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CAS No.: 24386-93-4

5-碘代杀结核菌素 Catalog No. CSN13857

Synonyms: NSC 113939;5-ITu;Itu

5-Iodotubercidin is a potent inhibitor (IC50 = 26 nM). It also inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

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实验方案

技术信息

生物活性

描述Adenosine kinase plays a fundamental role in fulfilling essential functions as a homeostatic and metabolic regulator by converting the adenosine into 5'-adenosine-monophosphate. 5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 value of 26 nM, which can markedly inhibit adenosine uptake into brain slices with IC50 of 22 nM. Five groups of Mongolian gerbils were set into non-ischemic group and ischemic group. In non-ischemic group, the locomotor activities were significantly declined when treated the gerbils with 1 and 5 mg/kg of 5-Iodotubercidin maintained in the 30°C enclosure for 5 hrs, the value was significantly lower than that in the saline-injected control animals. While in ischemic group, it was comparable to that of the saline controls when treated with 1 mg/kg of 5-Iodotubercidin. Furthermore, locomotor activity in ischemic group was significantly bigger than that in non-ischemic group at 5 hrs enclosure. After five days' treatment, the CAI region of the hippocampus was damaged and found in all animals, the damage score was 2.72 in 5-Iodotubercidin-treated animals, which was similarly as 2.69 in the control gerbils. The body temperature of gerbils treated with 5 mg/kg of 5-Iodotubercidin for 1 hr was small but non-significant decreased from 36.9 to 35℃. In DDT1 MF-2 cells, adenosine accumulation could be inhibited by 5-iodotubercidin as well as 120% decreasing of the adenosine affinity. Besides, 5-iodotubercidin also inhibited uridine uptake with IC50 value of 7mM, suggesting an enhancement of adenosine's receptor-mediated effects.
作用机制5-iodotubercidin increases the release of adenosine from hypoxic/hypoglycemic hippocampal slices^[2].
动物研究
剂量
Mice: 0.625 mg/kg - 2.5 mg/kg^[4] (i.p.) Mongolian gerbil: 1 mg/kg - 5 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.625 mg/kg - 2.5 mg/kg^[4] (i.p.) Mongolian gerbil: 1 mg/kg - 5 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Boison D. Adenosine kinase: exploitation for therapeutic gain. Pharmacol Rev. 2013;65(3):906-43.
[2] Phillis JW, Smith-Barbour M. The adenosine kinase inhibitor, 5-iodotubercidin, is not protective against cerebral ischemic injury in the gerbil. Life Sci. 1993;53(6):497-502.
[3] Parkinson FE, Geiger JD. Effects of iodotubercidin on adenosine kinase activity and nucleoside transport in DDT1 MF-2 smooth muscle cells. J Pharmacol Exp Ther. 1996;277(3):1397-401.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5500 mL
- 12.7502 mL
- 25.5004 mL
- 5 mM
- 0.5100 mL
- 2.5500 mL
- 5.1001 mL
- 10 mM
- 0.2550 mL
- 1.2750 mL
- 2.5500 mL

技术信息

CAS号

24386-93-4

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H13IN4O4

运输

蓝冰

分子量

392.15

别名

NSC 113939;5-ITu;Itu;5-碘结核菌素

溶解度

DMSO	77.0 mg/mL (196.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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