ストレプトキナーゼ

Streptokinase

HCID 9815560

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

Estreptoquinasa9002-01-1StreptaseKabikinaseStreptochinasiStreptokinasumStreptococcal fibrinolysinStreptokinase cRefChem:3892898X1OXL3SNUStreptokinase (peptidolytic)B01AD01
名称をさらに表示
ストレプトキナーゼストレプトキナーゼ, ランスフィールドC群ストレプトコッカスDKK-1 ヒトストレプトキナーゼ Β-溶血活性STREPTOCOCCUS(LANCEFIELD C群)由来カビキナーゼアウェリシンSKSKCA1KCa2.1UNQ492PRO1008awelysinDickkopf-1DKK-1 human
DTXSID901046751EC 3.4.-232-647-14-cyclohexylpyrrolidine-2-carboxylic Acid1219214-76-24-cyclohexylproline4-Cyclohexyl-pyrrolidine-2-carboxylic acidtrans-4-cyclohexylpyrrolidine-2-carboxylic acid

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

実験および物理化学的性質

Human DrugsThrombolytic medicines

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

安全と法規制

GHS分類

GHS Classification · 4 件

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

Other Safety InformationIMAP assessments - Kinase (enzyme activating), strepto-: Environment tier I assessment
Hazard Classes and CategoriesResp. Sens. 1 (100%)

毒性情報

Adverse Effects · 1 件

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.

Exposure RoutesOral
Toxicity Summary · 2 件

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.

Carcinogen ClassificationNo indication of carcinogenicity to humans (not listed by IARC).
Drug Induced Liver Injury · 5 件

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

化学と産業

薬理情報

ATC Code · 3 件

B - Blood and blood forming organs

QB - Blood and blood forming organs

B01AD01

Pharmacodynamics · 1 件

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 · 1 件

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 · 1 件

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.

MeSH Pharmacological ClassificationFibrinolysin or agents that convert plasminogen to FIBRINOLYSIN.

用途と製造

UsesFor the treatment of acute evolving transmural myocardial infarction, pulmonary embolism, deep vein thrombosis, arterial thrombosis or emolism and occlusion of arteriovenous cannulae
応用分野 · 3 件

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.

サプライヤー54 社

北京华美互利生物化工010-56205725 · [email protected]
南通飞宇生物科技有限公司0513-68819626 15152877458 · [email protected]
上海康朗生物科技有限公司021-61998208 18217752821 · [email protected]
上海金试生化科技有限公司18601717983 18601717983 · [email protected]
上海哲研生物科技有限公司021-18017610038 18017610038 · [email protected]

関連反応

2 件

化合物ノート

読み込み中…