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

BMS-654457 

Cat. No.: HY-12631
Handling Instructions

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

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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].

Molecular Weight

603.71

Formula

C₃₆H₃₇N₅O₄

CAS No.

1004551-41-0

SMILES

NC(C1=CC=C(N[[email protected]](C2=CC(C3=CC=C(C(N)=O)C=C3C(O)=O)=CC(NC(CC(C)C)=O)=C2)C[[email protected]]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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BMS-654457
Cat. No.:
HY-12631
Quantity: