| Identification | Back Directory | [Name]
3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one | [CAS]
1628224-94-1 | [Synonyms]
EOS-62164
Thrombin inhibitor 6
3-(5-(((5-chlorothiophen-2-yl)methyl)amino)-1-pivaloyl-1H-pyrazol-3-yl)pyridin-2(1H)-one
2(1H)-Pyridinone, 3-[5-[[(5-chloro-2-thienyl)methyl]amino]-1-(2,2-dimethyl-1-oxopropyl)-1H-pyrazol-3-yl]- | [Molecular Formula]
C18H19ClN4O2S | [MOL File]
1628224-94-1.mol | [Molecular Weight]
390.89 |
| Hazard Information | Back Directory | [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 |
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