159776-70-2
Chemical Structure
Melagatran
- CAS No.: 159776-70-2
- Formula:C22H31N5O4
- Molecular Weight:429.51
IUPAC Name: ((R)-2-((S)-2-((4-carbamimidoylbenzyl)carbamoyl)azetidin-1-yl)-1-cyclohexyl-2-oxoethyl)glycine
InChIKey: DKWNMCUOEDMMIN-PKOBYXMFSA-N
SMILES: NC(C(C=C1)=CC=C1CNC([C@@H]2CCN2C([C@@H](C3CCCCC3)NCC(O)=O)=O)=O)=N
Biological Activity: Melagatran is a reversible, selective, orally active direct inhibitor of thrombin with a Ki of 2 nM. Melagatran binds directly to the active site of thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin. Melagatran reduces the DNA binding activity of NF-κB and AP-1. Melagatran reduces fibrin deposition in organs, alleviates ischemic brain damage, and reduces the size of advanced atherosclerotic lesions. Melagatran can be used in the study of cardiovascular disease (coronary thrombosis, atherosclerosis) and ischemic brain damage[1][2][3][4][5][6][7].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Melagatran | 99.31% | Melagatran is a reversible, selective, orally active direct inhibitor of thrombin with a Ki of 2 nM. Melagatran binds directly to the active site of thrombin, inhibiting thrombin-mediated conversion of fibrinogen to fibrin. Melagatran reduces the DNA binding activity of NF-κB and AP-1. Melagatran reduces fibrin deposition in organs, alleviates ischemic brain damage, and reduces the size of advanced atherosclerotic lesions. Melagatran can be used in the study of cardiovascular disease (coronary thrombosis, atherosclerosis) and ischemic brain damage. | ||||||||||||||||||||
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Melagatran-d11 | Melagatran-d11 is the deuterium labeled Melagatran (HY-129056). Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion. | |||||||||||||||||||||
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- [1]. Eriksson M, et al. Effects of melagatran, a novel direct thrombin inhibitor, during experimental septic shock. Expert Opin Investig Drugs. 2000 May;9(5):1129-37. [Content Brief]
- [2]. Mehta JL, et al. Melagatran, an oral active-site inhibitor of thrombin, prevents or delays formation of electrically induced occlusive thrombus in the canine coronary artery. J Cardiovasc Pharmacol. 1998 Mar;31(3):345-51. [Content Brief]
- [3]. Gustafsson D, et al. Effects of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb Haemost. 1998 Jan;79(1):110-8. [Content Brief]
- [4]. Elg M, et al. Antithrombotic effects and bleeding time of thrombin inhibitors and warfarin in the rat. Thromb Res. 1999 May 1;94(3):187-97. [Content Brief]
- [5]. Wang CX, et al. Treatment with melagatran alone or in combination with thrombolytic therapy reduced ischemic brain injury. Exp Neurol. 2008 Sep;213(1):171-5. [Content Brief]
- [6]. Bea F, et al. Melagatran reduces advanced atherosclerotic lesion size and may promote plaque stability in apolipoprotein E-deficient mice. Arterioscler Thromb Vasc Biol. 2006 Dec;26(12):2787-92. [Content Brief]
- [7]. Ainscow EK, et al. Investigations into the liver effects of ximelagatran using high content screening of primary human hepatocyte cultures. Expert Opin Drug Saf. 2008 Jul;7(4):351-65. [Content Brief]
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