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Probucol

MCE China：Probucol

Brand：MedChemExpress (MCE)

Cat. No.HY-B0388

CAS：23288-49-5

Synonyms：DH-581

Purity：99.97%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases.

In Vitro：Probucol (10 μM, 2 h) inhibits ABCA1-mediated cholesterol efflux by affecting the ABCA1 translocation to the plasma membrane, the membrane cholesterol pool, and the 125I-apo-AI binding in J774 macrophages expressing ABCA1[3]. Probucol (10 μM, 24 h) promotes high glucose-induced proliferation and inhibits apoptosis by reducing reactive oxygen species generation in Müller cells[5]. Probucol (0.01–0.1 mL of a 50 mg probucol/mlacetone solution, 60 min) inhibits peroxidation of microsomal membrane lipids and DNA damage induced by Fe-NTA plus H2O2[6]. Probucol (3-10 μM) protects neuroblastoma cells from peroxide-induced damage by activating glutathione peroxidase (GPx)[7]. Probucol (10 μM) promotes osteoblasts differentiation of MC3TE-E1 cells through reducing oxidative stress[11].

In Vivo：Probucol (48 mg/day, diet, 12 weeks) alleviates atherosclerosis by accelerating the process of reverse cholesterol transport, improving the anti-inflammatory and anti-oxidant functions in rabbits[4]. Probucol (60 mg/kg, i.p., 2 weeks) promotes endogenous antioxidants and provides protection against adriamycin-induced cardiomyopathy in Sprague-Dawley rats[8]. Probucol (cumulative dose, 120 mg/kg, i.p., 4 weeks) provide complete protection against adriamycin cardiomyopathy without interfering with its antitumor effect in Sprague-Dawley rats[9]. Probucol (500 mg/kg, intracavernosal injection, daily) enhances the therapeutic efficiency of mesenchymal stem cells in the treatment of erectile dysfunction in diabetic SD rats by prolonging their survival time via Nrf2 pathway[10]. Probucol (1-3.5 mg/kg, p.o., 12 weeks) promotes prevents osteoporosis development through reducing oxidative stress in hormone-deficiency-induced postmenopausal osteoporosis SD rats[11]. Probucol (61 mg/kg, p.o., 80 days) exerts multiple beneficial morphological effects that result in better left ventricular remodeling and function, reduced neurohumoral activation, and preserved renal function in the rats[12]. Probucol (500-1000 mg/kg, p.o., once a day for 15 days) recovers pathological damage of myocardial tissue through improvement of myocardium-related proteins Caspase-3 and Caspase-9 in viral myocarditis rats[13].

IC50 & Target：Caspase 3 Caspase 9

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References：

[1]. 1. A Unique Antilipidemic Drug - Probucol". Journal of Atherosclerosis and Thrombosis. 15 (6): 304–5.  [Content Brief]

[2]. 2. Steinberg D. Studies on the mechanism of action of probucol. Am J Cardiol. 1986 Jun 27;57(16):16H-21H.  [Content Brief]

[3]. 3. Favari E, et al. Probucol inhibits ABCA1-mediated cellular lipid efflux. Arterioscler Thromb Vasc Biol. 2004 Dec;24(12):2345-50.  [Content Brief]

[4]. 4. Zhong JK, et al. Probucol alleviates atherosclerosis and improves high density lipoprotein function. Lipids Health Dis. 2011 Nov 12;10:210.  [Content Brief]

[5]. 5. Zhou X, et al. Probucol promotes high glucose-induced proliferation and inhibits apoptosis by reducing reactive oxygen species generation in Müller cells. Int Ophthalmol. 2019 Dec;39(12):2833-2842.  [Content Brief]

[6]. 6. Iqbal M, et al. Probucol as a potent inhibitor of oxygen radical-induced lipid peroxidation and DNA damage: in vitro studies. Redox Rep. 2004;9(3):167-72.  [Content Brief]

[7]. 7. Santos DB, et al. Probucol Protects Neuronal Cells Against Peroxide-Induced Damage and Directly Activates Glutathione Peroxidase-1. Mol Neurobiol. 2020 Aug;57(8):3245-3257.  [Content Brief]

[8]. 8. Siveski-Iliskovic, et al. Probucol promotes endogenous antioxidants and provides protection against adriamycin-induced cardiomyopathy in rats. Circulation. 1994 Jun;89(6):2829-35.  [Content Brief]

[9]. 9. Siveski-Iliskovic, et al. Probucol protects against adriamycin cardiomyopathy without interfering with its antitumor effect. Circulation. 1995 Jan 1;91(1):10-5.  [Content Brief]

[10]. 10. Wang H, et al. Probucol enhances the therapeutic efficiency of mesenchymal stem cells in the treatment of erectile dysfunction in diabetic rats by prolonging their survival time via Nrf2 pathway. Stem Cell Res Ther. 2020 Jul 21;11(1):302.  [Content Brief]

[11]. 11. Tao ZS, et al. Probucol promotes osteoblasts differentiation and prevents osteoporosis development through reducing oxidative stress. Mol Med. 2022 Jun 28;28(1):75.  [Content Brief]

[12]. 12. Sia YT, et al. Beneficial effects of long-term use of the antioxidant probucol in heart failure in the rat. Circulation. 2002 May 28;105(21):2549-55.  [Content Brief]

[13]. 13. Zhang W, et al. Probucol recovers pathological damage in viral Myocarditis through improvement of myocardium-related proteins. Microb Pathog. 2020 Oct;147:104257.  [Content Brief]