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TUG-770

CAS No. : 1402601-82-4

MCE 站：TUG-770

产品活性：TUG-770 是一种有效的，选择性的，具有口服活性的 GPR40/FFA1 激动剂，对人 FFA1 的 EC₅₀ 为 6 nM。TUG-770 对 FFA1 的选择性高于 FFA2，FFA3，FFA4，PPARγ，其他受体，转运蛋白和酶。TUG-770 可用于 2 型糖尿病研究。

研究领域：GPCR/G Protein

作用靶点：GPR40

In Vitro: TUG-770 (Compound 22) displays excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 shows excellent stability toward human liver microsomes (HLM), and good permeability in the Caco-2 cell assay.
TUG-770 exhibits lower potency on the rodent orthologs (mFFA1, pEC₅₀ = 6.83; rFFA1, pEC₅₀ = 6.49).
In the rat INS-1E cell line, TUG-770 significantly increases insulin secretion (10.75% of total content with 10 μM 22 vs 8.74 with vehicle) at high glucose concentration (12.4 mM) and, no effect (4.14% of total content with 10 μM 22 vs 4.02 with vehicle) at low glucose concentration (2.8 mM).

In Vivo: TUG-770 (Compound 22; 20 mg/kg; oral administration; daily; for 28 days) treatment significantly improves glucose tolerance, and has no effect on food intake, body weight, body composition or plasma leptin concentration. TUG-770 also significantly improves the insulin sensitivity index (plasma glucose x plasma insulin) .

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