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Asundexian

Cat. No. M21060
Asundexian Structure
Synonym:

BAY-2433334

Size Price Availability Quantity
5mg USD 575  USD575 In stock
10mg USD 940  USD940 In stock
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Quality Control & Documentation
Biological Activity

Asundexian (BAY2433334) is a reversible inhibitor of the active site of Factor XIa. Asundexian inhibits the activity of FXIa by directly, efficiently, and reversibly binding to its active site. the IC50 of human FXIa in Asundexian inhibition buffer is 1 nM.

Chemical Information
Molecular Weight 592.93
Formula C26H21ClF4N6O4
CAS Number 2064121-65-7
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ashkan Shoamanesh, et al. Lancet. Factor XIa inhibition with asundexian after acute non-cardioembolic ischaemic stroke (PACIFIC-Stroke): an international, randomised, double-blind, placebo-controlled, phase 2b trial

[2] Sunil V Rao, et al. Circulation. A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction

[3] David Gailani. Lancet. Making anticoagulation safer

[4] Jonathan P Piccini, et al. Lancet. Safety of the oral factor XIa inhibitor asundexian compared with apixaban in patients with atrial fibrillation (PACIFIC-AF): a multicentre, randomised, double-blind, double-dummy, dose-finding phase 2 study

[5] Stefan Heitmeier, et al. J Thromb Haemost. Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa

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Keywords: Asundexian, BAY-2433334 supplier, Factor Xa, inhibitors, activators

 
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