| 货号 | 10011562-25mg |
| 描述 | The lipid mediator thromboxane (TX)A2 plays a key role in platelet aggregation and vascular and bronchial smooth muscle constriction. The actions of TXA2 are mediated by its specific G protein-coupled receptor, referred to as the TXA2 receptor or TP. Two isoforms, TPα and TPβ, are produced from a single gene, differ in their carboxyl termini, and form homo- and hetero-oligomers.1 While both isoforms signal through similar pathways, they differ in the modulation by certain agonists.2 L-655,240 is a potent antagonist of the TP receptor in vitro(IC50 = 7 nM).3,4 It also is effective at blocking TP-mediated bronchoconstriction in vivo and platelet aggregation ex vivo.3 Whether the two TP isoforms differ in their sensitivity to L-655,240 is not known. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Laroche, G.,Lépine, M.C.,Thériault, C., et al. Oligomerization of the α and β isoforms of the thromboxane A2 receptor: Relevance to receptor signaling and endocytosis. Cellular Signalling 17, 1373-1383 (2005). 2.Wikström, K.,Kavanagh, D.J.,Reid, H.M., et al. Differential regulation of RhoA-mediated signaling by the TPα and TPβ isoforms of the human thromboxane A2 receptor: Independent modulation of TPα signaling by prostacyclin and nitric oxide. Cellular Signalling 20(8), 1497-1512 (2008). 3.Hall, R.A.,Gillard, J.,Guindon, Y., et al. Pharmacology of L-655,240 (3-[1-(4-chlorobenzyl)-5-fluoro-3-methyl-indol-2-yl]2,2-dimethylpro pan oic acid); a potent, selective thromboxane/prostaglandin endoperoxide antagonist. European Journal of Pharmacology 135(2), 193-201 (1987). 4.Ogletree, M.L. and Allen, G.T. Interspecies differences in thromboxane receptors: Studies with thromboxane receptor antagonists in rat and guinea pig smooth muscles. Journal of Pharmacology and Experimental Therapeutics 260, 789-794 (1992). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 373.9 |
| 分子式 | C21H21ClFNO2 |
| CAS号 | 103253-15-2 |
| 稳定性 | ≥ 2 years |
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