Tofogliflozin(CSG-452) is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouseSGLT2. IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1] Target:SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibitedSGLT2in cells overexpressingSGLT2, and K(i) values for human, rat, and mouseSGLT2inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward humanSGLT2versus humanSGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the testedSGLT2inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4]. in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg·kg 1·min 1 and increased EGP by 1-2 mg·kg 1·min 1, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasmainsulinlevels. No improvement of glycaemic conditions orinsulinlevel was observed with losartan treatment [3].

386.44

C₂₂H₂₆O₆

903565-83-3

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