[CAS NO. 193153-04-7]  Otamixaban

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PRODUCTS SPECIFICATIONS [193153-04-7]

Fulfillment
Catalog
AS906406
Brand
Arctom Scientific
CAS
193153-04-7

DESCRIPTION [193153-04-7]

Overview

MDLMFCD11100277
Molecular Weight446.50
Molecular FormulaC25H26N4O4
SMILESN=C(C1=CC=CC(C[C@@H](C(OC)=O)[C@H](NC(C2=CC=C(C=C2)C3=CC=[N+]([O-])C=C3)=O)C)=C1)N

For research use only. We do not sell to patients.

Summary

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. IC50 value: Target: Factor Xa Otamixaban is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa. In vivo experiments have demonstrated that Otamixaban is highly efficacious in rodent, canine and porcine models of thrombosis. In addition, recent clinical findings indicate that Otamixaban is efficacious, safe and well tolerated in humans and therefore has considerable potential for the treatment of acute coronary syndrome. This review article chronicles the discovery and pre-clinical data surrounding the fXa inhibitor Otamixaban as well as the recent clinical findings in humans.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00317395 Sanofi
Coronary Disease
June 2006 Phase 2
NCT00133731 Sanofi
Angioplasty, Transluminal, Percutaneous Coronary
September 2004 Phase 2
NCT01126086 Sanofi
Hepatic Impairment
May 2010 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 111.98 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Benzenepropanoic acid, 3-(aminoiminomethyl)-α-[(1R)-1-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]ethyl]-, methyl ester, (αR)-
Benzenepropanoic acid, 3-(aminoiminomethyl)-α-[1-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]ethyl]-, methyl ester, [R-(R*,R*)]-
FXV 673
Methyl (2R,3R)-2-[3-amidinobenzyl]-3-[[4-(1-oxido-4-pyridinyl)benzoyl]amino]butanoate
Otamixaban