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CP73850

CP73850用途

Zopolrestat(CP73850)是一种有效的口服活性醛糖还原酶(AR)抑制剂,IC50为3.1nm。Zopolrestat用于糖尿病并发症的研究[1]。

CP73850名称

[ CAS 号 ]:
110703-94-1

[ 中文名 ]:
唑泊司他

[ 英文名 ]:
CP 73850

[英文别名 ]:

CP73850生物活性

[ 描述 ]:

Zopolrestat(CP73850)是一种有效的口服活性醛糖还原酶(AR)抑制剂,IC50为3.1nm。Zopolrestat用于糖尿病并发症的研究[1]。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 醛糖还原酶

研究领域 >> 代谢疾病

[体外研究]

Zopolrestat是一种通过人和大鼠酶降低甘油醛和葡萄糖的有效抑制剂[1]。

[体内研究]

佐波尔司他(2.5 mg/kg-50 mg/kg；p、 o。；每日一次,连续5天)且未经治疗7天)可防止糖尿病大鼠肾皮质中山梨醇的积聚,并使半乳糖血症大鼠的肾血流量正常化[1]。动物模型：雄性Sprague-Dawley大鼠(通过静脉注射链脲佐菌素制造糖尿病)[1]。剂量：2.5mg/kg-50mg/kg给药：P.o。；每天一次,连续5天结果：在一项慢性试验中,其逆转大鼠坐骨神经、视网膜和晶状体中已经升高的山梨醇积累的ED50分别为1.9、17.6和18.4 mg/kg。

[参考文献]

[1]. Mylari BL, et al. Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners. J Med Chem. 1991;34(1):108-122.

CP73850物理化学性质

[ 密度 ]:
1.58g/cm3

[ 沸点 ]:
598.7ºC at 760mmHg

[ 分子式 ]:
C₁₉H₁₂F₃N₃O₃S

[ 分子量 ]:
419.37700

[ 闪点 ]:
315.9ºC

[ 精确质量 ]:
419.05500

[ PSA ]:
113.32000

[ LogP ]:
3.70040

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
3.5E-15mmHg at 25°C

[ 折射率 ]:
1.683

[ 储存条件 ]:
2-8°C，密封，干燥

CP73850MSDS

详细MSDS(安全技术说明书)

CP73850安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H413

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T+

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

CP73850文献

Inhibiting wild-type and C299S mutant AKR1B10; a homologue of aldose reductase upregulated in cancers.

Eur. J. Pharmacol. 584 , 213-221, (2008)

AKR1B10 is an aldose reductase (AR) homologue overexpressed in liver cancer and various forms of that enzyme in carcinomas catalyze the reduction of anticancer drugs, potential cytostatic drug, and dl...

Mediation of aldose reductase in lipopolysaccharide-induced inflammatory signals in mouse peritoneal macrophages.

Cytokine 36(3-4) , 115-22, (2006)

Aldose reductase (AR; AKR1B1) a member of aldo-keto reductase super family, that we had shown earlier mediates cytotoxic signals induced by high glucose, cytokines and growth factors, also mediates th...

Endotoxin causes pulmonary hypertension by upregulating smooth muscle endothelin type-B receptors: role of aldose reductase.

Shock 30(2) , 189-96, (2008)

Endothelin-1 (ET-1), a potent vasoconstrictor and mitogen, is upregulated in pulmonary tissue during endotoxemia and contributes markedly to endotoxin-induced pulmonary hypertension. It is, however, u...

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