Argatroban (74863-84-6) is a potent and selective inhibitor of thrombin (Ki = 19 nM)1. Prevents platelet-rich arterial thrombosis in a rabbit model2. Ameliorates early brain injury and improves neurological outcomes after subarachnoid hemorrhage in a rat model3. Argatroban reduces breast cancer malignancy and metastasis via osteopontin-dependent and independent mechanisms4.
1) Kikumoto et al. (1984), Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl++ +)sulfonyl]-l-arginyl)]-2-piperidinecarboxylic acid; Biochemistry, 23 85
2) Jang et al. (1990), Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition; Circulation, 81 219
3) Sugawara et al. (2009), Thrombin inhibition by argatroban ameliorates early brain injury and improves neurological outcomes after experimental subarachnoid hemorrhage in rats; Stroke, 40 1530
4) Schulze et al. (2008), The thrombin inhibitor Argatroban reduces breast cancer malignancy and metastasis via osteopontin-dependent and osteopontin-independent mechanisms; Breast Cancer Res. Treat., 112 243