Canagliflozin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性 SGLT2 抑制剂，对 hSGLT2、rSGLT2 和 mSGLT2 的 IC50 分别为 4.4、3.7 和 2.0 nM。

A highly potent and selective SGLT2 inhibitor with IC50 of 4.4, 3.7 and 2.0 nM for hSGLT2, rSGLT2 and mSGLT2, respectively; displays >100-fold selectivity over SGLT1; improves glycemic control and beta-cell function in rodent models of T2DM, and reduces body weight gain in rodent models of obesity.Diabetes Approved(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) 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.

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 rats Dosage: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.

JNJ 24831754ZAE | JNJ 28431754 | JNJ 28431754AAA | TA 7284

GPCR/G Protein

SGLT

hSGLT2|mSGLT2|rSGLT2

Metabolic Disease

Diabetes

842133-18-0

444.5157

C24H25FO5S

>98% (HPLC)

10 mM in DMSO

CC1=C(C=C(C=C1)[C@H]2[C@@H]([C@H]([C@@H]([C@H](O2)CO)O)O)O)CC3=CC=C(S3)C4=CC=C(C=C4)F

D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-, (1S)-

(-20℃)

With Ice Pack

≥ 2 years