2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. Betrixaban maleate

Betrixaban maleate  (Synonyms: PRT054021 maleate)

Cat. No.: HY-10268A Purity: 99.78%
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Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect.

For research use only. We do not sell to patients.

Betrixaban maleate Chemical Structure

Betrixaban maleate Chemical Structure

CAS No. : 936539-80-9

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Based on 4 publication(s) in Google Scholar

Other Forms of Betrixaban maleate:

Betrixaban maleate Related Antibodies

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Description

Betrixaban (PRT054021) maleate is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor with an IC50 of 1.5 nM. Betrixaban maleate shows antithrombotic effect[1][3].

IC50 & Target

IC50: 1.5 nM (fXa)[1]
Ki: 0.117 nM (fXa), 1.8 μM (hERG)[1]
In Vitro

Betrixaban (PRT054021) shows IC50 of 8.9 μM in patch clamp hERG assays[1].
Betrixaban shows an IC50 and a Ki of 6.3 μM and 3.5 μM for the plasma kallikrein, respectively[1].
Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM)[1].
Betrixaban (5-25 ng/mL) inhibits thrombin generation[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Betrixaban maleate Related Antibodies
In Vivo

Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has oral bioavailability of 51.6% in dog[1].
Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has oral bioavailability of 58.7% in monkey[1].
Betrixaban mediated whole-blood INR increase is reversed by r-Antidote. After i.v. infusion for 30 min, the total plasma concentrations of Betrixaban is 0.2±0.01 μM, and the percentages of unbound inhibitor is 40%±7.2%. After administration of r-Antidote, the total plasma concentration increased to 2.0±0.4 μM, and the percentage of unbound inhibitor declined to 0.3%±0.1%[2].
Betrixaban (3 mg/kg) shows nearly comparable inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs 96% inhibition) in the rabbit abdominal vena cava model of clot accretion on cotton threads[3].
Betrixaban (19.1 mg/kg) is at least as effective at maintaining patency as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs 70% vs 80% patency, respectively) in the ferric chloride injury model of rodent carotid artery[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

567.98

Formula

C27H26ClN5O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(N(C)C)C(C=C1)=CC=C1C(NC2=CC=C(OC)C=C2C(NC(C=C3)=NC=C3Cl)=O)=O.O=C(O)/C=C\C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (88.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7606 mL 8.8031 mL 17.6063 mL
5 mM 0.3521 mL 1.7606 mL 3.5213 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7606 mL 8.8031 mL 17.6063 mL 44.0156 mL
5 mM 0.3521 mL 1.7606 mL 3.5213 mL 8.8031 mL
10 mM 0.1761 mL 0.8803 mL 1.7606 mL 4.4016 mL
15 mM 0.1174 mL 0.5869 mL 1.1738 mL 2.9344 mL
20 mM 0.0880 mL 0.4402 mL 0.8803 mL 2.2008 mL
25 mM 0.0704 mL 0.3521 mL 0.7043 mL 1.7606 mL
30 mM 0.0587 mL 0.2934 mL 0.5869 mL 1.4672 mL
40 mM 0.0440 mL 0.2201 mL 0.4402 mL 1.1004 mL
50 mM 0.0352 mL 0.1761 mL 0.3521 mL 0.8803 mL
60 mM 0.0293 mL 0.1467 mL 0.2934 mL 0.7336 mL
80 mM 0.0220 mL 0.1100 mL 0.2201 mL 0.5502 mL
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Betrixaban maleate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Betrixaban936539-80-9PRT054021PRT 054021PRT-054021Factor XaFxaantithrombotic effectInhibitorinhibitorinhibit

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