|(S)-(4-硝基苯甲基)-6-硫肌苷|CsnPharm

CAS No.: 38048-32-7

S-(4-Nitrobenzyl)-6-thioinosine/S-(4-硝基苄基)-6-硫肌苷 Catalog No. CSN19697

Synonyms: NBMPR;NBTI;S-(4-Nitrobenzyl)-6-thioinosine

Nitrobenzylthioinosine is an inhibitor of Equilibrative Nucleoside Transporter 1 (ENT1).

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技术信息

生物活性

描述Nitrobenzylthioinosine (NBTI, NBMPR), a specific inhibitor of type 1 equilibrative nucleoside transporter, could regulate the extracellular adenosine concentration and have protective roles in seizures. In vivo, compared to control group, the expression of adenosine A1 receptor protein was increased at 24 h and 72 h after seizure, didn't change at 0 min and 1 w, and decreased at 2 w. In vitro, NBTI decreased the eEPSCs amplitude of pyramidal neurons in hippocampus CA1 region. It also inhibits eEPSCs amplitude on the basis of lower concentration adenosine (50µM), and adenosine A1 receptor inhibitor DPCPX partially reversed this effect^[1]. The NBMPR content of plasma from mice injected with NBMPR-P was maximal at about 20 min after injection and declined to < 0.2% of the peak value by 10 h. Erythrocyte-associated NBMPR was also maximal at 20 min, and declined to 11% of the peak value by 10 h after injection. Time courses for the disappearance of NBMPR from plasma and erythrocytes were monoexponential and yielded half-life values of 0.39 h and 0.68 h, respectively, an apparent volume of distribution of 0.61 l/kg, and a clearance of 1.1 l/h per kg^[2]. NBMPR can protect CA1 pyramidal neurons from ischemic death without statistically significant effects on adenosine levels or adenosine receptor-mediated inhibition of the proinflammatory cytokine TNF-alpha^[3]. NBMPR protected mice against potentially lethal treatment regimens with nebularine, tubercidin or toyocamycin; protection resulted when NBMPR was administered i.p. in advance of or simultaneously with nebularine, but not when NBMPR followed nebularine by 1 hr. Both NBMPR and its 5'-monophosphate protected mice against nebularine lethality when administered s.c^[4].
参考文献

[1] Hao Huang,et al. Nitrobenzylthioinosine mimics adenosine to attenuate the epileptiform discharge of hippocampal neurons from epileptic rats. Oncotarget. 2017 May 30;8(22):35573-35582.
[2] W P Gati , A R Paterson. Measurement of nitrobenzylthioinosine in plasma and erythrocytes: a pharmacokinetic study in mice. Cancer Chemother Pharmacol. 1997;40(4):342-6.
[3] F E Parkinson,et al. Effects of nitrobenzylthioinosine on neuronal injury, adenosine levels, and adenosine receptor activity in rat forebrain ischemia. J Neurochem. 2000 Aug;75(2):795-802.
[4] A R Paterson,et al. Protection of mice against lethal dosages of nebularine by nitrobenzylthioinosine, an inhibitor of nucleoside transport. Cancer Res. 1979 Sep;39(9):3607-11.

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
- 2.3843 mL
- 11.9215 mL
- 23.8429 mL
- 5 mM
- 0.4769 mL
- 2.3843 mL
- 4.7686 mL
- 10 mM
- 0.2384 mL
- 1.1921 mL
- 2.3843 mL

技术信息

CAS号	38048-32-7	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C17H17N5O6S	运输	蓝冰
分子量	419.41	别名	NBMPR;NBTI;S-(4-Nitrobenzyl)-6-thioinosine;NSC-296962;S-4-nitrophenylmethyl-6-thioinosine

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S-(4-Nitrobenzyl)-6-thioinosine/S-(4-硝基苄基)-6-硫肌苷 Catalog No. CSN19697

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