Background:

Canagliflozin is a novel, potent, and highly selective sodium glucose co-transporter (SGLT) 2 inhibitor [1]. It has been proved that Canagliflozin can increase urine glucose excretion by reducing the renal glucose threshold and by decreasing the filtered glucose re-absorption [2].

Canagliflozin has been shown to inhibit the Na+-mediated 14C-AMG intakes in CHO-hSGLT2, CHO-rat SGLT2 and CHO-mouse SGLT2?with IC50 values of 4.4, 3.7 and 2.0 nM, respectively [1].

Canagliflozin has been reported to reduce the blood glucose (BG) levels dose-dependently in both db/db Mice and Zucker diabetic fatty (ZDF) Rats. Additionally, canagliflozin has proved to decrease the respiratory exchange ratio, and body weight in DIO mice and ZDF rats [1].

Canagliflozin can be taken orally [1].

参考文献:
[1] Liang Y1,?Arakawa K,?Ueta K,?Matsushita Y,?Kuriyama C?Martin T,?Du F,?Liu Y,?Xu J,?Conway B,?Conway J,?Polidori D,?Ways K,?Demarest K. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One.?2012;7(2):e30555
[2] Sarnoski-Brocavich S,?Hilas O. Canagliflozin (Invokana), a Novel Oral Agent For Type-2 Diabetes. P T.?2013 Nov;38(11):656-66