2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. BMS-654457

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.

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

BMS-654457 Chemical Structure

BMS-654457 Chemical Structure

CAS No. : 1004551-41-0

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BMS-654457 Related Antibodies

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Description

BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.

In Vitro

BMS-654457 shows comparable in vitro potency against FXIa in humans (Ki=0.2 nM) and in rabbits (Ki =0.42 nM), and was over 500-fold selective against coagulation-related proteases (thrombin, FXa and FVIIa) in these species[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BMS-654457 Related Antibodies
In Vivo

BMS-654457 is effective in the prevention of arterial thrombosis in rabbits with limited effects on bleeding time. BMS-654457 is a promising antithrombotic therapy with a wide therapeutic window[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

603.71

Formula

C36H37N5O4
CAS No.
SMILES

NC(C1=CC=C(N[C@H](C2=CC(C3=CC=C(C(N)=O)C=C3C(O)=O)=CC(NC(CC(C)C)=O)=C2)C[C@]4(C)C5=CC=CC=C5)C4=C1)=N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Cell Assay

Platelet aggregation is measured in hirudin-treated rabbit platelet-rich plasma (PRP) with a platelet aggregometer. PRP is mixed with 2.5 μL of vehicle or BMS-654457 at 1 and 10 μM and incubated for 2 min at 37°C. Peak platelet aggregation is determined after the addition of 2.5 μL of the agonist (ADP at 10 μM, arachidonic acid at 250 μM and collagen at 10 μg/mL, final concentration)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rabbits[1]

[1]BMS-654457 or vehicle (10 % N-N-dimethylacetamide:90 % of 5 % dextrose) is administered as a bolus plus sustaining IV infusion begun 30 min prior to each protocol. Treatment groups include BMS-654457 (mg/kg+mg/kg/h) at 0.011+0.008, 0.037+0.027, 0.11+0.08, 0.37+0.27 and 1.1 +0.8 or vehicle (n=6 per group). The plasma concentration that increased iCBF to EC50 was estimated for BMS654457[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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BMS-654457 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-6544571004551-41-0BMS654457BMS 654457Factor XaFxaInhibitorinhibitorinhibit

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