Pifithrin-α, p-Nitro, Cyclic|60477-38-5|(PFN-α)-陌孚医药/Medlife

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Pifithrin-α, p-Nitro, Cyclic (Synonyms: PFN-α)

目录号: PL07031 纯度: ≥98.0%

CAS No. :60477-38-5

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中文名称	Pifithrin-α, p-Nitro, Cyclic
英文名称	Pifithrin-α, p-Nitro, Cyclic
英文别名	Pifithrin-alpha, p-Nitro, Cyclic;p-nitro-Cyclic Pifithrin-;A;2-(4-nitrophenyl)-5,6,7,8-tetrahydroimidazo[2,1-b][1,3]benzothiazole;p-Nitro-CyclicPifithrin-alpha;2-(4-Nitrophenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole;4-(4-nitrophenyl)-7-thia-2,5-diazatricyclo[6.4.0.0^{2,6}]dodeca-1(8),3,5-triene;Pifithrin-α, p-Nitro, Cyclic
Cas No.	60477-38-5
分子式	C₁₅H₁₃N₃O₂S
分子量	299.35
包装储存	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情	Pifithrin-α, p-Nitro, Cyclic (PFN-α)，是细胞通透性的 p53 抑制剂。Pifithrin-α, p-Nitro, Cyclic 对暴露于 Etoposide 的皮层神经元的保护作用比 Pifithrin-α 强一个数量级 (ED₅₀=30 nM)。Pifithrin-α, p-Nitro, Cyclic 也作为 p53 转录后活性抑制剂。Pifithrin-α, p-Nitro, Cyclic 不阻止 p53 上的 S15 残基磷酸化。
生物活性	Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED 50 =30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
性状	Solid
体外研究(In Vitro)	Pifithrin-α, p-Nitro, Cyclic (PFN-α) efficiently blocks p53-triggered cell death and p21/WAF1 expression in cortical neurons exposed to etoposide at concentrations one order magnitude lower than that in PFT-α. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Intraocular injection of pifithrin-α slightly increases survival of retinal ganglion cell (RGC) at the concentration of 6 μM but not at 0.06 μM. Pifithrin-α, p-Nitro, Cyclic (PFN-α) is not effective in vivo, even at 6 μM. Pifithrin-α, p-Nitro, Cyclic shows the half-life (t 1/2 ) of 6 hours (when incubated in biological conditions). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献	[1]. Pietrancosta N, et al. Imino-tetrahydro-benzothiazole derivatives as p53 inhibitors: discovery of a highly potent in vivo inhibitor and its action mechanism. J Med Chem. 2006 Jun 15;49(12):3645-52. [2]. Dinca EB, et al. p53 Small-molecule inhibitor enhances temozolomide cytotoxic activity against intracranial glioblastoma xenografts. Cancer Res. 2008 Dec 15;68(24):10034-9.

溶解度数据	In Vitro: DMF : 12.5 mg/mL (41.76 mM; Need ultrasonic)DMSO : 5 mg/mL (16.70 mM; Need ultrasonic)配制储备液

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