KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
|Solubility (25°C)||DMSO 100 mg/mL
Water 100 mg/mL
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Kunihiro Kishida, et al. Metabol Open. d-Allose is absorbed via sodium-dependent glucose cotransporter 1 (SGLT1) in the rat small intestine
 Cheng-Che Lee, et al. Biochem Pharmacol. Dapagliflozin attenuates arrhythmic vulnerabilities by regulating connexin43 expression via the AMPK pathway in post-infarcted rat hearts
 Yohei Sawa, et al. J Pharmacol Sci. Pretreatment with KGA-2727, a selective SGLT1 inhibitor, is protective against myocardial infarction-induced ventricular remodeling and heart failure in mice
 Robert L Dobbins, et al. Am J Physiol Gastrointest Liver Physiol. Selective sodium-dependent glucose transporter 1 inhibitors block glucose absorption and impair glucose-dependent insulinotropic peptide release
 Toshihide Shibazaki, et al. J Pharmacol Exp Ther. KGA-2727, a novel selective inhibitor of a high-affinity sodium glucose cotransporter (SGLT1), exhibits antidiabetic efficacy in rodent models
|Related SGLT Products|
Enavogliflozin (DPW-16001), an antidiabetic compound, is a first class selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor with oral activity.
|Remogliflozin etabonate (GSK189075)
Remogliflozin etabonate (GSK189075) is an orally active, selective and low-affinity inhibitor of sodium glucose cotransporter (SGLT2) with Ki of 1950 nM, 2140 nM, 43100 nM, 8570 nM for hSGLT2, rSGLT2, hSGLT1, rSGLT1, respectively. Remogliflozin etabonate exhibits antidiabetic efficacy in rodent models.
Bexagliflozin (EGT1442, EGT-0001442, THR-1442) is a potent and selective SGLT2 inhibitor with an IC50 of 2 nM.
|Ertugliflozin L-pyroglutamic acid
Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2.
Tofogliflozin (CSG-452) hydrate is a potent and highly specific sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 value of 2.9 nM.
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