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Pifithrin-α hydrobromide
  • 英文名称:Pifithrin-α hydrobromide
  • 品牌:Chemstan
  • 产地:武汉
  • 货号:CS-15484
  • cas:63208-82-2
  • 价格: ¥698/支
  • 发布日期: 2021-03-10
  • 更新日期: 2025-09-29
产品详请
产地 武汉
品牌 Chemstan
货号 CS-15484
用途 科研
英文名称 Pifithrin-α hydrobromide
包装规格 5 mg
纯度 100%%
CAS编号 63208-82-2
别名 PFTα hydrobromide,?Pifithrin hydrobromide,?Pifithrin-α hydrobromide,?Pifithrin-α (PFTα) HBr,?PFTα
分子式 C16H18N2OS稨Br?
是否进口
Description

Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.

IC50 & Target

p53[1]
AhR[2]

In Vitro

Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect. Notably, Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates[1] . Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and. Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex, activate reporter activity, and up-regulate the classic AhR target gene CYP1A1[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

When the experiment is performed with Pifthirin-α (PFT-α) hydrobromide, a pharmacological p53 inhibitor, the percentage of annexin V-positive Foxe3-/- SMCs decreases to WT levels. Pifithrin-α (2.2 mg/kg, i.p.) significantly reduces the incidence of aortic rupture and intramural hematomas in Foxe3-/- mice that underwent transverse aortic constriction (TAC) (50% to 17%, P<0.05). After Pifthirin-α treatment, the mean diameter of the ascending aorta and the percentage of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals (P<0.05)[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

367.30

Formula

C??H??BrN?OS

CAS No.

63208-82-2

SMILES

N=C1SC2=C(CCCC2)N1CC(C3=CC=C(C)C=C3)=O.[H]Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (136.13 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
ConcentrationSolventMass 1 mg 5 mg 10 mg
1 mM 2.7226 mL 13.6129 mL 27.2257 mL
5 mM 0.5445 mL 2.7226 mL 5.4451 mL
10 mM 0.2723 mL 1.3613 mL 2.7226 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式 选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300     5% Tween-80     45% saline

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD  in saline)

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.81 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References
  • [1]. Yu W, et al. Cyclosporine A Suppressed Glucose Oxidase Induced P53 Mitochondrial Translocation and Hepatic Cell Apoptosis through Blocking Mitochondrial Permeability Transition. Int J Biol Sci. 2016 Jan 1;12(2):198-209.

    [2]. Hoagland MS, et al. The p53 Inhibitor Pifithrin-α Is a Potent Agonist of the Aryl Hydrocarbon Receptor. J Pharmacol Exp Ther. 2005 Aug;314(2):603-10.

    [3]. Kuang SQ, et al. FOXE3 mutations predispose to thoracic aortic aneurysms and dissections. J Clin Invest. 2016 Mar 1;126(3):948-61.

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