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Otamixaban

Catalog No.
A3690
Direct factor Xa inhibitors,potent and selective
Grouped product items
SizePriceStock Qty
10mg
$450.00
In stock
100mg
$1,150.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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.

Chemical Properties

StorageStore at -20°C
M.Wt446.53
Cas No.193153-04-7
FormulaC25H26N4O4
SynonymsFXV 673; FXV-673; FXV673
Solubility≥22.35 mg/mL in DMSO; insoluble in H2O; ≥55 mg/mL in EtOH with gentle warming
Chemical Namemethyl (2R,3R)-2-[(3-carbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate
SDFDownload SDF
Canonical SMILESCC(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 ConditionSmall 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.

Protocol

Vitro experiment [1]:

Samples

plasma derived from humans, primates, dogs, rabbits and rats

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.

Reacting condition

100 ng/mL

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]:

Animal models

rat model of ferrous chloride-induced arterial thrombosis

Dosage form

50 μg/kg bolus and 5 μg/kg/min i.v. maintenance infusion

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.

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.

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.

Biological Activity

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)          

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