Terutroban

产品说明书

Print
Chemical Structure| 165538-40-9 同义名 : S-18886; Triplion
CAS号 : 165538-40-9
货号 : A287410
分子式 : C20H22ClNO4S
纯度 : 98%+
分子量 : 407.91
MDL号 : MFCD28411833
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 TP (thromboxane-A2 /prostaglandin-endoperoxide)-receptor blockade with terutroban decreases portal pressure in cirrhosis[3]. Terutroban is a selective TP receptor antagonist, i.e. a specific antagonist of the thromboxane A(2) and prostaglandin endoperoxide receptors, shown to improve endothelial function after a single administration in patients with coronary artery disease. It can chronically improve endothelium-dependent vasodilatation and inhibiting platelet aggregation[4]. Terutroban prevents the development of aorta hyperplasia and has beneficial effects on fibrotic processes by affecting TGF-β and heat shock protein-47 expression in SHRSPs(spontaneously hypertensive stroke-prone rats)[5]. Terutroban significantly protected retinal vascularity from ischaemia in experimental diabetes, and this result could be attributed not only to its antiplatelet/antithrombotic activities but also to its vascular properties[6]. In PAD (peripheral arterial disease) patients, terutroban dose-dependently inhibited platelet aggregation 24 h after dosing, and was at least as effective as aspirin at 5, 10 and 30 mg day(-1). Terutroban was well tolerated[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.45mL

0.49mL

0.25mL

12.26mL

2.45mL

1.23mL

24.52mL

4.90mL

2.45mL

参考文献

[1]Bots ML, Ford I, et al. Thromboxane prostaglandin receptor antagonist and carotid atherosclerosis progression in patients with cerebrovascular disease of ischemic origin: a randomized controlled trial. Stroke. 2014 Aug;45(8):2348-53.

[2]De La Cruz JP, Jebrouni N, et al. Effects of terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, on retinal vascularity in diabetic rats. Diabetes Metab Res Rev. 2012 Feb;28(2):132-8.

[3]Rosado E, Rodríguez-Vilarrupla A, Gracia-Sancho J, Tripathi D, García-Calderó H, Bosch J, García-Pagán JC. Terutroban, a TP-receptor antagonist, reduces portal pressure in cirrhotic rats. Hepatology. 2013 Oct;58(4):1424-35

[4]Lesault PF, Boyer L, Pelle G, Covali-Noroc A, Rideau D, Akakpo S, Teiger E, Dubois-Randé JL, Adnot S. Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis. Br J Clin Pharmacol. 2011 Jun;71(6):844-51

[5]Gelosa P, Sevin G, Pignieri A, Budelli S, Castiglioni L, Blanc-Guillemaud V, Lerond L, Tremoli E, Sironi L. Terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, prevents hypertensive vascular hypertrophy and fibrosis. Am J Physiol Heart Circ Physiol. 2011 Mar;300(3):H762-8

[6]De La Cruz JP, Jebrouni N, López-Villodres JA, Muñoz-Marín J, Guerrero A, González-Correa JA. Effects of terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, on retinal vascularity in diabetic rats. Diabetes Metab Res Rev. 2012 Feb;28(2):132-8

[7]Fiessinger JN, Bounameaux H, Cairols MA, Clement DL, Coccheri S, Fletcher JP, Hoffmann U, Turpie AG; TAIPAD investigators. Thromboxane Antagonism with terutroban in Peripheral Arterial Disease: the TAIPAD study. J Thromb Haemost. 2010 Nov;8(11):2369-76