Topiroxostat
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MedKoo CAT#: 314261

CAS#: 577778-58-6

Description: Topiroxostat (INN; trade names Topiloric, Uriadec) is a drug for the treatment of gout and hyperuricemia. It was approved for use in Japan in June 2013. Topiroxostat is a xanthine oxidase inhibitor which reduces serum urate levels.


Chemical Structure

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Topiroxostat
CAS# 577778-58-6

Theoretical Analysis

MedKoo Cat#: 314261
Name: Topiroxostat
CAS#: 577778-58-6
Chemical Formula: C13H8N6
Exact Mass: 248.08104
Molecular Weight: 248.24
Elemental Analysis: C, 62.90; H, 3.25; N, 33.85

Price and Availability

Size Price Availability Quantity
10.0mg USD 150.0 2 Weeks
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 650.0 2 Weeks
200.0mg USD 950.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2250.0 2 Weeks
2.0g USD 3250.0 2 Weeks
5.0g USD 4250.0 2 Weeks
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Synonym: FYX051; FYX051; FYX 051; Topiroxostat. trade names Topiloric Uriadec.

IUPAC/Chemical Name: 4-(5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl)picolinonitrile

InChi Key: UBVZQGOVTLIHLH-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H8N6/c14-8-11-7-10(3-6-16-11)13-17-12(18-19-13)9-1-4-15-5-2-9/h1-7H,(H,17,18,19)

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 248.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Utami SB, Mahati E, Li P, Maharani N, Ikeda N, Bahrudin U, Munemura C, Hosoyamada M, Yamamoto Y, Yoshida A, Nakayama Y, Higaki K, Nanba E, Ninomiya H, Shirayoshi Y, Ichida K, Yamamoto K, Hosoya T, Hisatome I. Apoptosis induced by an uromodulin mutant C112Y and its suppression by topiroxostat. Clin Exp Nephrol. 2014 Sep 20. [Epub ahead of print] PubMed PMID: 25239792.

2: Shimo T, Moto M, Ashizawa N, Matsumoto K, Iwanaga T, Saito K. Xanthine crystals induced by topiroxostat, a xanthine oxidoreductase inhibitor, in rats, cause transitional cell tumors. Arch Toxicol. 2014 Apr;88(4):1035-42. doi: 10.1007/s00204-014-1195-9. Epub 2014 Jan 22. PubMed PMID: 24448833.

3: Hosoya T, Ohno I, Nomura S, Hisatome I, Uchida S, Fujimori S, Yamamoto T, Hara S. Effects of topiroxostat on the serum urate levels and urinary albumin excretion in hyperuricemic stage 3 chronic kidney disease patients with or without gout. Clin Exp Nephrol. 2014 Dec;18(6):876-84. doi: 10.1007/s10157-014-0935-8. Epub 2014 Jan 22. PubMed PMID: 24448692; PubMed Central PMCID: PMC4271138.

4: Sugiyama A, Hashimoto H, Nakamura Y, Fujita T, Kumagai Y. QT/QTc study conducted in Japanese adult healthy subjects: a novel xanthine oxidase inhibitor topiroxostat was not associated with QT prolongation. J Clin Pharmacol. 2014 Apr;54(4):446-52. doi: 10.1002/jcph.226. Epub 2013 Nov 22. PubMed PMID: 24214189.