Betrixaban maleate

SKU: orb1302397

Description

Betrixaban is a selective, reversible factor Xa inhibitor developed as a non-vitamin K oral anticoagulant. It is used for venous thromboembolism (VTE) prophylaxis and is a valuable research tool for studying coagulation pathways in both in vitro enzymatic assays and in vivo thrombosis models.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	936539-80-9
MW	567.98
Purity	99.86% (May vary between batches)
Formula	C₂₇H₂₆ClN₅O₇
SMILES	OC(=O)\C=C/C(O)=O.COc1ccc(NC(=O)c2ccc(cc2)C(=N)N(C)C)c(c1)C(=O)Nc1ccc(Cl)cn1
Target	Factor Xa
Solubility	DMSO:50 mg/mL (88.03 mM)

Bioactivity

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Target IC50	FXa:1.5nM
In Vivo	Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey. Both Betrixaban and Apixa-ban-mediated whole-blood INR increases are similarly reversed by r-Antidote. After i.v. infusion of the three fXa inhibitors (each admin istered individually) for 30 min, the total plasma concentrations of rivaroxaban, Betrixaban and apixaban are 1.4±0.4 μM (mean±s.d.), 0.2±0.01 μM and 1.4±0.3 μM, respectively, and the percentages of unbound inhibitor are 2.2%±0.8% (mean±s.d.), 40%±7.2% and 1.5%±0.3%, respectively. After administration of r-Antidote, the total plasma concentrations of the inhibitors increased to 1.9±0.09 μM, 2.0±0.4 μM and 4.2±0.7 μM, respectively, and the percentage of unbound inhibitor declined to 0%, 0.3%±0.1% and 0.05%±0.02%, respectively. Thus, for each of the three inhibitors, correction of prothrombin time by r-Antidote to near-normal values is associated with a reduction in the free fraction of the inhibitor. Read more...
In Vitro	In patch clamp hERG assays, Betrixaban has IC50 of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki 0.5 μM) Read more...
Animal Research	Whole-blood INR values (mean±s.d.) in rats infused with Betrixaban (1 mg/kg per hour) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6 mg) over 5 min plus infusion (9 mg/h) for up to 90 min. Circles, vehicle+vehicle; squares, Betrixaban + vehicle; triangles, Betrixaban + r-Antidote. P≤0.02 compared to the r-Antidote treatment group determined by unpaired two-tailed t test. Whole-blood INR values (mean±s.d.) in rats infused with Apixaban (0.5 mg per kg body weight h 1) or vehicle and then treated with either vehicle or r-Antidote by i.v. bolus (6 mg) over 5 min plus infusion (6 mg/h) for up to 90 min. Circles, vehicle + vehicle; squares, apixaban + vehicle; triangles, apixaban+r-Antidote. P≤0.01 compared to the r-Antidote treatment group determined by unpaired two-tailed t test. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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antithrombotic effect, Betrixaban, Betrixaban Maleate, Betrixaban maleate, FactorXa, Factor Xa, Fxa, Inhibitor, inhibit, PRT 054021, PRT054021, PRT-054021

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Compound Identifiers

PubChem CID

16069304 ↗

Key Properties

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No computed properties available.

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