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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 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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 | |||
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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 |
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