Factor Xa
Factor X is a vitamin K–dependent serine endopeptidase playing critical roles in normal hemostasis. Factor X is synthesized in the liver and becomes activated into factor Xa (FXa) by both the intrinsic and the extrinsic Xase complexes. FXa converts prothrombin into thrombin in the prothrombinase complex, which in turn cleaves fibrinogen into an insoluble fibrin clot. Besides a role in coagulation, FXa signaling is mainly mediated by the activation of PARs, which belong to G-protein coupled receptor family. Currently, four members of the PAR, PAR-1 through -4 have been identified. PAR-1, -3 and PAR-4 but not PAR-2 can be cleaved by thrombin whereas PAR-1, PAR-2 and PAR-4 can mediate FXa signaling. FXa exerts inflammatory responses partially through enhancing generation of an inflammatory signaling molecule, thrombin. FXa increases expression of inflammatory cytokines including IL-6, IL-8, and monocyte chemotactic protein-1 (MCP-1), as well as the expression of the adhesion molecules, E-selectin, intracellular adhesion molecule-1 (ICAM-1) and vascular-cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells. Although the signaling function of FXa is mainly mediated through PARs, non-PAR cell receptors play pivotal roles in the potency and the specificity of FXa signaling. FXa is found in various malignant tissues. It can be expressed by tumor cells ectopically or delivered by stromal cells to the tumor microenvironment. FXa could be a novel diagnostic factor as well as a clinically invaluable post-treatment marker for fibrosis, atherosclerosis, and cancer.
References
1.Ebrahimi S,et al. J Cell Physiol. 2017;232(8):1966–1970.
References
1.Ebrahimi S,et al. J Cell Physiol. 2017;232(8):1966–1970.
Metabolic Enzyme/Protease
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Factor Xa
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Dechloro Rivaroxaban
产品货号 : M37156
cas no: 1415566-28-7
Dechloro Rivaroxaban 是一种有口服活性的 Factor Xa 高选择性抑制剂。Dechloro Rivaroxaban 抑制人体内游离的 FXa,其 Ki 为 0.4 nM。Dechloro Rivaroxaban 抑制凝血酶原和纤维蛋白相关 FXa 活性,IC50 值分别为 2.1 nM和 92 nM。 -
Garadacimab
产品货号 : M36796
cas no: 2162134-62-3
Garadacimab (CSL312) 是一流的全人 IgG4 单克隆抗体,靶向活化因子 XII (FXIIa)。Garadacimab 具有用于遗传性血管性水肿研究的潜力。 -
Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate
产品货号 : M35890
cas no: 503614-91-3
Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate has an inhibitory effect on coagulation factor Xa, and it can be used in the study of thrombophlebitis, atherosclerosis, cerebral embolism, stroke and pulmonary embolism. -
Asundexian
产品货号 : M35121
cas no: 2064121-65-7
Asundexian (BAY 2433334) 是一种口服活性凝血因子 FXIa 抑制剂。Asundexian 直接、有效、可逆地结合 FXIa 的活性位点,从而抑制其活性。Asundexian 抑制缓冲液中的人 FXIa 的 IC50 为 1 nM。 -
Zifaxaban
产品货号 : M34477
cas no: 1378266-98-8
Zifaxaban 是一种具有口服活性、竞争性和选择性 Xa 因子 (FXa) 抑制剂,对人 FXa 的 IC50 为 11.1 nM。Zifaxaban 的选择性比其他丝氨酸蛋白酶高 10000 倍以上。Zifaxaban 可用于动脉和静脉血栓形成研究。