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
基本信息
中文別名
化合物MIZAGLIFLOZIN 英文別名
MizagliflozinDSP-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(duì)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)
| Target | Value |
|
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. |