Fidarestat (Synonyms: SNK 860)
目录号: PL01512 纯度: ≥99%
CAS No. :136087-85-9
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中文名称
Fidarestat
中文别名
非达司他;(2S,4S)-2-氨基甲酰-6-氟-螺[苯并二氢吡喃-4,4'-咪唑啉]-2',5'-酮;(2S,4S)-6-氟-2',5'-二氧代-螺[色满-4,4'-咪唑啉]-2-甲酰胺;菲达瑞斯
英文名称
Fidarestat
英文别名
(2S,4S)-6-Fluoro-2',5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide;(2S,4S)-2-Aminoformyl-6-fluoro-spiro[chroman-4,4'-imidazolidine]-2',5'-dione;(2S,4S)-6-Fluoro-2',5'-dioxo-2,3-dihydrospiro[chromene-4,4'-imidazolidine]-2-carboxamide;Fidarestat;(2S,4S)-2,3-Dihydro-6-fluoro-2',5'-dioxospiro[4H-1-benzopyran-4,4'-imidazolidine]-2-carboxamide;(2S,4S)-6-FLUORO-2'',5''-DIOXOSPIRO(3,4-DIHYDRO-2H-1-BENZOPYRAN-4,4''-IMIDAZOLIDINE)-2-CARBOXAMIDE;Sk 860;Spiro(4H-1-benzopyran-4,4'-imidazolidine)-2-carboxamide,6-fluoro-2,3-dihydro-2',5'-dioxo-,(2S-cis)
Cas No.
136087-85-9
分子式
C12H10N3O4F
分子量
279.22
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Fidarestat (SNK 860) 是一种醛糖还原酶 (aldose reductase) 抑制剂,对 aldose reductase,AKR1B10 和 V301L AKR1B10 的 IC50 值分别为 26 nM,33 μM 和 1.8 μM。Fidarestat (SNK 860) 具有研究糖尿病的潜力。
生物活性
Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC 50 s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.
性状
Solid
IC50 & Target[1][2]
IC50: 26 nM (Aldose reductase), 33 μM (AKR1B10), 1.8 μM (V301L AKR1B10)
体外研究(In Vitro)
Fidarestat is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Fidarestat (SNK-860; 1 or 4 mg/kg. p.o., daily for 4 weeks) reduces the concentrations of sorbitol and fructose in diabetic rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Ruiz FX, et al. X-ray structure of the V301L aldo-keto reductase 1B10 complexed with NADP(+) and the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity. Chem Biol Interact. 2013 Feb 25;202(1-3):178-85.
[2]. Hotta N, et al. Effect of an aldose reductase inhibitor, SNK-860, on deficits in the electroretinogram of diabetic rats. Exp Physiol. 1995 Nov;80(6):981-9.
溶解度数据
In Vitro: DMSO : 250 mg/mL (895.35 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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