Molecular structure of BMS-740808, CAS Number: 280118-23-2
BMS-740808 (CAS 280118-23-2)
Application:
BMS-740808 is a highly potent, selective inhibitor of Factor X
CAS Number:
280118-23-2
Molecular Weight:
588.58
Molecular Formula:
C31H27F3N6O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Description
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SDS & Certificate of Analysis
BMS-740808 is a highly potent, selective inhibitor of Factor X, with Ki of 0.03 nM. BMS-740808 is highly potent with a rapid onset of inhibition (2.7 × 107 M-1 s-1), selective (>1000-fold over other proteases), efficacious in the AVShunt thrombosis model. BMS-740808 is synthesized by modification of employing bicyclic pyrazolo-pyridinone scaffold to Razaxaban, a pyrazole based Factor X inhibitor. Especially for BMS-740808, the introduction of a 3(R)-hydroxyl moiety on the pyrrolidine ring results in a significant enhancement in potency. BMS-740808 also shows the high affinity for thrombin.
BMS-740808 (CAS 280118-23-2) References
- 1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa. | Pinto, DJ., et al. 2006. Bioorg Med Chem Lett. 16: 4141-7. PMID: 16730984
- Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties. | Pinto, DJ., et al. 2006. Bioorg Med Chem Lett. 16: 5584-9. PMID: 16963264
- Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors. | Varnes, JG., et al. 2008. Bioorg Med Chem Lett. 18: 749-54. PMID: 18054227
- Preclinical discovery of apixaban, a direct and orally bioavailable factor Xa inhibitor. | Wong, PC., et al. 2011. J Thromb Thrombolysis. 31: 478-92. PMID: 21318583
- Advances in Inhibitors of FXa. | Guo, L. and Ma, S. 2015. Curr Drug Targets. 16: 1207-32. PMID: 25981610
- Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors. | Hao, X., et al. 2019. Expert Opin Drug Discov. 14: 915-931. PMID: 31172842
Inhibitor of:
Factor X.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
BMS-740808, 10 mg | sc-364445 | 10 mg | $480.00 | |||
BMS-740808, 50 mg | sc-364445A | 50 mg | $1455.00 |