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α-Lipoic Acid/α-硫辛酸 {[allProObj[0].p_purity_real_show]}

货号:A196877 同义名: DL-硫辛酸 / Thioctic acid; DL-α-Lipoic acid

α-Lipoic Acid是一种天然的类维生素抗氧化剂。

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α-Lipoic Acid/α-硫辛酸 化学结构 CAS号:1077-28-7
α-Lipoic Acid/α-硫辛酸 化学结构
CAS号:1077-28-7
α-Lipoic Acid/α-硫辛酸 3D分子结构
CAS号:1077-28-7
α-Lipoic Acid/α-硫辛酸 化学结构 CAS号:1077-28-7
α-Lipoic Acid/α-硫辛酸 3D分子结构 CAS号:1077-28-7
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

α-Lipoic Acid/α-硫辛酸 生物活性

描述 α-Lipoic Acid, a naturally occurring substance, has many biological activities[1]. In vitro studies, α-lipoic acid could increase the level of PON1 and PON3 protein, as well as regulate their mRNA expression in HepG2 cells[2]. Besides this, it was found that α-lipoic acid had good antioxidant activity in C2C12 myotubes, through upregulating catalase expression[3]. In vivo studies, α-lipoic acid has the ability of protecting the cortical neurons against the high-fat diet-induced cerebral damage in mice, by inhibiting the oxidative stress and inflammatory reactions[4]. In addition, α-lipoic acid could contribute to the mitigation of α-cypermethrin-induced toxicity in cerebellum of treated rats[5].

α-Lipoic Acid/α-硫辛酸 细胞实验

Cell Line
Concentration Treated Time Description References
AR42J cells 5 µM 1, 2, and 3 hours Α-Lipoic acid increased the protein levels of PPAR-γ and its target genes HO-1 and catalase. Mol Med Rep. 2022 Aug;26(2):264
LMP (CD34pos, CD45RApos, CD133pos) 100 µM 10 days To evaluate the effect of ALA on the expansion of LMP cells, results showed that ALA significantly increased the expansion of LMP cells. Biomolecules. 2022 Mar 11;12(3):431
EMP (CD34pos, CD45RAneg, CD133low) 100 µM 10 days To evaluate the effect of ALA on the expansion of EMP cells, results showed that ALA significantly increased the expansion of EMP cells. Biomolecules. 2022 Mar 11;12(3):431
SSPB CD34 positive cells 30 to 250 µM 10 days To evaluate the effect of ALA on the ex vivo expansion of SSPB CD34 positive cells, results showed that ALA decreased total cell expansion in a dose-dependent manner but significantly increased the expansion of CD34 positive cells. Biomolecules. 2022 Mar 11;12(3):431
Human colorectal adenocarcinoma cells Caco-2 50, 150, 300 µM 12hours ALA significantly promoted Caco-2 cell migration, increased the expression of mucosal tight junction factors ZO-1 and OCLN, and accelerated cell injury repair. Mediators Inflamm. 2022 Jun 7;2022:1894379
Human colonic epithelial cells NCM460 50, 150, 300 µM 12hours and 24hours ALA significantly promoted NCM460 cell migration, increased the expression of mucosal tight junction factors ZO-1 and OCLN, and accelerated cell injury repair. Mediators Inflamm. 2022 Jun 7;2022:1894379
MC3T3-E1 100 nM 2 days To assess the effect of α-LA on PCa-mediated osteoblast differentiation, results showed that α-LA significantly inhibited PCa-mediated osteoblast differentiation. Sci Rep. 2024 Feb 22;14(1):4404
LMH cells 10 µM As2O3 + 25 µM LA 24 hours To evaluate the protective effect of α-lipoic acid on arsenic-induced hepatocyte injury, results showed that α-lipoic acid significantly alleviated the decline in cell proliferation rate induced by arsenic. Adv Sci (Weinh). 2025 Mar;12(11):e2413255
HEI-OC1 cells 500 µM 24 hours To investigate the protective effect of α-LA against cisplatin-induced ototoxicity, results showed that α-LA pretreatment significantly improved cell viability. Int J Mol Sci. 2022 Sep 19;23(18):10981
3T3-L1 preadipocytes 5 µM, 25 µM, 100 µM 24 hours, 48 hours, 10 d, 17 d Α-Lipoic acid ameliorated the morphology of Atp7a−/− cells similarly to the copper chelator BCS but through a different mechanism. LA did not decrease intracellular copper levels but instead increased selenium levels and selenoprotein expression, improving the cellular redox environment. Proc Natl Acad Sci U S A. 2023 Oct 3;120(40):e2305961120
AR42J cells 2 or 5 µM 45 minutes Α-Lipoic acid dose-dependently inhibited the cerulein/resistin-induced increase in intracellular ROS levels and IL-6 expression levels. Mol Med Rep. 2022 Aug;26(2):264
C4-2B 50, 100, 200, 300, 500, 1000, 2000 µM 48 hours To assess the impact of α-LA on cell viability, results showed that α-LA treatment significantly reduced cell viability in a dose-dependent manner. Sci Rep. 2024 Feb 22;14(1):4404
22Rv1 50, 100, 200, 300, 500, 1000, 2000 µM 48 hours To assess the impact of α-LA on cell viability, results showed that α-LA treatment significantly reduced cell viability in a dose-dependent manner. Sci Rep. 2024 Feb 22;14(1):4404
BMMs 100 nM 7 days To assess the effect of α-LA on PCa-mediated osteoclast differentiation, results showed that α-LA significantly inhibited PCa-mediated osteoclast differentiation. Sci Rep. 2024 Feb 22;14(1):4404
HSC/MPP (CD34pos, CD45RAneg, CD133pos) 100 µM 7 days To evaluate the effect of ALA on the expansion of HSC/MPP cells, results showed that ALA significantly increased the expansion of HSC/MPP cells. Biomolecules. 2022 Mar 11;12(3):431

α-Lipoic Acid/α-硫辛酸 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Normal diet vs. 0.2% α-lipoic acid supplemented diet model Oral (dietary addition) 0.2% dietary supplementation Ad libitum for 5 weeks Investigated the effect of α-lipoic acid on hepatic lipid deposition, showing reduced plasma triglyceride levels, hepatic triglyceride content, downregulated FASN and FABP1 protein expression, and upregulated p-HSL protein expression. Nutrients. 2021 Jul 8;13(7):2331
Drosophila melanogaster Aged Drosophila midgut model Oral 0.5 mM Started at day 26 and lasted for 14 days ALA significantly reversed the age-associated hyperproliferation of intestinal stem cells (ISCs) and the decline of intestinal function in aged Drosophila, extending their lifespan. ALA reversed age-associated ISC dysfunction by promoting the activation of the endocytosis–autophagy network. EMBO Rep. 2020 Aug 5;21(8):e49583
Rats High fat diet-induced obesity model Oral gavage 100 mg/kg Daily for 4 weeks ALA attenuated the hepatic and renal complications induced by obesity in rats through reducing oxidative stress and inflammation. Naunyn Schmiedebergs Arch Pharmacol. 2023 Nov;396(11):3017-3031
Rats Sprague Dawley rats Intraperitoneal injection 100 mg/kg Single injection, sacrificed after 30 minutes To study the effects of α-lipoic acid on metabolites of the methionine pathway. Results showed a massive increase in serum S-adenosylhomocysteine (SAH) and marked depletion of liver S-adenosylmethionine (SAM) after α-lipoic acid injection. Free Radic Biol Med. 2009 Oct 15;47(8):1147-53
Hailan Brown chickens Arsenic-induced liver injury model Feed additive 27.27 mg/kg As2O3 + 200/400 mg/kg LA Continued for 20 or 32 weeks To evaluate the protective effect of α-lipoic acid on arsenic-induced liver injury, results showed that α-lipoic acid significantly alleviated arsenic-induced liver function damage and lipid metabolism disorders. Adv Sci (Weinh). 2025 Mar;12(11):e2413255
Wistar rats Metabolic dysfunction-associated steatotic liver disease (MASLD) model Intragastric administration 30 mg/kg Once daily for eight weeks To evaluate the protective effect of α-lipoic acid on hepatic sphingolipid metabolism and insulin signaling transduction in MASLD rats. Results showed that α-LA decreased sphinganine, dihydroceramide, and sphingosine levels, increased ceramide level, and activated the PI3K/Akt/mTOR pathway. Nutrients. 2024 May 16;16(10):1501
Sprague-Dawley rats Incisional pain model Intraperitoneal injection 60 mg/kg and 120 mg/kg Single injection or repeated injections (three consecutive days before surgery and on POD 0, POD 1, and POD 2 after surgery) To evaluate the analgesic effects of ALA in a postsurgical pain model. Results showed that single and repeated intraperitoneal injections of ALA significantly reduced evoked mechanical hyperalgesia after surgery, and repeated preemptive injections effectively alleviated spontaneous postsurgical pain. Channels (Austin). 2021 Dec;15(1):398-407
Wistar rats Hypercaloric choline-deficient diet-induced NAFLD model Dietary supplementation 61 mg/kg Once daily for 8 weeks To investigate the impact of α-lipoic acid on oxidative stress and lipid accumulation induced by a hypercaloric choline-deficient diet. Results showed that α-lipoic acid detains obesity development but exacerbates diet-induced oxidative stress and lipid accumulation in the liver. Nutrients. 2021 Jun 10;13(6):1999
Rats Normal rats and pylorus-ligated rats Oral, intravenous, intraduodenal, intraportal administration Oral 20 mg LA/kg, intravenous 5 mg LA/kg Single administration To study the enantioselective pharmacokinetics of α-lipoic acid, it was found that the exposure of R-α-lipoic acid was higher than that of S-α-lipoic acid, and the enantioselectivity occurred in the absorption phase rather than the elimination phase. Int J Mol Sci. 2015 Sep 21;16(9):22781-94

α-Lipoic Acid/α-硫辛酸 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01931787 Recurrent Small Cell Lung Canc... 展开 >>er 收起 << Phase 1 Completed - United States, North Carolina ... 展开 >> Comprehensive Cancer Center of Wake Forest University Winston-Salem, North Carolina, United States, 27157 收起 <<
NCT01471652 Chronic Fatigue Syndrome Phase 2 Withdrawn(PI left the institut... 展开 >>ion) 收起 << - United States, New York ... 展开 >> Columbia University Department of Clinical Genetics New York, New York, United States, 10032 收起 <<
NCT00664001 Acute Mountain Sickness Phase 3 Completed - United Kingdom ... 展开 >> University of Edinburgh Edinburgh, United Kingdom 收起 <<

α-Lipoic Acid/α-硫辛酸 参考文献

[1]Gomes MB, Negrato CA. Alpha-lipoic acid as a pleiotropic compound with potential therapeutic use in diabetes and other chronic diseases. Diabetol Metab Syndr. 2014;6(1):80.

[2]Ozgun E, Sayilan Ozgun G, et al. Effect of lipoic acid on paraoxonase-1 and paraoxonase-3 protein levels, mRNA expression and arylesterase activity in liver hepatoma cells. Gen Physiol Biophys. 2017;36(4):465-470.

[3]Lee CT, Chang LC, Wu PF. Lipoic Acid Exerts Antioxidant and Anti-inflammatory Effects in Response to Heat Shock in C2C12 Myotubes. Inflammation. 2016;39(3):1160-8.

[4]Liu Y, Zhang Q, et al. The α-lipoic acid improves high-fat diet-induced cerebral damage through inhibition of oxidative stress and inflammatory reaction. Environ Toxicol Pharmacol. 2017.

[5]Elsawy H, Al-Omair MA, et al. Protective effect of α-lipoic acid against α-cypermethrin-induced changes in rat cerebellum. J Chem Neuroanat. 2017.

α-Lipoic Acid/α-硫辛酸 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.85mL

0.97mL

0.48mL

24.23mL

4.85mL

2.42mL

48.47mL

9.69mL

4.85mL

α-Lipoic Acid/α-硫辛酸 技术信息

CAS号1077-28-7
分子式C8H14O2S2
分子量 206.33
SMILES Code C(C1CCSS1)CCCC(O)=O
MDL No. MFCD00005474
别名 DL-硫辛酸 ;Thioctic acid; DL-α-Lipoic acid; (±)-α-Lipoic acid
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

DMSO: 105 mg/mL(508.9 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
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