60477-38-5
中文名稱
Pifithrin-α, p-nitro, cyclic
英文名稱
Pifithrin-α, p-nitro, cyclic
CAS
60477-38-5
分子式
C15H13N3O2S
分子量
299.35
MOL 文件
60477-38-5.mol
更新日期
2024/11/09 19:15:09
60477-38-5 結(jié)構(gòu)式
基本信息
中文別名
PIFITHRIN-Α, P-NITRO, CYCLIC化合物PIFITHRIN-Α, P-NITRO, CYCLIC
5,6,7,8-四氫-2-(4-硝基苯基)咪唑并[2,1-b]苯并噻唑
英文別名
p-Nitro-CyclicPifithrin-αp-Nitro-Cyclic Pifithrin-a
Cyclic pifithrin-α-p-nitro
p-nitro-Cyclic Pifithrin-α
Pifithrin-α, p-nitro, cyclic
Pifithrin-alpha, p-Nitro, Cyclic
p-nitro Cyclic Pifithrin-.alpha.
Pifithrin-α, p-Nitro, Cyclic - CAS 60477-38-5 - Calbiochem
Imidazo[2,1-b]benzothiazole, 5,6,7,8-tetrahydro-2-(4-nitrophenyl)-
2-(4-Nitro-phenyl)-5,6,7,8-tetrahydro-benzo[d]imidazo[2,1-b]thiazole
物理化學(xué)性質(zhì)
熔點(diǎn)233-234 °C(Solv: N,N-dimethylformamide (68-12-2); water (7732-18-5))
密度1.53±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20C
溶解度≤1mg/ml in dimethyl formamide
酸度系數(shù)(pKa)6.14±0.20(Predicted)
形態(tài)黃色固體
顏色Light yellow to yellow
常見(jiàn)問(wèn)題列表
生物活性
Pifithrin-α, p-Nitro, Cyclic (PFN-α)，是細(xì)胞通透性的 p53 抑制劑。Pifithrin-α, p-Nitro, Cyclic 對(duì)暴露于 Etoposide 的皮層神經(jīng)元的保護(hù)作用比 Pifithrin-α 強(qiáng)一個(gè)數(shù)量級(jí) (ED50=30 nM)。Pifithrin-α, p-Nitro, Cyclic 也作為 p53 轉(zhuǎn)錄后活性抑制劑。Pifithrin-α, p-Nitro, Cyclic 不阻止 p53 上的 S15 殘基磷酸化。體外研究
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.
體內(nèi)研究
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).