Plasmin degrades fibrin clots as well as fibrinogen and other plasma proteins. This in turn leads to the degradation of blood clots.
Drug Induced Liver Injury
Drug-Induced Liver Injury Severity and Toxicity (DILIst)
STREPTOKINASE
DILI Positive
Intracoronary; Intravenous
DOI:10.1016/j.drudis.2019.09.022
安全データ
- F
- 10-21
- wgk
- 3
- rtecs
- OB8880000
- 毒性
- LD50 oral in mouse: > 10gm/kg
- hs_code
- 3504009000
- risk_code
- 36/37/38
- hazard_code
- B,Xi
- safety_code
- 22-24/25-36-26
- ストレージクラス
- 11 - Combustible Solids
化学と産業
薬理情報
ATC Code
B - Blood and blood forming organs
QB - Blood and blood forming organs
B01AD01
Pharmacodynamics
Streptokinase creates an active complex which promotes the cleavage of the Arg/Val bond in plasminogen to form the proteolytic enzyme plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
Mechanism of Action
Plasminogen is an inactive molecule that becomes activated to plasmin when the Arg/Val bond is cleaved. Plasmin breaks down fibrin clots created by the blood clotting cascade. Streptokinase forms a highly specific 1:1 enzymatic complex with plasminogen which converts inactive plasminogen molecules into active plasmin. Plasmin degrades fibrin clots as well as fibrinogen and other plasma proteins. This in turn leads to the degradation of blood clots.
Metabolism/Metabolites
Free toxin may be removed by opsonization via the reticuloendothelial system (primarily the liver and kidneys) or it may be degraded through cellular internalization via the lysosomes. Lysosomes are membrane-enclosed organelles that contain an array of digestive enzymes, including several proteases.
用途と製造
応用分野
説明Streptokinase is a protein produced by certain strains of hemolytic group C streptococcus, and it was the first clinically useful fibrinolytic. Unlike other plasminogen activators, streptokinase is not an enzyme and cannot break any bonds in a plasminogen molecule by itself. It forms an equimolecular compound with plasminogen, thus forming a streptokinase–plasminogen complex. In the plasminogenic region of the resulting complex, certain conformational changes lead to a break in a few peptide bonds, and transformation of this complex into a streptokinase–plasmin complex, or free plasmin, which also decomposes fibrin.
使用This drug has a half-life in the plasma of 15–30 min, and is used intravenously to treat patients with severe, massive pulmonary embolism and thrombus of the veins; it is also used during myocardial infarctions. Recently, a number of streptokinase derivatives have been proposed, in particular acetylated derivatives, which are developed for use as fibrinolytics.
一般的な説明Streptokinase (Kabikinase, Streptase)is a catabolic 47,000-d protein secreted by group Cβ-hemolyticstreptococci. It is a protein with no intrinsic enzymaticactivity. Streptokinase activates plasminogen toplasmin, a proteolytic enzyme that hydrolyzes fibrin andpromotes the dissolution of thrombi. Plasminogen is activatedwhen streptokinase forms a 1:1 stoichiometric complexwith it. Allergic reactions to streptokinase occur commonlybecause of antibody formation in individuals treatedwith it. Furthermore, the antibodies inactivate streptokinaseand reduce its ability to prolong thrombin time.Streptokinase is indicated for acute myocardial infarction,for local perfusion of an occluded vessel, and before angiography,by intravenous, intra-arterial, and intracoronaryadministration, respectively.
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