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666843-10-3

中文名稱 Mizagliflozin
英文名稱 Mizagliflozin
CAS 666843-10-3
分子式 C28H44N4O8
分子量 564.67
MOL 文件 666843-10-3.mol
更新日期 2024/08/08 15:33:23
666843-10-3 結(jié)構(gòu)式 666843-10-3 結(jié)構(gòu)式

基本信息

中文別名
化合物MIZAGLIFLOZIN
英文別名
Mizagliflozin
DSP-3235 free base
KGA-3235 free base
GSK-1614235 free base
Propanamide, 3-[[3-[4-[[3-(β-D-glucopyranosyloxy)-5-(1-methylethyl)-1H-pyrazol-4-yl]methyl]-3-methylphenoxy]propyl]amino]-2,2-dimethyl-

物理化學(xué)性質(zhì)

沸點(diǎn)837.0±65.0 °C(Predicted)
密度1.274±0.06 g/cm3(Predicted)
儲(chǔ)存條件4°C, protect from light
溶解度Methanol: 250 mg/mL (442.74 mM); DMSO: 100 mg/mL (177.09 mM)
酸度系數(shù)(pKa)12.65±0.70(Predicted)
形態(tài)Solid
顏色Off-white to light yellow

常見問題列表

生物活性
Mizagliflozin (KWA 0711)是一種新型、有效、選擇性的 sodium glucose co-transporter 1 (SGLT1) 抑制劑,對human SGLT1的Ki值為27 nM。Mizagliflozin的選擇性比(Ki value for human SGLT2/Ki value for human SGLT1)為303。Mizagliflozin還有改善慢性便秘的潛在應(yīng)用。
靶點(diǎn)
TargetValue
human SGLT1
(Cell-free assay)
27 nM(Ki)
體內(nèi)研究

Mizagliflozin (DSP-3235 free base) (3-30 mg/kg; oral) exerts a laxative effect.
Mizagliflozin administrated intravenously (0.3?mg/kg) and orally (3?mg/kg) declined with a short half-life (0.23 and 1.14?h, respectively)

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.
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