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Tebuconazole

MCE China：Tebuconazole

Brand：MedChemExpress (MCE)

Cat. No.HY-B0852

CAS：107534-96-3

Purity：99.66%

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：Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.

In Vitro：Tebuconazole (TEB) (20–80 μM, 24 h) shows lipid accumulation in HepG2 cells[2]. Tebuconazole (20–80 μM, 12 h) increases the nuclear translocation of peroxisome proliferator-activated receptors and the expression of lipid uptake and oxidation-related markers in HepG2 cells[2]. Tebuconazole (20–80 μM, 24 h) increases oxidative stress levels, induces the loss of mitochondrial membrane potential and lower levels of microsomal triglyceride transfer protein in the HepG2 cells[2]. Tebuconazole (0-750 μM, 24 hours) decreases MAC-T cells viability and proliferation and induced mitochondria-mediated apoptotic MAC-T cell death by activating ER stress[3]. Tebuconazole (0-100 μM, 24 hours) induces dose-dependent cell death in H9c2 cardiomyoblasts and in adult rat ventricular myocytes (ARVM)[4]. Tebuconazole (30-60 μM, 24 hours) induces DNA damage and ROS generation and lipid peroxidation in H9c2 cells[4].

In Vivo：Tebuconazole (TEB) (10-50 mg/kg, p.o., once daily for 28 days) induces a multiplicity of CYPs and oxidative stress in liver; inhibits testicular P450 and glutathione S-transferase activities; and produces anti-androgenic effects in male rats[5]. Tebuconazole (25-100 mg/kg, p.o., daily for 10 days) causes the proliferation of fetal Leydig cells and increases fetal serum testosterone and progesterone levels in gestational rat[6].

IC50 & Target：CYP51

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References：

[1]. Warrilow AG, et al. Azole affinity of sterol 14α-demethylase (CYP51) enzymes from Candida albicans and Homo sapiens. Antimicrob Agents Chemother. 2013 Mar;57(3):1352-60.  [Content Brief]

[2]. Kwon HC, et.al. Tebuconazole Fungicide Induces Lipid Accumulation and Oxidative Stress in HepG2 Cells. Foods. 2021 Sep 22;10(10):2242.  [Content Brief]

[3]. Lee WY, et.al. Tebuconazole Induces ER-Stress-Mediated Cell Death in Bovine Mammary Epithelial Cell Lines. Toxics. 2023 Apr 21;11(4):397.  [Content Brief]

[4]. Ben Othmène Y,et.al. Tebuconazole induces ROS-dependent cardiac cell toxicity by activating DNA damage and mitochondrial apoptotic pathway. Ecotoxicol Environ Saf. 2020 Nov;204:111040.  [Content Brief]

[5]. Yang JD, et.al. Effects of tebuconazole on cytochrome P450 enzymes, oxidative stress, and endocrine disruption in male rats. Environ Toxicol. 2018 Jun 19.  [Content Brief]

[6]. Ma F, et.al. Gestational exposure to tebuconazole affects the development of rat fetal Leydig cells. Chemosphere. 2021 Jan;262:127792.  [Content Brief]