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172152-36-2

中文名稱 艾普拉唑
英文名稱 2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole
CAS 172152-36-2
分子式 C19H18N4O2S
分子量 366.44
MOL 文件 172152-36-2.mol
更新日期 2024/12/23 11:22:49
172152-36-2 結(jié)構(gòu)式 172152-36-2 結(jié)構(gòu)式

基本信息

中文別名
替拉唑
奧普拉唑
艾普拉唑
伊拉普拉唑
艾普拉唑/奧普拉唑
艾普拉唑[干冰運(yùn)輸]
英文別名
IY 81149
Ilaprazole(IY 81149)
Ilaprazole USP/EP/BP
IY81149
IY-81149
IY 81149
2-[(4-methoxy-3-methylpyridin-2-yl)methylsulfinyl]-6-pyrrol-1-yl-1H-benzimidazole
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole
2-[[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]5-(1H-pyrrol-1-yl) 1H benzimidazole
2-[[(4-Methoxy-3-methyl-2-pyridinyl)methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-1H-benzimidazole
1H-BenziMidazole,2-[[(4-Methoxy-3-Methyl-2-pyridinyl)Methyl]sulfinyl]-6-(1H-pyrrol-1-yl)-
2-[(4-methoxy-3-methyl-pyridin-2-yl)methylsulfinyl]-5-pyrrol-1-yl-3H-benzoimidazole USP/EP/BP
所屬類別
原料藥:抑制胃酸分泌藥

物理化學(xué)性質(zhì)

沸點(diǎn)651.0±65.0 °C(Predicted)
密度1.39
儲(chǔ)存條件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
酸度系數(shù)(pKa)8.23±0.10(Predicted)
形態(tài)固體
顏色Off-white to gray
InChIInChI=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)
InChIKeyHRRXCXABAPSOCP-UHFFFAOYSA-N
SMILESC1(S(CC2=NC=CC(OC)=C2C)=O)NC2=CC(N3C=CC=C3)=CC=C2N=1

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見(jiàn)問(wèn)題列表

簡(jiǎn)介
艾普拉唑是一種強(qiáng)效的質(zhì)子泵抑制劑,通過(guò)干擾胃壁細(xì)胞上分泌胃酸的質(zhì)子泵而起作用,其抑制胃酸的效果在同類藥物中是最強(qiáng)的。
藥理作用

艾普拉唑?qū)俨豢赡嫘唾|(zhì)子泵抑制劑,其結(jié)構(gòu)屬于苯并咪唑類。艾普拉唑經(jīng)口服后 選擇性地進(jìn)入胃壁細(xì)胞,轉(zhuǎn)化為次磺酰胺活性代謝物,與H + /K+ -ATP酶上的巰基作 用,形成二硫鍵的共價(jià)結(jié)合,不可逆抑制H + /K+ -ATP酶,產(chǎn)生抑制胃酸分泌的作用。

用途
艾普拉唑目前主要用于胃糜爛、胃炎、反流性食管炎、消化性潰瘍,以及幽門螺旋桿菌等感染。
副作用

艾普拉唑的普遍副作用有(發(fā)病率超過(guò)1%、低于10%)有腹瀉(2.41%)、頭暈?zāi)垦#?.41%)、血細(xì)胞轉(zhuǎn)氨酶(ALT/AST)上升(1.81%);罕見(jiàn)副作用(發(fā)病率超過(guò)0.1%、低于1%)有皮疹、蕁麻疹、腰痛、腹脹、口干口苦口臭、胸悶氣短、心悸、月經(jīng)時(shí)間增加、腎功能異常(蛋白尿、BUN上升)、心電圖異常(室性期前收縮、I度房室傳導(dǎo)阻滯)、白細(xì)胞減少等。所述副作用常以輕、輕中度,可自主修復(fù)。

生物活性
Ilaprazole (IY-81149)是新型的質(zhì)子泵 (proton pump)抑制劑,用于治療消化不良、消化性潰瘍、胃食管返流疾病和十二指腸潰瘍。它能抑制H+/K+-ATPase,IC50為6 μM。
靶點(diǎn)
TargetValue
Proton pump
()
H+/K+-ATPase
(Cell-free assay)
6 μM
TOPK
()
111 μM(Kd)
體外研究

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

體內(nèi)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.
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