Topiroxostat

Topiroxostat Properties

Boiling point	594.7±60.0 °C(Predicted)
Density	1.45±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 23.5 mg/mL (94.67 mM; Need ultrasonic and warming)
form	Powder
pka	7.47±0.10(Predicted)
color	White to off-white
InChI	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)
InChIKey	UBVZQGOVTLIHLH-UHFFFAOYSA-N
SMILES	C1(C#N)=NC=CC(C2NN=C(C3C=CN=CC=3)N=2)=C1
FDA UNII	0J877412JV
UNSPSC Code	51111800
NACRES	NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H315-H319-H335

Precautionary statements

P261-P305+P351+P338

WGK Germany

WGK 3

Storage Class

11 - Combustible Solids

NFPA 704

	0
2		0

Topiroxostat price More Price(40)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	21267	Topiroxostat ≥98%	577778-58-6	5mg	$75	2026-04-30	Buy
Cayman Chemical	21267	Topiroxostat ≥98%	577778-58-6	10mg	$134	2026-04-30	Buy
Cayman Chemical	21267	Topiroxostat ≥98%	577778-58-6	50mg	$589	2026-04-30	Buy
Cayman Chemical	21267	Topiroxostat ≥98%	577778-58-6	100mg	$882	2026-04-30	Buy
ChemScene	CS-2033	Topiroxostat ≥99%	577778-58-6	1g	$34	2026-06-04	Buy

Product number	Packaging	Price	Buy
21267	5mg	$75	Buy
21267	10mg	$134	Buy
21267	50mg	$589	Buy
21267	100mg	$882	Buy
CS-2033	1g	$34	Buy

Topiroxostat Chemical Properties, Uses, Production

Description

Topiroxostat is an orally-administered, non-purine, selective xanthine oxidase (XO) inhibitor developed for the treatment of hyperuricemia specifically for patients with gout in Japan. The drug was discovered and developed by Fuji Yakuhin. In contrast to conventional XO inhibitors such as febuxostat, topiroxostat interacts with key amino acid residues of the solvent channel.

Chemical Properties

Topiroxostat is soluble in organic solvents such as DMSO and dimethyl formamide (DMF). The solubility of topiroxostat in these solvents is approximately 10 and 20 mg/ml, respectively.

Uses

Topiroxostat is a selective xanthine oxidase inhibitor developed for treatment and management of hyperuricemia and gout. Xanthine oxidase, or xanthine oxidoreductase (XOR), regulates purine metabolism, and inhibition of the enzyme results in efficacious reduction of serum urate levels. Approved for therapeutic use in Japan since 2013, topiroxostat is marketed under the name Topiloric and Uriadec and is orally administered twice daily.

Biological Activity

Topiroxostat is an inhibitor of xanthine oxidoreductase (IC50 = 5.3 nM), an enzyme that converts xanthine to urate. Formulations containing topiroxostat are effective in vivo, lowering urate levels in the serum of patients with hyperuricemia. In rats, but not primates, topiroxostat treatment results in the formation of xanthine crystals, resulting in nephritis. Topiroxostat also inhibits ATP-binding cassette transporter G2 (ABCG2; IC50 = 0.18 μM), a high-capacity urate transporter that functions in both renal and extrarenal urate secretion.

Pharmacology

Topiroxostat is a novel inhibitor of xanthine oxidase, and is postulated to exert a renoprotective effect. Puromycin aminonucleoside nephrosis (PAN) is a rat model of minimal change nephrotic syndrome. In this study, we examined whether topiroxostat ameliorates the kidney injury in PAN rats that was induced by a single intraperitoneal injection of PA (100mg/kg body weight). Rats were divided into four groups: control rats, PAN rats, control rats treated with topiroxostat (1.0mg/kg/day), and PAN rats treated with topiroxostat. Topiroxostat significantly reduced the amount of uric acid in the kidney cortex, while serum UA concentration remained unaffected by this treatment. Urinary protein excretion decreased significantly on day 10 in PAN rats upon topiroxostat treatment. Podocyte injury in PAN rats, as indicated by the reduction in WT‐1‐positive cell numbers and podocin immunoreactivity and foot process effacement, was partially yet significantly alleviated with topiroxostat treatment. In the kidney cortex, the increase in oxidative stress markers such as nitrotyrosine and 8‐hydroxy‐2‐deoxyguanosine (8‐OHdG) and the enhanced expressions of xanthine oxidase and NADPH oxidase 4 (NOX4) in PAN rats were significantly ameliorated by topiroxostat. Using cultured podocytes NOX4 expression was upregulated by adding 12mg/dL UA into the culture medium. These results suggest that topiroxostat ameliorates proteinuria and kidney injury in PAN rats by lowering oxidative stress and tissue UA concentration. The renoprotective effects of topiroxostat could be attributed to its potential to inhibit xanthine oxidase and NOX4 in concert with suppression of intracellular UA production. Abstract : Topiroxostat ameliorates proteinuria and renal injury independently of serum UA level in PAN‐induced nephrotic rats. Topiroxostat exerts a renoprotective effect owing to its antioxidant effects and property to lower UA levels in the kidney cortex.

Clinical Use

Topiroxostat, a novel XO inhibitor, ameliorated proteinuria in association with podocyte injury markers such as decrease in WT-1 and podocin expressions and foot process effacement on electron microscope.

Synthesis

The synthesis commenced with the reaction of two commercially available components, nitrile oxide 177 and isonicotinohydrazide (178). Condensation of these two subunits in the presence of sodium methoxide followed by acidic quench gave rise to 1,2,4-triazole 179 in 89% yield. Next, utilization of the N-oxide for installation of the nitrile functionality was required to furnish the drug, but it is interesting to note that this step has been the subject of study by Yamamoto and co-workers at Tohoku University in Japan. Although the process preparation describes the formation of the drug using sodium cyanide and dimethylcarbamoyl chloride followed by isolation through a salt formation/ freebasing process to deliver topiroxostat (XXIII) in 66% yield, Yamamoto has described this same sequence using zinc cyanide and tosylate salt formation (freebasing of the drug was not attempted).

Synthesis_577778-58-6

Carcinogenicity

Carcinogenicity was evaluated in 2-year oral dose studies in mice and rats. Tumors developed in both animal species (mice, mammary adenocarcinoma; rats, transitional cell papilloma/papillary carcinoma in the kidney and bladder, transitional cell carcinoma in the ureter, renal cell carcinoma and angiosarcoma in the kidney, follicular cell adenoma in the thyroid), secondary to chronic renal impairment probably due to xanthine crystal deposition. Comparison of the exposure (AUC)7 to unchanged topiroxostat at the non-carcinogenic doses in mice and rats and at the maximum recommended clinical dose yielded a safety margin of <1-fold in both animal species. However, the applicant has considered that the observed tumorigenesis is not relevant to humans because xanthine crystal deposition is pronounced in rodents in comparison with other animal species including humans.

References

[1] Patent: CN107573330, 2018, A. Location in patent: Paragraph 0039; 0040-0042; 0065; 0067; 0069; 0071; 0073-0076
[2] Patent: CN105566301, 2016, A. Location in patent: Paragraph 0064; 0065
[3] Patent: CN104151297, 2016, B. Location in patent: Paragraph 0049; 0050

Topiroxostat Preparation Products And Raw materials

Raw materials

4-Cyanopyridine Topiroxostat Impurity 56 4-Pyridinecarboxylicacid,2-cyano-,hydrazide(9CI)

Preparation Products

Topiroxostat Suppliers

Global Suppliers ( 396)

Supplier	Tel	Email	Country	ProdList	Advantage
Shandong Loncom Pharmaceutical Co., Ltd.	0531-88116830 18047572271	sales@bestcomm.cn	China	46	58
Jinan LuoHe PharmaTech Co., Ltd.	86-0531-68658065 15726150375	1071018499@qq.com	China	525	58
HuBei VernalBay Biopharmaceutical Co., Ltd.	17371337933 17371337933	3495784513@qq.com	China	20	58
Shanghai Boyle Chemical Co., Ltd.		sales@boylechem.com	China	2915	55
Chembest Research Laboratories Limited	021-20908456	sales@BioChemBest.com	China	5996	61
Beijing HwrkChemical Technology Co., Ltd	89508211 18501085097	sales.bj@hwrkchemical.com	China	9409	55
Energy Chemical	400-0056266	sales8178@energy-chemical.com	China	44850	61
Jia Xing Isenchem Co.,Ltd	0573-85285100 18627885956	isenchem@163.com	China	9389	66
Adamas Reagent, Ltd.	400-6009262 15618770481	yhx@titansci.com	China	14098	59
Shanghai Hanhong Scientific Co.,Ltd.	021-54306202 13764082696	info@hanhongsci.com	China	42917	64

Supplier	Advantage
Shandong Loncom Pharmaceutical Co., Ltd.	58
Jinan LuoHe PharmaTech Co., Ltd.	58
HuBei VernalBay Biopharmaceutical Co., Ltd.	58
Shanghai Boyle Chemical Co., Ltd.	55
Chembest Research Laboratories Limited	61
Beijing HwrkChemical Technology Co., Ltd	55
Energy Chemical	61
Jia Xing Isenchem Co.,Ltd	66
Adamas Reagent, Ltd.	59
Shanghai Hanhong Scientific Co.,Ltd.	64

View Latest Price from Topiroxostat manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2026-09-24	Topiroxostat 577778-58-6		10g	99%min	100kg	WUHAN FORTUNA CHEMICAL CO., LTD
2026-08-25	Topiroxostat 577778-58-6		1kg	0.99	1000kg	Shaanxi Xianhe Biotech Co., Ltd
2026-08-21	Topiroxostat 577778-58-6	$95.00-100.00	1kg	99.99%	100Tons	Hebei Dangtong Import and export Co LTD

Topiroxostat
577778-58-6
$0.00
99%min
WUHAN FORTUNA CHEMICAL CO., LTD

Topiroxostat
577778-58-6
$0.00
0.99
Shaanxi Xianhe Biotech Co., Ltd

Topiroxostat
577778-58-6
$95.00-100.00
99.99%
Hebei Dangtong Import and export Co LTD

Topiroxostat Spectrum

Topiroxostat(577778-58-6)¹HNMR

577778-58-6 (Topiroxostat) Related Search:

Methylisonicotinate-N-oxide 4-Pyridinecarboximidic acid, hydrazide 2-Carbamoyl-isonicotinic acid ethyl ester 2-Cyano-4-pyridine carboxylic acid methyl ester 2-Cyano-4-pyridine carboxylic acid

Topiroxostat Impurity 2 2-Cyano-N'-(imino(pyridin-4-yl)methyl)isonicotinohydrazide Topiroxostat Impurity 23 Pyridine, 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl]-, 1-oxide Topiroxostat Impurity 5

Methyl nicotinate Topiroxostat Impurity 6 4-Pyridinecarboxylicacid,2-cyano-,hydrazide(9CI) Topiroxostat Impurity 15 VILAZODONE

tadalafi Pidotimod Dapoxetine

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Topiroxostat Topiroxostat,FYX-051 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole Topiroxostat 5-(2-Cyano-4-pyridyl)-3-(4-pyridyl)-1,2,4-triazole 4-[5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile 2-Pyridinecarbonitrile, 4-[5-(4-pyridinyl)-1H-1,2,4-triazol-3-yl]- Topiroxostat impurty Topiroxostat C13H8N6 high quality Cas number：577778-58-6 4-(3-(Pyridin-4-yl)-1H-1,2,4-triazol-5-yl)picolinonitrile [14C]-Topiroxostat 3-(3-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole Factory supply Topiroxostat Cas 577778-58-6 with high quality and best price FYX-051; FYX051; FYX 051; TOPIROXOSTAT. TRADE NAMES TOPILORIC; URIADEC. Topiroxostat. trade names Topiloric Uriadec. CS-1334 4-(5-pyridin-4-yl-1H-1,2,4-triazol-3-yl)pyridine-2-carbonitrile 4-[5-(4-Pyridyl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile Toby Starr 4-(3-(Pyridin-4-yL inonitriL 2-Pyridinecarbonitrile, 4-[3-(4-pyridinyl)-1H-1,2,4-triazol-5-yl]- Topiroxosta Topicast impurity N-desmethyl N-Nitroso Topotecan-D3 Topiroxostat, 10 mM in DMSO Topiester D4-Topiroxostat 4-(5-(pyridin-4-yl)-1h-1,2,4-triazol-3-yl)picolinonitrile FYX 051 577778-58-6 577779-58-6 147366-18-1 577730-39-1 Inhibitors API 577778-58-6