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Canagliflozin hemihydrate

CAS No. : 928672-86-0

MCE 国际站：Canagliflozin hemihydrate

产品活性：Canagliflozin hemihydrate (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂，作用于表达 mSGLT2，rSGLT2 和 hSGLT2 的 CHO细胞，IC₅₀ 分别为 2 nM，3.7 nM 和 4.4 nM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：SGLT

In Vitro: Canagliflozin inhibits Na⁺-dependent ¹⁴C-AMG uptake in CHO-hSGLT2 cells, with an IC₅₀ of 4.4±1.2 nM. Similar IC₅₀ values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC₅₀ = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits ¹⁴C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC₅₀ of 684±159 nM and >1,000 nM, respectively.

In Vivo: Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice.
Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats.

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