Identification | Back Directory | [Name]
L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol (1:1) | [CAS]
951382-34-6 | [Synonyms]
CPD1060 l-prolinecompd Ipragliflozin-002-L L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol (1:1) L-Proline compd. with (1S)-1,5-anhydro-1-C-[3-(benzo[b]thien-2-ylmethyl)-4-fluorophenyl]-D-glucitol (1:1)ChemicalBook (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol,(2S)-pyrrolidine-2-carboxylic acid L-proline compound with (3R,4R,5S,6R)-2-(3-(benzo[b]thiophen-2-ylmethyl)-4-fluorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (1:1) | [Molecular Formula]
C26H30FNO7S | [MDL Number]
MFCD27956926 | [MOL File]
951382-34-6.mol | [Molecular Weight]
519.58 |
Hazard Information | Back Directory | [Uses]
Ipragliflozin (L-Proline) is a highly potent and selective SGLT2 inhibitor with an IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. | [in vivo]
Ipragliflozin (L-Proline) shows good pharmacokinetic properties following oral dosing, and dose-dependently increases urinary glucose excretion, which lasts for over 12 h in normal mice [3]. Oral administration of ipragliflozin increases urinary glucose excretion in a dose-dependent manner, an effect which is significant at doses of 0.3 mg/kg or higher and lasts over 12 h[4]. Single administration of ipragliflozin dose-dependently increases urinary glucose excretion, reduces blood glucose and plasma insulin levels, and improves glucose intolerance [5]. | [IC 50]
SGLT2 | [References]
[1] Imamura M, et al. Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012 May 15;20(10):3263-79. DOI:10.1016/j.bmc.2012.03.051 [2] Suzuki M, et al. Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther. 2012 Jun;341(3):692-701. DOI:10.1124/jpet.112.191593 [3] Tahara A, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36. DOI:10.1007/s00210-011-0713-z [4] Tahara A, et al. Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. J Pharmacol Sci. 2012;120(1):36-44. DOI:10.1254/jphs.12089fp [5] Tahara A, et al. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013 Sep 5;715(1-3):246-55. DOI:10.1016/j.ejphar.2013.05.014 |
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