AP39 - CAS:1429061-80-2

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AP39

目录号 : KM3108 CAS No. : 1429061-80-2 纯度 : 95%

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。

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生物活性

AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H₂S) donor. AP39 increases intracellular H₂S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research.

体外研究

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).

体内研究

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).

Animal Model:	12-month-old WT or APP/PS1 mice
Dosage:	100 nM/kg
Administration:	IP; daily; for 6 weeks
Result:	Reversed the spatial learning and memory deficits of the aged AD model mice. Alleviated brain atrophy and ventricle asymmetryand inhibited Aβ plaque deposition in the brains in AD model mice.

分子式

C₃₇H₃₈BrO₂PS₃

分子量

721.77

CAS号

1429061-80-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (138.55 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3855 mL	6.9274 mL	13.8548 mL
5 mM	0.2771 mL	1.3855 mL	2.7710 mL
10 mM	0.1385 mL	0.6927 mL	1.3855 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (1.15 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (1.15 mM); Clear solution

此方案可获得 ≥ 0.83 mg/mL (1.15 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 8.3 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

科研文献

•Antioxid Redox Signal. 2021 Aug 19.

纯度： 95%

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