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p-nitro-Cyclic Pifithrin-α Sale

(Synonyms: Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α) 目录号 : GC15613

A cell-permeable form of cyclic PFT-α

p-nitro-Cyclic Pifithrin-α Chemical Structure

Cas No.:60477-38-5

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产品描述

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.

Chemical Properties

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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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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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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