p-nitro-Cyclic Pifithrin-α
(Synonyms: Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α) 目录号 : GC15613
A cell-permeable form of cyclic PFT-α
Cas No.:60477-38-5
Sample solution is provided at 25 µL, 10mM.
p-nitro-Cyclic Pifithrin-α is an inactivator of p53.
The activation of the tumor suppressor gene p53 plays a key role in regulating the in-vitro death of neurons, following apoptotic stimuli molecules including glutamate and DNA-damaging agents. Thus, p53 inhibitors may prove effective in suppressing the degenerative processes in neurodegenerative disorders.
In vitro: Pifithrin-α (PFT-α) was identified as an inactivator of p53 blocking p53-dependent transcriptional activation and apoptosis. Cyclic PFT-α was a stable analog of PFT-α. p-nitro-Cyclic PFT-α, a cell-permeable form of cyclic PFT-α, was found to be one order of magnitude more active than PFT-α in protecting cortical neurons exposed to etoposide. p-nitro-Cyclic PFT-α acted in a p53-dependently but did not block phosphorylation of p53 on Ser15 in response to etoposide treatment, although it prevented p53 posttranscriptional activity [1].
In vivo: In a previou study, C57BL/6 mice were fed a high-fat (HFD) or control diet for 8 weeks; PFT was administered three times per week. Results showed that PFT administration could suppress HFD-induced weight gain, steatosis, oxidative stress, ALT elevation, and apoptosis. PFT treatment also able to blunt the HFD-induced upregulation of miRNA34a and increase SIRT1 expression. In the livers of HFD-fed, PFT-treated mice, activation of the SIRT1/PGC1α/PPARα axis increased the expression of malonyl-CoA decarboxylase [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] . Pietrancosta, N.,Moumen, A.,Dono, R., et al. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: Discovery of a highly potent in vivo inhibitor and its action mechanism. Journal of Medicinal Chemistry 49(12), 3645-3652 (2006).
[2] Derdak Z, Villegas KA, Harb R, Wu AM, Sousa A, Wands JR. Inhibition of p53 attenuates steatosis and liver injury in a mouse model of non-alcoholic fatty liver disease. J Hepatol. 2013 Apr;58(4):785-91.
Cas No. | 60477-38-5 | SDF | |
别名 | Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α | ||
化学名 | 5,6,7,8-tetrahydro-2-(4-nitrophenyl)-imidazo[2,1-b]benzothiazole | ||
Canonical SMILES | O=[N+](C(C=C1)=CC=C1C2=CN(C(S3)=N2)C4=C3CCCC4)[O-] | ||
分子式 | C15H13N3O2S | 分子量 | 299.3 |
溶解度 | ≤1mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.3411 mL | 16.7056 mL | 33.4113 mL |
5 mM | 0.6682 mL | 3.3411 mL | 6.6823 mL |
10 mM | 0.3341 mL | 1.6706 mL | 3.3411 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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