HY-126124 AP39 | MedChemExpress (MCE)

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AP39

CAS No. : 1429061-80-2

MCE 国际站：AP39

产品活性：AP39 是三苯基膦衍生的茴香脑二硫代硫酮和靶向线粒体的硫化氢 (H₂S) 供体。AP39 在氧化应激条件下发挥细胞保护作用并保持线粒体 DNA 完整性。AP39 增加细胞内 H₂S 水平。AP39 可以防止小鼠模型中心肌再灌注损伤，有潜力用于阿尔茨海默氏病的研究。

研究领域：Others

作用靶点：Others

In Vitro: AP39 (25,100 nM; for 24 h) results in increase in cell viability in APP/PS1 neurons and has no effect on cell viability in WT neurons.
AP39 (100 nM) increases the levels of OPA1 and Mfn1 but not Mfn2. Moreover, AP39 decreases the levels of Fis1 but not Drp1.
AP39 (25-250 nM; 2 h) induces a concentration-dependent increase in H₂S generation and in the fluorescence of the H₂S-detecting dye AzMC.
AP39 (100 nM) significantly increases the basal respiratory rate and the OCR-linked maximal respiratory capacity of the APP/PS1 neurons. AP39 significantly increases the ATP production in WT and APP/PS1 neurons. AP39 significantly protects against mtDNA damage in APP/PS1 neurons by partially restoring mtDNA integrity.
AP39 consists of a mitochondria-targeting motif, triphenylphosphonium (TPP⁺), coupled to a H₂S-donating moiety (dithiolethione) by an aliphatic linker.AP39 (100 nM) reduces intracellular oxidative stress and in the meantime it consequently sustaines the cell viability, mitochondrial respiration and mitochondrial DNA integrity. These effects tend to be stimulatory at lower concentrations (30 and 100 nM), but tend to diminish or convert into inhibitory effects at a higher concentration (300 nM).

In Vivo: AP39 (100 nM/kg/day; ip; for 6 weeks) ameliorates the learning and memory deficits of APP/PS1 mice. AP39 (25-250 nM/kg/day; ip; for 6 weeks) induces a dose-dependent increase in H₂S generation in the cortex and hippocampus of WT and APP/PS1 mice.
AP39 (0.01, 0.1, 1 μmol/kg; iv; bolus 10 min before reperfusion) dose‐dependently reduces infarct size anaesthetized by thiobutabarbital (200 mg/kg, i.p) in male Sprague Dawley rats, 300-350 g (9-11 weeks).

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