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Betrixaban hydrochloride(330942-05-7(free base))

Catalog No. T4690 CAS T4690

Synonyms: PRT054021 hydrochloride

Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) is a potent, selective, and orally efficacious factor Xa (fXa) inhibitor (IC50: 1.5 nM).

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Betrixaban hydrochloride(330942-05-7(free base)) Chemical Structure

Betrixaban hydrochloride(330942-05-7(free base)), CAS T4690

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
2 mg	In stock	$ 55.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 156.00
25 mg	In stock	$ 355.00
50 mg	In stock	$ 547.00
100 mg	In stock	$ 788.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 99.54%

Biological Description

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Description	Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) is a potent, selective, and orally efficacious factor Xa (fXa) inhibitor (IC50: 1.5 nM).
Targets&IC50	FXa:1.5 nM
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)[1].
In vivo	Betrixaban (0.5 mg/kg, i.v. and 2.5 mg/kg, p.o.) 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].

Synonyms	PRT054021 hydrochloride
Molecular Weight	488.36
Formula	C23H23Cl2N5O3
CAS No.	T4690

Storage

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

Solubility Information

DMSO: 20 mg/mL (44.26 mM)

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):2179-85. 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 Bioactive Compounds Library Max NO PAINS Compound Library FDA-Approved & Pharmacopeia Drug Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library FDA-Approved Drug Library

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Keywords

Betrixaban hydrochloride(330942-05-7(free base)) T4690 Metabolism Factor Xa PRT054021 hydrochloride Betrixaban hydrochloride(330942057(free base)) PRT054021 Hydrochloride PRT 054021 Hydrochloride PRT-054021 Hydrochloride Betrixaban hydrochloride(330942 05 7(free base)) inhibitor inhibit

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