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Mizagliflozin

Catalog No. T16083 CAS 666843-10-3

Synonyms: GSK-1614235 free base, KGA-3235 free base, DSP-3235 free base

Mizagliflozin (GSK-1614235 free base) is a sodium-glucose transporter inhibitor( Ki of 27 nM for human SGLT1). Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

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Mizagliflozin, CAS 666843-10-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 74.00
2 mg	In stock	$ 107.00
5 mg	In stock	$ 166.00
10 mg	In stock	$ 288.00
25 mg	In stock	$ 571.00
50 mg	In stock	$ 819.00
100 mg	In stock	$ 1,130.00
1 mL * 10 mM (in DMSO)	In stock	$ 223.00

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Purity: 98.66%

Purity: 98.32%

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Description	Mizagliflozin (GSK-1614235 free base) is a sodium-glucose transporter inhibitor( Ki of 27 nM for human SGLT1). Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic drug that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.
Targets&IC50	SGLT1 (human):(ki)27 nM, SGLT2 (human):8170 nM(ki)
In vivo	Mizagliflozin, a novel selective sodium glucose co-transporter 1 (SGLT1) inhibitor, for the amelioration of chronic constipation.?Mizagliflozin's inhibitory activity against SGLTs was evaluated by an in vitro assay of cells transiently expressing SGLTs.?The safety profile of an initial single dose (2-160mg, orally) and multiple doses (2-20mg, orally, once daily immediately prior to breakfast on Days 1 and 13, and three times daily immediately prior to every meal on Days 3-12) of mizagliflozin was determined by performing a phase I study in healthy male subjects.?In addition, the effect of mizagliflozin and lubiprostone on fecal wet weight was compared using a dog model of loperamide-induced constipation and rat model of low-fiber-diet-induced constipation.?Mizagliflozin potently inhibited human SGLT1 in a highly selective manner.?The results of the phase I study showed mizagliflozin increased stool frequency and loosened stool consistency;?these effects increased progressively with an increase in the dosage and the number of doses of mizagliflozin.?In addition, the oral administration of mizagliflozin increased fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation, similar to lubiprostone.?The potential use of a novel selective SGLT1 inhibitor, mizagliflozin, for the amelioration of chronic constipation[1].

Synonyms	GSK-1614235 free base, KGA-3235 free base, DSP-3235 free base
Molecular Weight	564.67
Formula	C28H44N4O8
CAS No.	666843-10-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Methanol: 250 mg/mL (442.74 mM), Sonification is recommended.

DMSO: 100 mg/mL (177.09 mM), Sonification is recommended.

References and Literature

1. Inoue T, et al. Mizagliflozin, a novel selective SGLT1 inhibitor, exhibits potential in the amelioration of chronic constipation. Eur J Pharmacol. 2017 Jul 5;806:25-31. 2. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library GPCR Compound Library Target-Focused Phenotypic Screening Library Orally Active Compound Library Bioactive Compound Library Glutamine Metabolism Compound Library NO PAINS Compound Library Glycometabolism Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library

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Keywords

Mizagliflozin 666843-10-3 GPCR/G Protein SGLT Chronic GSK1614235 DSP3235 DSP-3235 KGA3235 selective Sodium-dependent glucose cotransporters constipation GSK-1614235 free base DSP 3235 antidiabetic disorder KGA-3235 free base gastrointestinal DSP-3235 free base GSK 1614235 inhibit GSK-1614235 KGA-3235 Inhibitor KGA 3235 inhibitor

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