PU02

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Chemical Structure| 313984-77-9 同义名 : -
CAS号 : 313984-77-9
货号 : A698789
分子式 : C16H12N4S
纯度 : 99%+
分子量 : 292.36
MDL号 : MFCD23381174
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 The 5-hydroxytryptamine type 3 receptors (5-HT3Rs) are pentameric ligand-gated cation-selective ion channels belonging to the Cys-loop receptor superfamily. 5-HT3Rs mediate numerous important functions in serotonergic neurotransmission and as heteroreceptors in other neurotransmitter systems. PU-02 is a potent and selective antagonist of the 5-HT3Rs with IC50 values of ~1 μM and exhibits substantially lower activities at other Cys-loop receptors[1]. Increasing PU-02 concentrations (0-200 μM) led to a steady decrease in cell viability of HepG2 cells (IC50 = 49 μM). PU-02 (15 μM; 12 or 16 hr) exhibited inhibitory effects on proliferation of HepG2 cells. Moreover, typical apoptotic features, including nuclear condensation and nuclear fragmentation, were observed on HepG2 cells after 24 h of treatment with 20 μM PU-02[2].
作用机制 The naphthalene group of PU02 docks into the hydrophobic cavity formed by Ser248, Leu288, Ile290, Thr294, and Gly306 residues[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.10mL

3.42mL

1.71mL

34.20mL

6.84mL

3.42mL

参考文献

[1]Trattnig SM, et al. Discovery of a novel allosteric modulator of 5-HT3 receptors: inhibition and potentiation of Cys-loop receptor signaling through a conserved transmembrane intersubunit site. J Biol Chem. 2012 Jul 20;287(30):25241-54

[2]Yang XG, et al. 6-[(1-naphthylmethyl)sulfanyl]-9H-purine induces G2/M phase arrest and apoptosis in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2012 Nov 15;695(1-3):27-33