Melagatran

CAT: 0804-HY-129056-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-129056-01Size:1 mg
Selected
PRICE
AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
Product image 1
1 / 1
Description
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].
CAS Number
[159776-70-2]
UNSPSC
12352005
Hazard Statement
H315-H319-H335
Target
AP-1; NF-κB; Thrombin
Type
Reference compound
Related Pathways
Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/melagatran.html
Purity
99.31
Solubility
DMSO : 175 mg/mL (ultrasonic)
Smiles
NC(C(C=C1)=CC=C1CNC([C@@H]2CCN2C([C@@H](C3CCCCC3)NCC(O)=O)=O)=O)=N
Molecular Formula
C22H31N5O4
Molecular Weight
429.51
Precautions
P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501
References & Citations
[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.|[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.|[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. |[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. |[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. |[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. |[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3

Alternative Products

CatalogName
TRC-M208450-5MGMelagatran
A19083-100Melagatran 100mg
MF-0144085-01Melagatran monohydrate
TRC-M208452-0.25MGMelagatran-d11
A19083-5Melagatran 5mg
A19083-25Melagatran 25mg
A19083-1Melagatran 1mg
A19083-50Melagatran 50mg
A19083-10Melagatran 10mg
sc-212214N-Hydroxy Melagatran

Popular Products