| Hazard Information | Back Directory | [Uses]
DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research[1]. | [in vivo]
DSO-5a (3-30 mg/kg; P.O.; 30 min) reduces blood glucose excursions in a dose-dependent manner in C57BL/6 mice[1].
DSO-5a (10 mg/kg/day; P.O.; 2-4 weeks) reduces the blood glucose concentration of diabetic db/db mice[1].
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 3 mg/kg; 10 mg/kg; 30 mg/kg | | Administration: | Oral administration;30 min before glucose challenge (3 g/kg) | | Result: | Showed that the change rates of AUC at 3, 10 and 30 mg/kg were 5.03, 16.42 and 28.30%, respectively.
In BB3 knockout mice, DSO-5a failed to inhibit blood glucose drift. |
| Animal Model: | Diabetic db/db mice[1] | | Dosage: | 10 mg/kg/day | | Administration: | Oral administration; 2-4 weeks | | Result: | After two weeks of treatment, the blood glucose excursion of db/db mice was significantly reduced.
After four weeks, fasting blood glucose levels, glycosylated serum protein (GSP), and HOMA-IR were significantly decreased in the DSO-5a treatment group.
Increased the protein expression of PPAR-gamma in white adipose tissue of db/db mice.
|
| [IC 50]
PPARγ | [References]
[1] Wu L, et al. Discovery of Dimethyl Shikonin Oxime 5a, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Type 2 Diabetes Mellitus. J Med Chem. 2023 Jun 22;66(12):8011-8029. DOI:10.1021/acs.jmedchem.3c00323 |
|
|