Pifithrin-α - CAS:63208-82-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Pifithrin-α 促销
英文名称:	Pifithrin-α
别名:	吡菲他林-α 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone hydrobromide
CAS No:	63208-82-2	分子式:	C₁₆H₁₈N₂Os^.HBr	分子量:	367.3
CAS No:	63208-82-2
分子式:	C₁₆H₁₈N₂Os^.HBr
分子量:	367.3
MDL:	MFCD00417851

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P10054 Pifithrin-α ≥97% (HPLC) (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(20 mg/mL)

产品描述：

基本信息

产品编号：P10054
产品名称：Pifithrin-α
CAS:	63208-82-2	储存条件	粉末	-20℃	四年

分子式：	C16H18N2Os.HBr		溶于液体	-80℃	六个月
分子量	367.30			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	73mg/mL (198.74mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）	5% DMSO+ 40% PEG 300+ 5%Tween80+ 50%ddH2O	3.65mg/ml
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.7226mL	13.6129mL	27.2257mL
5mM	0.5445mL	2.7226mL	5.4451mL
10mM	0.2723mL	1.3613mL	2.7226mL
50mM	0.0545mL	0.2723mL	0.5445mL

生物活性

产品描述	一种p53抑制剂，抑制p53依赖性的p53应答基因转录。
靶点/IC50	p53 AhR
体外研究	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. 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.
体内研究	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 (2.2mg/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).

推荐实验方法(仅供参考)

激酶实验：

The ligand binding competition assays are performed. Cytosolic cell extracts from Hepa-1 cells are generated by the resuspension of the cell pellets in HEDG buffer [25mM Hepes, 1mM EDTA,1mM dithiothreitol, and 10% (v/v) glycerol, pH 7.5] containing 0.4mM leupeptin, 4mg/mL aprotinin,and 0.3mM phenylmethylsulfonyl fluoride, homogenization, and centrifugation at 100,000 g for 45 min. Aliquots of the supernatant (120μg) are incubated at room temperature for 2h with the indicated concentrations of Pifithrin-α in the presence of 3nM [3H]TCDD in HEDG buffer. After incubation on ice with hydroxyapatite for 30 min, HEDG buffer with 0.5% Tween 80 is added. The samples are centrifuged, washed twice,resuspended in 0.2mL of scintillation fluid, and subjected to scintillation counting. Nonspecific binding is determined using a 150-fold molar excess of TCDF and subtracted from the total binding to obtain the specific binding. The specific binding is reported relative to [3H]TCDD alone.

细胞实验:

The human hepatoma cell lines HepG2 (p53++) are cultured in RMPI 1640 medium with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37℃ in an atmosphere containing 5% CO2.Cells are exposed to GOX (0-5 0U) for 0-8 hours with or without Pifithrin-α (20μM/L),Pifithrin-μ (5μM/L), CsA (10μM/L), Sanglifehrin A (20μM/L) and NAC (5mM/L) for 1hour,respectively.After treatment, cells are collected and processed for further experiments.

动物实验:

Mice

The Foxe3-null (Foxe3-/-) mice are used. To investigate the role of p53 in Foxe3-related apoptosis,Pifithrin-α is administered by i.p. injection at a dosage of 2.2mg/kg, then dissolved in PBS 1 hour before TAC and then every 48 hours. Animals are euthanized 2 weeks after the surgery, and the ascending aortic tissues are harvested for either RNA, total protein,histomorphometric analysis, or TUNEL assay.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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