Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Inhibitors & Agonists > Others > Other Targets

Topiroxostat(FYX-051)

  Cat. No.:  DC8037   Featured
Chemical Structure
577778-58-6
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 577778-58-6
Chemical Name: 4-(5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl)picolinonitrile
Synonyms: FYX-051; FYX051; FYX 051; Topiroxostat. trade names Topiloric, Uriadec.
SMILES: N1C(C2C=CN=C(C#N)C=2)=NC(C2C=CN=CC=2)=N1
Formula: C13H8N6
M.Wt: 248.24
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
Target: IC50 value: 5.3 nM [1] Target: xanthine oxidoreductase
In Vivo: FYX-051 exhibited a weak CYP3A4-inhibitory activity (18.6%); its Cmax and bioavailability were as high as 4.62 μg/mL (3 mg/kg) and 69.6%, respectively. Moreover, the t1/2 value of 39 was greater (19.7 h) than that of compound 2 (0.97 h) [1]. In the mechanistic study by 52-week oral treatment with topiroxostat at 3 mg/kg to F344 male rats, with and without citrate, simple and papillary transitional cell hyperplasias of the urinary bladder epithelium were observed in 5/17 in the topiroxostat-alone treatment group, along with xanthine-induced nephropathy, in contrast to neither xanthine crystals nor lesions in urinary organs by co-treatment group with citrate [2].
In Vitro: Steady-state kinetics study showed that FYX-051 initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previously [3]
References: [1]. Sato T, et al. Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected]. Bioorg Med Chem Lett. 2009 Nov 1;19(21):6225-9. [2]. Shimo T, et al. Xanthine crystals induced by topiroxostat, a xanthine oxidoreductase inhibitor, in rats, cause transitional cell tumors. Arch Toxicol. 2014 Jan 22. [3]. Matsumoto K, et al. FYX-051: a novel and potent hybrid-type inhibitor of xanthine oxidoreductase. J Pharmacol Exp Ther. 2011 Jan;336(1):95-103.
MSDS
TITLE DOWNLOAD
MSDS_11884_DC8037_577778-58-6
COA
LOT NO. DOWNLOAD
Cat. No. Product name Field of application
DC82301 IC-8 IC8 is an ionizable cationic lipid. It has been used in combination with other lipids for the formation of lipid nanoparticles (LNPs). Immunization with severe acute respiratory coronavirus 2 (SARS-CoV-2) spike glycoprotein mRNA in IC8- and manganese-containing LNPs induces IgG responses to SARS-CoV-2 Delta and Omicron variants in mice.1 Administration of mRNA encoding B7-H3 X CD3 bispecific T cell engaging (BiTE) antibodies in IC8-containing LNPs reduces tumor growth in MV4-11 and A375 mouse xenograft models.
DC75721 CL2A-SN38 (Govitecan) CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .
DC46471 RP101988 RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
DC37901 PD-173212 PD-173212 is a small molecule N-type calcium channel blocker.
DC37333 N,N-Diethyl-p-toluamide N,N-Diethyl-p-toluamide is a mosquito repellent.
DC37321 AI3-15902 AI3-15902 is a biochemical.
DC37283 Methyl phenylcarbamate Methyl phenylcarbamate is a biochemical.
DC37252 Ampyrone Ampyrone is a metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.
DC37245 Piperonyl butoxide Piperonyl butoxide (PBO) is an organic compound used as a component of pesticide formulations. It is a waxy white solid. It is a synergist. That is, despite having no pesticidal activity of its own, it enhances the potency of certain pesticides such as carbamates, pyrethrins, pyrethroids, and rotenone.[1] It is a semisynthetic derivative of safrole.
DC36443 DC-Chol DC-Chol is a cationic cholesterol derivative. DC-Chol, as a component of lipoplexes with DOPE, has been used for transfection of mRNA into A549 cells without affecting cell viability. Incubation of DC-chol/DOPE liposomes or lipoplexes with human whole blood has no effect on neutrophil elastase or β-thromboglobulin levels or the number of platelets and red and white blood cells, indicating hemocompatibility. DC-Chol has also been widely used in the synthesis of liposomes for the delivery of siRNA, DNA, and chemotherapeutic agents into cells and mice.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia