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Topiroxostat

99.5%

Topiroxostat

質(zhì)檢下載產(chǎn)品說明書核磁下載

品牌：源葉(MedMol)

產(chǎn)品編號：S85842 一鍵復(fù)制產(chǎn)品信息

CAS號：577778-58-6

分子式：C₁₃H₈N₆

分子量：248.2428

貨號	規(guī)格	價格	上海	北京	武漢	南京
S85842-5mg	99.5%	￥280.00 S85842-5mg ￥280.00 現(xiàn)貨	1408 >10	-	-	-
S85842-10mg	99.5%	￥400.00 S85842-10mg ￥400.00 現(xiàn)貨	707 2 >10	2	-	-
S85842-50mg	99.5%	￥1200.00 S85842-50mg ￥1200.00 現(xiàn)貨	150 >10	-	-	-
S85842-100mg	99.5%	￥1520.00 S85842-100mg ￥1520.00 現(xiàn)貨	80 >10	-	-	-
S85842-250mg	99.5%	￥2800.00 S85842-250mg ￥2800.00 現(xiàn)貨	33 >10	-	-	-

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產(chǎn)品介紹

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

產(chǎn)品描述：

靶點：

IC50: 5.3 nM (XOR) Ki: 5.7 nM (XOR);P450;ROS;XanthineOxidase

體外研究：

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

體內(nèi)研究：

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. 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. Animal Model: Male Wistar/ST strain rats (7 weeks old) injected with potassium oxonate 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.

參考文獻：

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. 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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	4.028 ml	20.142 ml	40.283 ml
5 mM	0.806 ml	4.028 ml	8.057 ml
10 mM	0.403 ml	2.014 ml	4.028 ml
50 mM	0.081 ml	0.403 ml	0.806 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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