Home>>Signaling Pathways>> Metabolism>> Factor Xa>>Otamixaban

Otamixaban

Catalog No.GC17726

Products are for research use only. Not for human use. We do not sell to patients.

Otamixaban Chemical Structure

Cas No.: 193153-04-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$267.00
In stock
5mg
$243.00
In stock
10mg
$378.00
In stock
25mg
$720.00
In stock
50mg
$1,080.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

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.

Background

Otamixaban (FXV673) is a potent, selective, rapid acting, competitive and reversible inhibitor of factor Xa with IC50 value of 0.4 nM.[5]
Factor Xa is a serine endopeptidase which is activated into factor Xa by both factor IX with its cofactor, factor VIII known as intrinsic Xase, and factor VII with its cofactor, tissue factor. Factor Xa (fXa) is a pivotal serine protease situated at the juncture of the intrinsic and extrinsic pathways of the blood coagulation cascade.[2] Its singular role in thrombin activation and potentiating effects on clot formation makes it as a target for therapeutic intervention. FXa is responsible for the initiation of the coagulation cascade,[3] cleaving prothrombin to its active form thrombin, which then acts to convert soluble fibrinogen to insoluble fibrin and to activate platelets. Stabilization of the platelet aggregation by fibrin mesh ultimately leads to clot formation.[4] Thus, the inhibition of fXa (in the physiologically relevant prothrombinase complex) represents an attractive target for the development of novel antithrombotic agents.[5]
Otamixaban (FXV673) selectively and competitively inhibit FXa, suppressing prothrombin activity at the sites of blood clot (thrombus) formation. This leads to a decrease in blood clot formation in a dose dependent manner.[1] Reducing blood clot formation will decrease blood flow blockages, thus possibly lowering the risk of myocardial infarction, unstable angina, venous thrombosis, and ischemic stroke.[6] In conclusion, FXV673 is an effective inhibitor of fXa in the physiologically relevant human prothrombinase complex. Recently a new series of specific, direct acting inhibitors of Factor Xa has been developed. And they may be more effective against Factor Xa in that they inhibit both free Factor Xa and Factor Xa in the prothrombinase complex.[7]
References:
1.K. R. Guertin et al. Optimization of the-Aminoester Class of Factor Xa Inhibitors.Part 2: Identification of FXV673 as a Potent and Selective Inhibitor with Excellent In Vivo Anticoagulant Activity. Bioorg. Med. Chem. Lett. 12 (2002) 1671–1674.
2.Meyer-Michel Samama. et al. Monitoring plasma levels of factor Xa inhibitors: how, why and when? Expert Rev. Hematol.2013, 6(2), 155-164.
3.Rebello SS1. et al. Antithrombotic efficacy of a novel factor Xa inhibitor, FXV673, in a canine model of coronary artery thrombolysis. Br J Pharmacol. 2001 Aug;133(7):1190-8.
4.Valeria Chu. et al. Pharmacological Characterization of a Novel Factor Xa Inhibitor, FXV673. Thrombosis Research 103 (2001) 309–324.
5.Katsung, B., S. Masters and A. Trevor. Basic and Clinical Pharmacology 11th Edition. United States of America: McGraw-Hill, 2009.
6.Rebello SS1. et al. Role of short-term inhibition of factor Xa by FXV673 in arterial passivation: a study in a chronic model of thrombosis in conscious dogs. J Cardiovasc Pharmacol. 2001,38(2):288-97.
7.Turpie AG. "Oral, Direct Factor Xa Inhibitors in Development for the Prevention and Treatment of Thromboembolic Diseases". Arterioscler Thromb Vasc Biol,2007,27 (6): 1238-47.

Chemical Properties

Cas No. 193153-04-7 SDF
Chemical Name methyl (2R,3R)-2-[(3-carbamimidoylphenyl)methyl]-3-[[4-(1-oxidopyridin-1-ium-4-yl)benzoyl]amino]butanoate
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-]
Formula C25H26N4O4 M.Wt 446.53
Solubility ≥ 22.35 mg/mL in DMSO, ≥ 55 mg/mL in EtOH with gentle warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.2395 mL 11.1975 mL 22.3949 mL
5 mM 0.4479 mL 2.2395 mL 4.479 mL
10 mM 0.2239 mL 1.1197 mL 2.2395 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for Otamixaban

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for Otamixaban

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.