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Otamixaban

Cat. No. M29033
Otamixaban Structure
Synonym:

FXV673

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Quality Control & Documentation
Biological Activity

Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.

Chemical Information
Molecular Weight 446.5
Formula C25H26N4O4
CAS Number 193153-04-7
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Philippe Gabriel Steg, et al. JAMA. Anticoagulation with otamixaban and ischemic events in non-ST-segment elevation acute coronary syndromes: the TAO randomized clinical trial

[2] John W Eikelboom, et al. Lancet. Otamixaban in acute coronary syndromes

[3] Marc S Sabatine, et al. Lancet. Otamixaban for the treatment of patients with non-ST-elevation acute coronary syndromes (SEPIA-ACS1 TIMI 42): a randomised, double-blind, active-controlled, phase 2 trial

[4] Kevin R Guertin, et al. Curr Med Chem. The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development

[5] Edith A Nutescu, et al. IDrugs. Drug evaluation: the directly activated Factor Xa inhibitor otamixaban

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Keywords: Otamixaban, FXV673 supplier, Factor Xa, inhibitors, activators


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