Mizagliflozin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Mizagliflozin (DSP-3235、KGA-3235、GSK-1614235) 是一种有效的、选择性的、口服活性的 SGLT1 抑制剂，Ki 为 27 nM，选择性是 SGLT2 的 350 倍以上。

Mizagliflozin (DSP-3235, KGA-3235, GSK-1614235)?is a potent, selective, orally active SGLT1 inhibitor with Ki of 27 nM, displays >350-fold selectivity over SGLT2; increases stool frequency and loosens stool consistency in phase I study; increases fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation, similar to lubiprostone.Diabetes Phase 1 Clinical.

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Animal Model:Male Wistar rats (rat model of low-fiber-diet-induced constipation)Dosage:3, 10, 30 mg/kg Administration:Oral Result:Increased fecal wet weight in a rat model of low-fiber-diet-induced constipation.

DSP-3235 | KGA-3235 | GSK-1614235

GPCR/G Protein

SGLT

SGLT

Metabolic Disease

Diabetes

666843-10-3

564.68

C28H44N4O8

>98% (HPLC)

In Vitro:?H2O : ≥ 100 mg/mL (177.09 mM))

O=C(N)C(C)(C)CNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C(C)=C1

3-((3-(4-((5-isopropyl-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)-1H-pyrazol-4-yl)methyl)-3-methylphenoxy)propyl)amino)-2,2-dimethylpropanamide

(-20℃)

With Ice Pack

≥ 2 years