Dapagliflozin(BMS512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2) is in development for the treatment of type 2 diabetes mellitus (T2DM).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
SGLT2 inhibitors: a new emerging therapeutic class in the treatment of type 2 diabetes mellitus.
Ghosh RK, et al. J Clin Pharmacol. 2012 Apr;52(4):457-63. PMID: 21543663.
|Related SGLT Products|
LX2761 is a locally acting SGLT1 and SGLT2 inhibitor in vitro with IC50 values of 2.2 nM and 2.7 nM for hSGLT1 and hSGLT2, respectively.
Canagliflozin hemihydrate (JNJ-28431754; TA 7284) is a highly potent and selective SGLT2 inhibitor for hSGLT2 with IC50 of 2.2 nM.
LX-4211 is an oral dual SGLT1/SGLT2 inhibitor with IC50 of 36 nM and 1.8 nM, respectively.
Phloretin is a dihydrochalcone found in apple tree leaves, which shows beneficial effects on diabetes.
Phloridzin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively.
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