Canagliflozin 842133-18-0

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Molecular Weight:

444.52 Canagliflozin is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM, exhibits 413-fold selectivity over hSGLT1.

Biological Activity

Canagliflozin is a novel C-glucoside with thiophene ring. Canagliflozin inhibits Na+-dependent 14C-AMG uptake in a concentration-dependent fashion. Canagliflozin inhibits 14C-AMG
uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 0.7 μM and >1 μM,
respectively. Canagliflozin inhibits the facilitative (non-Na+-linked) GLUT-mediated 2H-2-DG
uptake in L6 myoblasts by less than 50%.


In sham-injected oocytes,
Canagliflozin (10 μM) or phlorizin (3 mM) alone in the presence of 50 μM
DNJ does not affect currents. In SGLT3-injected oocytes, DMSO and
Canagliflozin 10 μM inhibits DNJ-induced currents by 15.6% and 23.4%,
respectively.


Canagliflozin shows pronounced anti-hyperglycemic effects in high-fat
diet fed KK (HF-KK) mice. Oral administration at 30 mg/kg of
Canagliflozin to male SD rats induces glucose excretion over 24 hours by
3,696 mg per 200 g body weight. Pharmacokinetic studies reveals a much
higher exposure of Canagliflozin following oral administration.


Following intravenous and oral doses of 3 and 10 mg/kg, respectively, to
male SD rats, AUC0−inf, po, t1/2 and oral
bioavailability are determined to be 35,980 ng·h/mL, 5.2 hours, and 85%,
respectively. Thus, inhibition of SGLT2 in renal tubules after oral
dosing of Canagliflozin is likely to continuously suppress reabsorption
of glucose.


The extensive UGE would reflect excellent pharmacokinetic
properties of Canagliflozin in vivo as well as high potency of SGLT2
inhibition. Since most of the filtered glucose is reabsorbed by SGLT2 in
the renal tubules, the novel compound would be useful for an
anti-diabetic agent. Single oral administration of Canagliflozin at 3
mg/kg remarkably reduced blood glucose levels without influencing food
intake in hyperglycemic high-fat diet fed KK (HF-KK) mice. There is a
48% reduction in blood glucose level versus vehicle at 6 hours.


In
contrast, Canagliflozin only slightly affects blood glucose levels in
normoglycemic mice. Therefore, Canagliflozin would control hyperglycemia
in the therapy of T2DM with low risk of hypoglycemia.

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Product Categories : GPCR & G Protein > SGLT Inhibitor