艾普拉唑

简介药理作用用途副作用生物活性靶点体外研究体内研究艾普拉唑试剂级价格

艾普拉唑

CAS号:172152-36-2
英文名:Ilaprazole
中文名:艾普拉唑
CBNumber:CB51459367
分子式:C19H18N4O2S
分子量:366.44
MOL File:172152-36-2.mol

艾普拉唑化学性质

沸点 :651.0±65.0 °C(Predicted)
密度 :1.39
储存条件 :Sealed in dry,Store in freezer, under -20°C
溶解度 :DMF: 10mg/mL; DMSO: 15mg/mL; DMSO:PBS (pH 7.2) (1:7): 0.12mg/mL; Ethanol: 0.3mg/mL
形态 :A solid
酸度系数(pKa) :8.23±0.10(Predicted)
颜色 :Off-white to gray
InChI :InChI=1S/C19H18N4O2S/c1-13-17(20-8-7-18(13)25-2)12-26(24)19-21-15-6-5-14(11-16(15)22-19)23-9-3-4-10-23/h3-11H,12H2,1-2H3,(H,21,22)
InChIKey :HRRXCXABAPSOCP-UHFFFAOYSA-N
SMILES :C1(S(CC2=NC=CC(OC)=C2C)=O)NC2=CC(N3C=CC=C3)=CC=C2N=1

艾普拉唑性质、用途与生产工艺

简介艾普拉唑是一种强效的质子泵抑制剂，通过干扰胃壁细胞上分泌胃酸的质子泵而起作用，其抑制胃酸的效果在同类药物中是最强的。
药理作用
艾普拉唑属不可逆型质子泵抑制剂，其结构属于苯并咪唑类。艾普拉唑经口服后选择性地进入胃壁细胞，转化为次磺酰胺活性代谢物，与H + /K+ -ATP酶上的巯基作用，形成二硫键的共价结合，不可逆抑制H + /K+ -ATP酶，产生抑制胃酸分泌的作用。
用途艾普拉唑目前主要用于胃糜烂、胃炎、反流性食管炎、消化性溃疡，以及幽门螺旋杆菌等感染。
副作用
艾普拉唑的普遍副作用有（发病率超过1%、低于10%）有腹泻（2.41%）、头晕目眩（2.41%）、血细胞转氨酶（ALT/AST）上升（1.81%）；罕见副作用（发病率超过0.1%、低于1%）有皮疹、荨麻疹、腰痛、腹胀、口干口苦口臭、胸闷气短、心悸、月经时间增加、肾功能异常（蛋白尿、BUN上升）、心电图异常（室性期前收缩、I度房室传导阻滞）、白细胞减少等。所述副作用常以轻、轻中度，可自主修复。
生物活性 Ilaprazole (IY-81149)是新型的质子泵 (proton pump)抑制剂，用于治疗消化不良、消化性溃疡、胃食管返流疾病和十二指肠溃疡。它能抑制H+/K+-ATPase，IC50为6 μM。
靶点
Target Value
Proton pump
()
H+/K+-ATPase
(Cell-free assay) 6 μM
TOPK
() 111 μM(Kd)
体外研究

On cumulation of 14C-aminopyrine in histamine stimulated parietal cells, the IC ₅₀ of Ilaprazole (IY-81149) sodium is 9 nM.

体内研究

Ilaprazole (3-30 mg/kg; i.d.) dose-dependently inhibits gastric acid secretion.
In anesthetized rats, Ilaprazole dose-dependently increased gastric pH which was lowered by histamine infusion. In the case of i.v. injection, the ED ₅₀ of Ilaprazole and omeprazole is 1.2 and 1.4 mg/kg and in the case of i.d. administration, the ED ₅₀ of Ilaprazole and omeprazole is 3.9 and 4.1 mg/kg, respectively. Ilaprazole also significantly inhibits pentagastrin-stimulated gastric secretion. Its ED ₅₀ is 2.1 mg/kg and that of Omeprazole is 3.5 mg/kg with i.d. administration. In the case of i.v. injection, Ilaprazole is equipotent to Omeprazole. Ilaprazole also inhibits gastric acid secretion strongly in fistular rats. The ED ₅₀ of Ilaprazole administered intraduodenally is 0.43 mg/kg and that of Omeprazole is 0.68 mg/kg.

Animal Model:	Male SD rat (after pylorus ligation)
Dosage:	3, 10, 30 mg/kg
Administration:	Intraduodenally
Result:	The acid output and volume significantly inhibited by about 60 % and 46 % at 3 mg/kg were s, respectively. At 30 mg/kg, it showed 93 % and 73 % inhibition on acid output and volume, respectively.