Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) is a potent, selective, and orally efficacious factor Xa (fXa) inhibitor (IC50: 1.5 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (44.26 mM)
You can also refer to dose conversion for different animals. More
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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