Betrixaban
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 319884

CAS#: 330942-05-7

Description: Betrixaban, also known as PRT054021, MK-4448; PRT-021; PRT-054021; MLN-1021, is a potent, orally active and highly selective factor Xa inhibitor undergone human clinical trials for prevention of embolism after knee surgery, and prevention of stroke following atrial fibrillation. Betrixaban is currently being studied in a human clinical trial for extended duration thromboprophylaxis to prevent venous thromboembolism in acute medically ill patients.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2950
Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 4250
Size
Price

50mg
USD 450
500mg
USD 1650
5g
Ask price

Betrixaban, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 319884
Name: Betrixaban
CAS#: 330942-05-7
Chemical Formula: C23H22ClN5O3
Exact Mass: 451.1411
Molecular Weight: 451.911
Elemental Analysis: C, 61.13; H, 4.91; Cl, 7.84; N, 15.50; O, 10.62


Synonym: PRT054021; PRT 054021; PRT-054021; PRT054,021; PRT 054,021; PRT-054,021; MK-4448; PRT-021; MLN-1021; Betrixaban.

IUPAC/Chemical Name: N-(5-Chloropyridin-2-yl)-2-((4-(N,N-dimethylcarbamimidoyl)benzoyl)amino)-5- methoxybenzamide

InChi Key: XHOLNRLADUSQLD-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H22ClN5O3/c1-29(2)21(25)14-4-6-15(7-5-14)22(30)27-19-10-9-17(32-3)12-18(19)23(31)28-20-11-8-16(24)13-26-20/h4-13,25H,1-3H3,(H,27,30)(H,26,28,31)

SMILES Code: O=C(NC1=NC=C(Cl)C=C1)C2=CC(OC)=CC=C2NC(C3=CC=C(C(N(C)C)=N)C=C3)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Chan NC, Bhagirath V, Eikelboom JW. Profile of betrixaban and its potential in the prevention and treatment of venous thromboembolism. Vasc Health Risk Manag. 2015 Jun 26;11:343-51. doi: 10.2147/VHRM.S63060. eCollection 2015. Review. PubMed PMID: 26170684; PubMed Central PMCID: PMC4489817.

2: Cohen AT, Harrington R, Goldhaber SZ, Hull R, Gibson CM, Hernandez AF, Gold A. Recognition of biomarker identified high-risk patients in the acute medically ill venous thromboembolism prevention with extended duration betrixaban study resulting in a protocol amendment. Am Heart J. 2015 Jan;169(1):186-7. doi: 10.1016/j.ahj.2014.09.004. Epub 2014 Sep 19. PubMed PMID: 25497265.

3: Meddahi S, Samama MM. [Pharmacologic and clinical characteristics of direct inhibitors of factor Xa: rivaroxaban, apixaban, edoxaban and betrixaban]. J Mal Vasc. 2014 May;39(3):183-94. doi: 10.1016/j.jmv.2014.02.001. Epub 2014 Mar 18. Review. French. PubMed PMID: 24650612.

4: Cohen AT, Harrington R, Goldhaber SZ, Hull R, Gibson CM, Hernandez AF, Kitt MM, Lorenz TJ. The design and rationale for the Acute Medically Ill Venous Thromboembolism Prevention with Extended Duration Betrixaban (APEX) study. Am Heart J. 2014 Mar;167(3):335-41. doi: 10.1016/j.ahj.2013.11.006. Epub 2013 Dec 10. PubMed PMID: 24576517.

5: Chan NC, Hirsh J, Ginsberg JS, Eikelboom JW. Betrixaban (PRT054021): pharmacology, dose selection and clinical studies. Future Cardiol. 2014 Jan;10(1):43-52. doi: 10.2217/fca.13.98. PubMed PMID: 24344662.

6: Palladino M, Merli G, Thomson L. Evaluation of the oral direct factor Xa inhibitor - betrixaban. Expert Opin Investig Drugs. 2013 Nov;22(11):1465-72. doi: 10.1517/13543784.2013.825605. Epub 2013 Aug 22. Review. PubMed PMID: 23964817.

7: Connolly SJ, Eikelboom J, Dorian P, Hohnloser SH, Gretler DD, Sinha U, Ezekowitz MD. Betrixaban compared with warfarin in patients with atrial fibrillation: results of a phase 2, randomized, dose-ranging study (Explore-Xa). Eur Heart J. 2013 May;34(20):1498-505. doi: 10.1093/eurheartj/eht039. Epub 2013 Mar 13. PubMed PMID: 23487517; PubMed Central PMCID: PMC3659305.

8: Morganroth J, Gretler DD, Hollenbach SJ, Lambing JL, Sinha U. Absence of QTc prolongation with betrixaban: a randomized, double-blind, placebo- and positive-controlled thorough ECG study. Expert Opin Pharmacother. 2013 Jan;14(1):5-13. doi: 10.1517/14656566.2013.753057. Epub 2012 Dec 10. PubMed PMID: 23216423.

9: Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenz amide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3. PubMed PMID: 19297154.

10: Turpie AG, Bauer KA, Davidson BL, Fisher WD, Gent M, Huo MH, Sinha U, Gretler DD; EXPERT Study Group. A randomized evaluation of betrixaban, an oral factor Xa inhibitor, for prevention of thromboembolic events after total knee replacement (EXPERT). Thromb Haemost. 2009 Jan;101(1):68-76. PubMed PMID: 19132191.