(R)-Lansoprazole 是Lansoprazole 的R型异构体。Lansoprazole 是口服有效的质子泵抑制剂,能抑制胃酸生成。Lansoprazole 是中性鞘磷脂酶(N-SMase)的抑制剂(外泌体抑制剂),能透过血脑屏障。
产品描述
Dexlansoprazole is the R-isomer of lansoprazole and a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity.Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)
体外活性
Dexlansoprazole, constitutes >80% of circulating drug after oral administration of lansoprazole, provides lower clearance and 5-fold greater systemic exposure than the S-enantiomer following oral administration of lansoprazole. Dexlansoprazole MR is a modified release formulation of dexlansoprazole, which employs a novel Dual Delayed Release (DDR) technology that delivers the drug in two discrete phases of release, thereby inhibiting newly activated proton pumps that turn over following initial PPI inactivation of H+,K+-ATPase. Dexlansoprazole MR maintains plasma drug concentrations above the threshold level longer than lansoprazole at all doses, resulting in an optimized drug exposure-intragastric pH relationship. [1] Dexlansoprazole selectively suppresses gastric acid secretion by direct inhibition of the H+K+-ATPase proton pump in the gastric parietal cell, inhibition of this cell membrane enzyme ultimately blocks the final step in acid production. [2]
Cas No.
138530-94-6
分子式
C16H14F3N3O2S
分子量
369.36
别名
TAK 390;Dexlansoprazole;右旋兰索拉唑;R-(+)-Lansoprazole;T 168390
储存和溶解度
DMSO:74 mg/mL (200.34 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years