SKI2852,1346554-47-9

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SKI2852

CAS No. : 1346554-47-9

MCE 国际站：SKI2852

产品活性：SKI2852 是一种有效的、选择性的、具有口服活性的 11β-羟基类固醇脱氢酶 1 型(11β-HSD1) 抑制剂，其对 mHSD1 和 hHSD1 的 IC₅₀ 分别为 1.6 nM 和 2.9 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：11β-HSD

In Vitro: SKI2852 inhibits 11β-HSD1 with an IC₅₀ of 4.4 ± 0.5 nM in HEK293 cells stably transfected with human 11β-HSD1 cDNA.
The amide carbonyl group of SKI2852 established a central hydrogen bond interaction with the hydroxyl side chain of Ser170, one of the key residues (Ser170, Tyr183, and Lys 187) that define the catalytic triad for 11β-HSD1 activity.

In Vivo: SKI2852 (20 mg/kg; oral; once daily for 25 days) significantly reduces blood glucose and HbA1c levels and improved the lipid profiles in ob/ob mice.
In Vivo PK Data for SKI2852

species	iva				pob
	CL (L/kg/h)	Vss (L/kg)	t1/2 (h)	AUC (μg × h/mL)	Cmax (μg/mL)	tmax (h)	AUC (μg × h/mL)	F (%)
mousec	0.42	1.1	1.7	2.35	2.21	1.0	11.26	96
ratc	0.93	2.1	1.8	1.12	1.02	1.3	3.39	60
dogd	0.36	2.4	4.7	1.47	1.12	2.1	11.52	98

^a10% hydroxylpropyl-β-cyclodextrin was used as vehicle. ^b0.5% methylcellulose and 1% Tween80 was used as vehicle. ^cDosed iv at 1 mg/kg, po at 5mg/kg. ^dDosed iv at 0.5 mg/kg, po at 4 mg/kg.

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