| Bioactivity | 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]. |
| Invitro | DSO-5a (50 nM; 60min) 在 hBB3-HEK 细胞中诱导 IP-1 积累，pEC50 值为 8.485，引起强烈的钙反应的 pEC50 值为 7.964[1]。DSO-5a (500 nM; 60min) 在 mBB3-HEK 细胞中诱导 IP-1 积累，pEC50 值为 7.262，引起强烈的钙反应的 pEC50 值为 7.174[1]。DSO-5a (0-100 nM； 8min) 在 hBB3-H1299 和 mBB3-HEK 细胞中引起 ERK1/2 的剂量依赖性激活[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | DSO-5a (3-30 mg/kg; P.O.; 30 分钟) 在 C57BL/6 小鼠中以剂量依赖性方式降低血糖波动[1]。DSO-5a (10 mg/kg/day; P.O.; 2-4 周) 可以降低糖尿病 db/db 小鼠血糖浓度[1]。 Animal Model: |
| Name | DSO-5a |
| CAS | 2195411-63-1 |
| Formula | C23H24N2O7 |
| Molar Mass | 440.45 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |