p-nitro-Cyclic Pifithrin-α (Synonyms: Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α) |
Catalog No.GC15613
One-Click Copy Product Info
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pifitrina p-nitro-cÍclica-α (PFN-α) es un inhibidor de p53 permeable a las células y de forma activa.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 60477-38-5
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Sinónimos | Cyclic pifithrin-α-p-nitro,p-nitro-Cyclic PFT-α | ||
| Chemical Name | 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-] | ||
| Formula | C15H13N3O2S | M.Wt | 299.3 |
| Solubility | ≤1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3411 mL | 16.7056 mL | 33.4113 mL |
| 5 mM | 668.2 μL | 3.3411 mL | 6.6823 mL |
| 10 mM | 334.1 μL | 1.6706 mL | 3.3411 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)