| Description | Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity. |
| In vitro | 每只小鼠脑室内给药0.06–16 μg Gliquidone,可以拮抗叔丁啡,吗啡和美沙酮 产生的抗损伤效应.每只小鼠脑室内给药6 μg Gliquidone可以抑制皮下注射0.125 mg/kg可乐定和皮下注射0.30 mg/kg氯压胍产生的抗损伤效应 ,但是每只小鼠脑室内给药3 μg没有效果. 在雄性swiss白化病小鼠中,每只小鼠脑室内给药0.1–1.0 μg Gliquidone,可以剂量依赖性抑制阿米替林和氯丙咪嗪产生的抗损伤效应.糖尿病大鼠给药10 mg/kg格列喹酮,可以明显降低血压,减少非酶糖基化以及晶体中总蛋白量并能明显提高晶体中谷胱甘肽水平. |
| Target activity | K+ channel:27.2 nM |
| Synonyms | AR-DF 26, 格列喹酮, Glurenorm |
| molecular weight | 527.63 |
| Molecular formula | C27H33N3O6S |
| CAS | 33342-05-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 97 mg/mL (183.8 mM) Ethanol: 6 mg/mL (11.37 mM) |
| References | 1. Angel I, et al. Fundam Clin Pharmacol, 1991, 5(2), 107-115. 2. Galeotti N, et al. Neuropharmacology, 2001, 40(1), 75-84. 3. Ocana M, et al. Br J Pharmacol, 1995, 114(6), 1296-1302. 4. Galeotti N, et al. Br J Pharmacol, 1999, 126(5), 1214-1220. 5. Yarat A, et al. Free Radic Biol Med, 2001, 31(9), 1038-1042. 6. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease[J]. Bioorganic chemistry. 2019 Mar;84:87-97. |
| Citations | 1. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease. Bioorganic Chemistry. 2019 Mar;84:87-97 |