Tenecteplase, also known as tPA, is a recombinant tissue plasminogen activator (rtPA) produced by genetically modified Chinese hamster ovary (CHO) cells. It is a 527-amino acid glycoprotein with specific modifications in its cDNA construct, including Thr103 to Asp, Asp117 to Gln in the kringle-1 domain, and a tetra-alanine substitution at amino acids 296 to 299 in the protease domain. This sterile, lyophilized powder is designed for single intravenous (IV) bolus administration after reconstitution with sterile water and should be administered immediately after reconstitution.
191588-94-0
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Basic information
- Product Name: tenecteplase
- Synonyms: tenecteplase;Tnkase;Plasminogen activator (human tissue-type), 103-L-asparagine-117-L-glutamine-296-L-alanine-297-L-alanine-298-L-alanine-299-alanine-;Tnk-tpa;Unii-wgd229o42w
- CAS NO:191588-94-0
- Molecular Formula:
- Molecular Weight: 0
- EINECS: N/A
- Product Categories: N/A
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Chemical Properties
- Melting Point: N/A
- Boiling Point: N/A
- Flash Point: N/A
- Appearance: /
- Density: N/A
- Refractive Index: N/A
- Storage Temp.: N/A
- Solubility: N/A
- CAS DataBase Reference: tenecteplase(CAS DataBase Reference)
- NIST Chemistry Reference: tenecteplase(191588-94-0)
- EPA Substance Registry System: tenecteplase(191588-94-0)
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Safety Data
- Hazard Codes: N/A
- Statements: N/A
- Safety Statements: N/A
- WGK Germany:
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 191588-94-0(Hazardous Substances Data)
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191588-94-0 Usage
Uses
Used in Acute Thrombotic Disorders:Tenecteplase is used as a thrombolytic agent for the treatment of acute thrombotic disorders. It works by converting plasminogen to plasmin, which breaks down the fibrin in blood clots, thus restoring blood flow to the affected area. This application is particularly relevant in conditions such as acute myocardial infarction, ischemic stroke, and massive pulmonary embolism, where rapid clot dissolution is crucial for patient recovery and survival.
Used in Pharmaceutical Industry:
In the pharmaceutical industry, tenecteplase is used as a key component in the development of drugs targeting thrombotic conditions. Its recombinant nature and specific modifications allow for a more controlled and targeted approach to clot dissolution, reducing the risk of bleeding complications associated with other thrombolytic agents. This makes tenecteplase a valuable asset in the development of novel therapeutic strategies for various thrombotic disorders.
Mechanism of action
Tenecteplase is composed of 527 amino acids with 17 disulfide bridges. It differs structurally from anteplase by three point mutations. The mutations were bioengineered to occur at amino acid 103, where threonine (T) is replaced by asparagine; at amino acid 117, where asparagine (N) is replaced by glutamine; and at amino acids 296 to 299, where lysine (K)-histidinearginine-arginine are replaced with four alanines. Thus, the name TNK is derived from the mutations. The replacement of these amino acids along with their attached carbohydrate side chains results in a prolonged half-life (~17 minutes) and allows a single bolus application. These point-mutation changes also change the binding of tenecteplase to plasminogen activator inhibitor-1 (PAI-1) by 80-fold, thus improving activity. A physiological enzyme, PAI-1 inhibits fibrinolysis. Finally, tenecteplase shows a 15-fold higher fibrin specificity. The drug is still eliminated via hepatic mechanisms.Clinical Use
Thrombolytic: Acute myocardial infarctionDrug interactions
Potentially hazardous interactions with other drugs Drugs that affect coagulation or platelet function: increased risk of bleeding.Metabolism
Tenecteplase is cleared from circulation by binding to specific receptors in the liver followed by catabolism to small peptides.Check Digit Verification of cas no
The CAS Registry Mumber 191588-94-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,9,1,5,8 and 8 respectively; the second part has 2 digits, 9 and 4 respectively.Calculate Digit Verification of CAS Registry Number 191588-94:
(8*1)+(7*9)+(6*1)+(5*5)+(4*8)+(3*8)+(2*9)+(1*4)=180
180 % 10 = 0
So 191588-94-0 is a valid CAS Registry Number.
191588-94-0Upstream product
191588-94-0Downstream Products
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