Bioactivity | FOXO1-IN-3 is a highly-selective and orally active FOXO1 inhibitor. FOXO1-IN-3 reduces hepatic glucose production in mice. FOXO1-IN-3 improves insulin sensitivity and glucose control in db/db mice without causing weight gain[1]. | ||||||||||||
Target | FOXO1 | ||||||||||||
Invitro | FOXO1-IN-3 (Compound 10) (10 μM,6 小时) 抑制正常小鼠原代肝细胞中 cAMP/Dexamethasone (HY-14648) 诱导的 G6pc 和 Pck1 mRNA 表达[1]。 RT-PCRsup>[1] Cell Line: | ||||||||||||
In Vivo | FOXO1-IN-3 (Compound 10) (16 mg/kg,口服,每天两次,持续 10 天) 可降低 db/db 小鼠的血糖[1]。FOXO1-IN-3 (16 mg/kg,口服,每天两次,持续 7 天) 和 FGF21 (0.45 mg/kg) 在 Streptozotocin (HY-13753) 诱导的 β 细胞消除糖尿病小鼠中具有协同降糖作用[1]。FOXO1-IN-3 (静脉注射 1 mg/kg,口服 10 mg/kg) 在小鼠中显示出显着的血浆暴露和口服生物利用度,尽管中的半衰期相对较短[1]。 Animal Model: | ||||||||||||
Name | FOXO1-IN-3 | ||||||||||||
CAS | 2451093-95-9 | ||||||||||||
Formula | C22H23N7O | ||||||||||||
Molar Mass | 401.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Lee YK, et al. FOXO1 inhibition synergizes with FGF21 to normalize glucose control in diabetic mice. Mol Metab. 2021 Jul;49:101187. |