Otamixaban
Otamixaban (CAS 193153-04-7), also known as FXV673, is a selective, reversible, competitive inhibitor of coagulation factor Xa (FXa). Factor Xa, a serine protease located centrally in the coagulation cascade, converts prothrombin to thrombin, leading to fibrin formation and platelet activation critical for clot development. Otamixaban inhibits both free and clot-bound FXa, demonstrated by an IC50 value of 0.4 nM, consequently reducing thrombin generation and subsequent fibrin production. Otamixaban is used in research related to thrombosis, myocardial infarction, ischemic stroke, and unstable angina.
| Storage | Store at -20°C |
| M.Wt | 446.53 |
| Cas No. | 193153-04-7 |
| Formula | C25H26N4O4 |
| Synonyms | FXV 673; FXV-673; FXV673 |
| Solubility | ≥22.35 mg/mL in DMSO; insoluble in H2O; ≥55 mg/mL in EtOH with gentle warming |
| Chemical Name | methyl (2R,3R)-2-[(3-carbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate |
| SDF | Download SDF |
| Canonical SMILES | CC(C(CC1=CC=CC(=C1)C(=N)N)C(=O)OC)NC(=O)C2=CC=C(C=C2)C3=CC=[N+](C=C3)[O-] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Vitro experiment [1]: | |
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Samples |
plasma derived from humans, primates, dogs, rabbits and rats |
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Preparation method |
The solubility of this compound in DMSO is >22.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
100 ng/mL |
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Applications |
The anticoagulant effect of Otamixaban in plasma was rabbit>human>monkey>rat>dog. Humans were approximately 2.5 fold more sensitive to otamixaban than dogs in both the PT and aPTT assays. 100 ng/mL would be the effective plasma concentration to target for human clinical studies. |
| Animal experiment [1]: | |
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Animal models |
rat model of ferrous chloride-induced arterial thrombosis |
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Dosage form |
50 μg/kg bolus and 5 μg/kg/min i.v. maintenance infusion |
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Application |
In rat model of ferrous chloride-induced arterial thrombosis, Otamixaban exhibited a dose-dependent increase in time to occlusion with a maximal effective dose at about 50 μg/kg bolus and 5 μg/kg/min i.v. maintenance infusion. Compared to control, this dose caused a 40% reduction in thrombus mass. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Guertin KR1, Choi YM. The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development. Curr Med Chem. 2007;14(23):2471-81. | |
| Description | Otamixaban(FXV673) is a potent, selective, rapid acting, competitive and reversible inhibitor of fXa with a Ki value of 0.5 nM. | |||||
| Targets | Factor Xa | |||||
| IC50 | 0.5 nM (Ki) | |||||
Quality Control & MSDS
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Chemical structure
