Canagliflozin hemihydrate

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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。

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

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.

Canagliflozin (30 mg/kg treatment for 4 weeks) reduces 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.Animal Model:Diet-induced obese, insulin resistantmice (DIO) Mice Dosage:30 mg/kg Administration:Oral gavage; daily; 4 weeks Result:Reduced BG levels, respiratory exchange ratio, and body weight gain.Animal Model:Male Zucker fatty (ZF) obese, insulin resistant ratsDosage:3 mg/kg Administration:Oral gavage; daily; 3 weeks Result:UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.

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GPCR/G Protein

SGLT

SGLT

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928672-86-0

907.05

C48H52F2O11S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 100 mg/mL (220.50 mM )

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(-20℃)

With Ice Pack

≥ 2 years