| Identification | Back Directory | [Name]
Tirofiban hydrochloride monohydrate | [CAS]
150915-40-5 | [Synonyms]
Tirofiban HCl
Unii-6H925F8o5j
TirofibanHcl142373-60-2/
Tirofiban hcl Monohydrate
TIROFIBAN, HYDROCHLORIDE HYDRATE
Tirofiban hydrochloride monohydrate
4-(4-Pyridinyl)butanol hydrochloride
N-(Butylsulfonyl)-O-[4-(4-piperidynyl)butyl]-L-tyrosine, Hydrochloride Hydrate
N-(Butylsulfonyl)-O-(4-(4-piperidinyl)butyl)-L-tyrosine monohydrochloride monohydrate
L-Tyrosine, N-(butylsulfonyl)-o-(4-(4-piperidinyl)butyl)-, monohydrochloride, monohydrate
(2S)-2-(Butylsulfonylamino)-3-[4-[4-(4-piperidyl)butoxy]phenyl]propanoic acid hydrochloride hydrate
(S)-2-(butylsulfonamido)-3-(4-(4-(piperidin-4-yl)butoxy)phenyl)propanoic acid hydrochloride hydrate
Tirofiban hydrochloride monohydrate
N-(Butylsulfonyl)-O-(4-(4-piperidinyl)butyl)-L-tyrosine monohydrochloride monohydrate | [EINECS(EC#)]
682-504-6 | [Molecular Formula]
C22H39ClN2O6S | [MDL Number]
MFCD07368623 | [MOL File]
150915-40-5.mol | [Molecular Weight]
495.07 |
| Chemical Properties | Back Directory | [Appearance]
White Solid | [Melting point ]
135-137°C | [storage temp. ]
-20°C Freezer | [solubility ]
DMSO: >12mg/mL at warmed to 60°C | [form ]
powder | [color ]
white to beige | [Optical Rotation]
[α]/D -10 to -18° (c=1, MeOH) | [Merck ]
14,9464 | [InChIKey]
HWAAPJPFZPHHBC-MGIYCFTINA-N | [SMILES]
S(CCCC)(=O)(=O)N[C@@H](CC1=CC=C(C=C1)OCCCCC1CCNCC1)C(O)=O.Cl.O |&1:8,r| |
| Hazard Information | Back Directory | [Chemical Properties]
White Solid | [Definition]
ChEBI: Tirofiban hydrochloride is a hydrochloride. It contains a tirofiban. | [Biochem/physiol Actions]
Tirofiban hydrochloride is a potent non-peptide, glycoprotein IIb/IIIa inhibitor. Blocks platelet aggregation and thrombus formation. | [in vivo]
Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) shows activity of increasing contraction force, ventricular compliance, and improving heart function by increasing HR, LVESP, dp/dtmax, and reducing LVEDP[2].
Tirofiban hydrochloride monohydrate (60 μg/kg; i.v.; once) enhances eNOS activity, decreases iNOS activity and reduces area of no-reflow after reperfusion following AMI[2].
Tirofiban hydrochloride monohydrate (50 μg/per; irrigate; once) shows anticoagulant effect with patency rates of 59% at 24 hours after microvascular anastomosis in the crush model[3]. | Animal Model: | Male Sprague-Dawley rats (10 to 15-week-age; 270-330 g)[2]. | | Dosage: | 60 μg/kg | | Administration: | Intravenous injection; once. | | Result: | Increased contraction force, ventricular compliance, and improved heart function.
Reduced the size of no-reflow and infarct.
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| Animal Model: | Sprague-Dawley rats (350-400 g; crush injury model)[3] | | Dosage: | 50 μg/per (50 μg/mL, 1 mL for each) | | Administration: | Irrigate 1 mL within the vessel lumen (before placement of the last suture); once. | | Result: | Showed anticoagulant effect with patency rates of 59%. |
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| Safety Data | Back Directory | [Hazard Codes ]
Xi | [Risk Statements ]
36/37/38 | [Safety Statements ]
26-37-45 | [WGK Germany ]
3 | [HS Code ]
2935.90.6000 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| Questions And Answer | Back Directory | [Tirofiban hydrochloride monohydrate]
Tirofiban is an anti-angina drug, it is successfully developed by the United States Merck company , Patent Number is EP 478363, and in 1998 it was sold in the United States, the trade name is Aggrastat,it is clinically used in treating acute coronary syndromes, including unstable angina or non-Q-wave myocardial infarction, and percutaneous transluminal coronary angioplasty (PTCA) or atherosclerotic plaque excision patients with in combination with heparin.
Drugs currently used in clinical are mainly tirofiban hydrochloride injections under the tradename Xin Weining, it is a reversible non-peptide platelet surface glycoprotein (GP) Ⅱb/Ⅲa receptor antagonist, it can competitively inhibit combination of fibrinogen and platelet (GP) Ⅱb/Ⅲa receptor . Intravenous injection is a dose-dependent inhibition of outside human platelet aggregation, prolonged bleeding time,and thrombosis caused by ADP, collagen, arachidonic acid,thromboxane analog U46619 and thrombin.
In healthy volunteers ,they are injected in routinely recommended doses, the peak plasma concentration is similar to that of steady-state plasma concentrations during the infusion ,T1/2 is 2h. Within 0.01~25 μg/ml dose range, PPB of this product is 65%, independent of concentration. Free drug accounts for 35% in plasma, Vd is 22~42 L. In healthy volunteers, CL is 213~314 ml/min, the renal clearance rate is 39%-69% of plasma clearance.
[Usage ]
(1) tirofiban hydrochloride monohydrate in combination with heparin is used in treating acute coronary syndromes, including unstable angina or non-Q-wave myocardial infarction, and percutaneous transluminal coronary angioplasty (PTCA) or atherectomy artery surgery patients.
(2) to give this product 0.4μg/(kg · min) bolus, 300 min, followed by a maintenance dose of 0.1μg/(kg · min). Unstable angina or non-Q-wave myocardial infarction patients need an infusion of 48~108 h. Row PTCA or atherectomy arterial patients need to continue infusion 12~24 h after surgery.
The above information is edited by the chemicalbook of Tian Ye.
| [Precautions ]
1. Adverse reactions: The most common adverse reactions are fever, or bleeding complications; other visible adverse reactions are nausea, headache, rash or urticaria, systemic reactions visible is reduction in platelet count.
2. Disable: allergy to the drug, the use of tirofiban in patients with thrombocytopenia occurring, there is active bleeding or bleeding constitution history before 30 days, history of intracranial hemorrhage, nearly a month of stroke or brain hemorrhage stroke, intracranial tumors, aneurysms, arteriovenous malformations, vital organs, surgery or severe trauma requiring surgical treatment, patients with aortic dissection, pericarditis, severe hypertension.
3. caution: recent (1 year) bleeding in patients, with coagulopathy, platelet disorder, or a history of thrombocytopenia, platelet count less than 150 × 109/L patients who have a history of cerebrovascular disease (1 year) , with recent subdural extracapsular surgery, nearly a month having a major surgery or a history of severe physical trauma, dissecting aneurysm, hemorrhagic retinal diseases, chronic hemodialysis patients.
| [Uses]
Acute coronary syndrome (angina pectoris, myocardial infarction, surgery hydrant).
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa inhibitor. It can prevent platelet aggregation and thrombosis.
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| Company Name: |
J & K SCIENTIFIC LTD.
|
| Telephone: |
18210857532 18210857532 |
| Website: |
https://www.jkchemical.com |
| Company Name: |
T&W GROUP
|
| Telephone: |
021-61551611 13296011611 |
| Website: |
www.trustwe.com/ |
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