1. Metabolic Enzyme/Protease
  2. Xanthine Oxidase
    Cytochrome P450
  3. Topiroxostat

Topiroxostat (Synonyms: FYX-051)

Cat. No.: HY-14874 Purity: 99.68%
Handling Instructions

Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.

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

Topiroxostat Chemical Structure

Topiroxostat Chemical Structure

CAS No. : 577778-58-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 50 In-stock
Estimated Time of Arrival: December 31
25 mg USD 75 In-stock
Estimated Time of Arrival: December 31
50 mg USD 125 In-stock
Estimated Time of Arrival: December 31
100 mg USD 205 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment[1][2].

IC50 & Target

IC50: 5.3 nM (XOR)[1]
Ki: 5.7 nM (XOR)[2]

In Vitro

These potent and more sustained effects of Topiroxostat (FYX-051, compound 39) have been confirmed by a crystallographic analysis of XOR-Topiroxostat complex. The cyano group of Topiroxostat has been reported to play an important role in the binding activity between Topiroxostat and XOR. This is attributable to the formation of a hydrogen bond between Asn 768 of XOR and the cyano group of Topiroxostat[1].

In Vivo

Topiroxostat (FYX-051; 0.03-10 mg/kg; oral administration; for 1 hour; male Wistar/ST strain rats) treatment shows a potent and long-lasting hypouricemic effect in a rat model of potassium oxonate-induced hyperuricemia[2] .
The Cmax and bioavailability of Topiroxostat (FYX-051, compound 39) are as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of Topiroxostat is 19.7 hours[1].

Animal Model: Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate[2]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg
Administration: Oral administration; for 1 hour
Result: Caused a dose-dependent decrease in serum urate levels with an extremely low ED50 of 0.15 mg/kg, evaluated at 1 h after oral administration.
Clinical Trial
Molecular Weight

248.24

Formula

C₁₃H₈N₆

CAS No.

577778-58-6

SMILES

N#CC1=NC=CC(C2=NNC(C3=CC=NC=C3)=N2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 23.5 mg/mL (94.67 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0284 mL 20.1418 mL 40.2836 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL
10 mM 0.4028 mL 2.0142 mL 4.0284 mL
*Please refer to the solubility information to select the appropriate solvent.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TopiroxostatFYX-051FYX051FYX 051Xanthine OxidaseCytochrome P450XOCYPsXORAsn 768uricacidhyperuricemiaCYP3A4pharmacokineticInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Topiroxostat
Cat. No.:
HY-14874
Quantity:
MCE Japan Authorized Agent: