| CAS NO: | 144494-65-5 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 440.6 |
| Cas No. | 144494-65-5 |
| Formula | C22H36N2O5S |
| Solubility | insoluble in EtOH; insoluble in DMSO; insoluble in H2O |
| Chemical Name | (2S)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid |
| Canonical SMILES | CCCCS(=O)(=O)NC(CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Tirofiban is a selective platelet GPIIb/IIIa receptor antagonist with IC50 value of 9 nM, it inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP.[1]
The GPIIb/IIIa receptor is a heterodimer composed of alpha and beta subunits. Each subunit consists of a larger extracellular region, a transmembrane domain, and a short intracellular cytoplasmic tail. There are over 80,000 GPIIb/IIIa receptors present on the plasma membrane of platelets. These receptors are relatively quiescent in the dormant platelet.[2]
In vitro, Tirofiban selectively inhibits the GP-IIb/IIIa receptor and have minimal effects on the ɑvβ3 vitronectin receptor. It inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L. [1]
In vivo. Tirofiban inhibits platelet aggregation responses to ADP and collagen in canine models. When administered to humans at 0.15μg/kg/min for 4 h. Tirofiban produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation. [3][4]
References:
[1] Egbertson MS, Chang CT, Duggan ME, et al. Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp. J Med Chem. 1994 Aug 5; 37 (16):2537-51.
[2] Hofmann LV1, Razavi M, Arepally A, et al. GPIIb-IIIa receptor inhibitors: what the interventional radiologist needs to know. Cardiovasc Intervent Radiol. 2001 Nov-Dec; 24 (6):361-7.
[3] Barrett JS1, Murphy G, Peerlinck K, et al. Pharmacokinetics and pharmacodynamics of MK-383, a selective non-peptide platelet glycoprotein-IIb/IIIa receptor antagonist, in healthy men. Clin Pharmacol Ther. 1994 Oct; 56 (4):377-88.
[4] Peerlinck K1, De Lepeleire I, Goldberg M, et al. MK-383 (L-700,462), a selective nonpeptide platelet glycoprotein IIb/IIIa antagonist, is active in man. Circulation. 1993 Oct; 88 (4 Pt 1):1512-7.
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