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Betrixaban maleate

Catalog No. T4980 CAS 936539-80-9

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

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Betrixaban maleate, CAS 936539-80-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
5 mg	In stock	$ 79.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 225.00
50 mg	In stock	$ 396.00
100 mg	In stock	$ 593.00
500 mg	In stock	$ 1,290.00

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Purity: 99.46%

Purity: 98.81%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.
Targets&IC50	FXa:1.5nM
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)
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[1]. 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[2].
Kinase Assay	To measure the inhibition of fXa activity by direct fXa inhibitors and the reversal of its inhibitory effect by r-Antidote, purified human plasma fXa (3 nM) (Haematologic Technologies), varying concentrations of inhibitor (0, 2.5, 5.0 and 7.5 nM) and r-Antidote are added to the assay buffer (20 mM Tris, 150 mM NaCl, 5 mM Ca2+ and 0.1% BSA, pH 7.4). After incubation at room temperature for 30 min, 100 μM Spectrozyme-fXa is added to the mixture, and the initial rate of sub?strate cleavage is monitored continuously for 5 min at 405 nm in a 96-well plate reader. The initial velocity of product formation as a function of inhibitor and r-Antidote concentrations is analyzed by Dynafit to estimate the binding affinity of r-Antidote to each inhibitor[2]. .
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.

Molecular Weight	567.98
Formula	C27H26ClN5O7
CAS No.	936539-80-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22mg/mL

References and Literature

1. Zhang P, et al. Discovery of Betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):21 2. Lu G, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51.

Related compound libraries

This product is contained In the following compound libraries：

EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cardiovascular Disease Compound Library Bioactive Compound Library FDA-Approved & Pharmacopeia Drug Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max Anti-Aging Compound Library

Related Products

Related compounds with same targets

Dechloro Rivaroxaban Fidexaban Rivaroxaban Impurity Rivaroxaban Rivaroxaban-d4 Zifaxaban Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate Betrixaban

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Keywords

Betrixaban maleate 936539-80-9 Metabolism Factor Xa Inhibitor PRT 054021 PRT-054021 Betrixaban Maleate Betrixaban antithrombotic effect Fxa PRT054021 inhibit inhibitor

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