133652-38-7 Usage
Description
Reteplase, also known as Retavase, is a deletion mutant variant of tissue plasminogen activator (tPA) produced in recombinant E. coli. It is a third-generation thrombolytic agent with a mechanism of action similar to alteplase. Reteplase acts directly by catalyzing the cleavage of plasminogen and initiating thrombolysis, exhibiting high thrombolytic potency. The protein consists of the kringle-2 domain and protease domain of tPA but lacks the kringle-1 domain and the growth factor domain. The expression in E. coli results in a non-glycosylated protein, and the deletion of several domains allows for a longer half-life and slower clearance. Despite the deletions and refolding, the catalytic center remains intact, and the kringle-2 domain enables binding to lysine in fibrin, making it effective for rapid and complete lysis of coronary thrombi.
Uses
Used in Myocardial Infarction Therapy:
Reteplase is used as a plasminogen activator for the treatment of acute myocardial infarction. It is effective in the rapid and complete lysis of coronary thrombi, which is crucial for restoring blood flow to the affected area and minimizing damage to the heart muscle.
Used in Pharmaceutical Industry:
Reteplase is used as a third-generation thrombolytic agent for the development of new therapies and treatments for various conditions that involve blood clotting, such as stroke, deep vein thrombosis, and pulmonary embolism. Its high thrombolytic potency and fibrin selectivity make it a valuable asset in the pharmaceutical industry for the development of targeted and effective treatments.
Originator
Boehringer Mannheim (Germany)
Mechanism of action
Reteplase is a recombinant deletion mutant of tPA lacking the finger, epidermal growth factor,
kringle 1 domain, and carbohydrate side chain. As a highly fibrin-specific
thrombolytic agent, reteplase is missing the first 172 amino acids that are present in alteplase and
has 355 amino acids with a molecular weight of 39 kDa. Because of the removal of the finger kringle
1 domain, reteplase binding to fibrin is reduced from that of alteplase, and reteplase has reduced
fibrin selectivity. In addition, the structural modification reduces hepatic elimination, leading to a
longer half-life (reteplase, 14–18 minutes; alteplase, 3–4 minutes).
Clinical Use
Administered as a double bolus of 10 U every 30 minutes, reteplase is approved for use in acute
myocardial infarction.
Drug interactions
Potentially hazardous interactions with other drugs
Antiplatelets, heparin, vitamin K antagonists:
increased risk of bleeding.
Metabolism
Cleared primarily by liver and kidneys.
Check Digit Verification of cas no
The CAS Registry Mumber 133652-38-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,3,6,5 and 2 respectively; the second part has 2 digits, 3 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 133652-38:
(8*1)+(7*3)+(6*3)+(5*6)+(4*5)+(3*2)+(2*3)+(1*8)=117
117 % 10 = 7
So 133652-38-7 is a valid CAS Registry Number.