Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Methanol: 250 mg/mL (442.74 mM), Sonification is recommended.
DMSO: 100 mg/mL (177.09 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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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