FOXO1-IN-3,2451093-95-9

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FOXO1-IN-3

CAS No. : 2451093-95-9

MCE 国际站：FOXO1-IN-3

产品活性：FOXO1-IN-3 是一种高度选择性且具有口服活性的 FOXO1 抑制剂。FOXO1-IN-3 减少小鼠肝脏葡萄糖的产生。FOXO1-IN-3 可改善 db/db 小鼠的胰岛素敏感性和血糖控制，且不会导致体重增加。

研究领域：Others

作用靶点：Others

In Vitro: FOXO1-IN-3 (Compound 10) (10 μM, 6 h) suppresses cAMP/Dexamethasone (HY-14648) induced G6pc and Pck1 mRNA expression in primary hepatocytes isolated from normal mice.

In Vivo: FOXO1-IN-3 (Compound 10) (16 mg/kg, p.o., twice daily, for 10 days) reduces blood glucose in db/db mice.
FOXO1-IN-3 (16 mg/kg, p.o., twice daily, for 7 days) and FGF21 (0.45 mg/kg) has synergistic glucose-lowering effects in Streptozotocin (HY-13753) induced β-cell-ablated diabetic mice.
FOXO1-IN-3 (1 mg/kg for i.v., 10 mg/kg for p.o.) shows significant plasma exposure and oral bioavailability despite relatively short half-life in mice.
PK properties of FOXO1-IN-3 (compound 10)

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Dose (mg/kg)	parameters	value
i.v. (1 mg/kg)	T1/2	1.23 h
	AUCinf	1.86 μM·h
	CL	22.7 mL/kg·min
p.o. (10 mg/kg)	Tmax	0.67 h
	AUCinf	4.66 μM·h
	F%	25.5%