3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one manufacturers
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| | 3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one Basic information |
| | 3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one Chemical Properties |
| density | 1.38±0.1 g/cm3(Predicted) | | pka | 10.30±0.10(Predicted) |
| | 3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one Usage And Synthesis |
| Uses | Thrombin inhibitor 6 is a potent thrombin inhibitor (IC50: 1 nM). Thrombin inhibitor 6 has the function as an anticoagulant[1]. | | in vivo | Thrombin inhibitor 6 (compound 73) (9 mg/kg, i.v.) prolongs the tail bleeding time in CD-1 mice[1]. Thrombin inhibitor 6 (5 mg/kg, p.o.) shows F(%) of 22.8%, AUC of 713.3 h.ng/mL and Cmax of 127 ng/mL in male CD-1 mice[1].
| Animal Model: | CD-1 mice[1] | | Dosage: | 9 mg/kg | | Administration: | Intravenous injection (i.v.) | | Result: | The mice bled for 25 min following transection.
Led to 1.5-fold increase of liberated whole blood cells.
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| | References | [1] Short KM, et al. Discovery of novel N-acylpyrazoles as potent and selective thrombin inhibitors. Eur J Med Chem. 2022 Oct 27;246:114855. DOI:10.1016/j.ejmech.2022.114855 |
| | 3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one Preparation Products And Raw materials |
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