95510-70-6

• 常用中文名：奥美拉唑钠
• 常用英文名：Omeprazole sodium monohydrate
• CAS号：95510-70-6
• 分子式：C₁₇H₂₀N₃NaO₄S
• 分子量：385.413
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2018-05-06 08:00:00
• 更新时间：2024-01-08 19:04:01
• Omeprazole (H 16868) 是一种质子泵 (proton pump) 抑制剂 (PPI),有潜力用于胃肠道疾病的研究。Omeprazole 竞争性抑制 CYP2C19 活性,Ki 为 2 到 6 μM。Omeprazole 还抑制革兰氏阳性菌和革兰氏阴性菌生长。Omeprazole 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。

名称

• 中文名: 奥美拉唑钠
• 英文名: Omeprazole sodium
• 中文别名: 5-甲氧基-2-[(4-甲氧基-3,5-二甲基-2-吡啶基)-甲基亚砜]-3H-苯并咪唑钠盐
• 英文别名: Omeprazole powder/pellets/sodium; Sodium 5-methoxy-2-{[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl}benzimidazol-1-ide hydrate (1:1:1); MFCD01939422; Omeprazole sodium hydrate; Omeprazole,sodium salt; sodium 5-methoxy-2-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl]benzoimidazole; 5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)sulfinyl)-1h-benzimidazole sodium salt; 1H-Benzimidazole, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-, sodium salt, hydrate (1:1:1)

物化性质

• 密度: 1.37g/cm3
• 沸点: 600ºC at 760mmHg
• 熔点: 220°C
• 分子式: C₁₇H₂₀N₃NaO₄S
• 分子量: 385.413
• 闪点: 316.7ºC
• 精确质量: 385.107208
• PSA: 94.68000
• LogP: 3.48690
• 外观性状: 在水中透明
• 储存条件: 室温

生物活性

• 描述: Omeprazole (H 16868) 是一种质子泵 (proton pump) 抑制剂 (PPI),有潜力用于胃肠道疾病的研究。Omeprazole 竞争性抑制 CYP2C19 活性,Ki 为 2 到 6 μM。Omeprazole 还抑制革兰氏阳性菌和革兰氏阴性菌生长。Omeprazole 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 感染
  信号通路 >> 代谢酶/蛋白酶 >> 磷脂
  信号通路 >> 自噬 >> 自噬
  研究领域 >> 代谢疾病
  信号通路 >> 跨膜转运 >> 质子泵
  信号通路 >> 抗感染 >> 细菌
• 体外研究: 奥美拉唑(h16868)是一种质子泵抑制剂,用于治疗消化不良、消化性溃疡病、胃食管反流病、咽喉反流和Zollinger-Ellison综合征。奥美拉唑(H 16868)几乎消除了所有患者的胃内酸度：24小时胃内pH值中位数从1.4上升到5.3,平均小时氢离子活性从38.50降至1.95 mmol(mEq)/1(p<0.001)。这种对24小时胃内酸性的抑制作用比以前报道的每天服用1克西咪替丁或每天服用300毫克雷尼替丁更为深刻[1]。研究了一组健康男性受试者单次和多次口服30和60毫克奥美拉唑的药代动力学。奥美拉唑(H 16868)从其肠溶制剂中的吸收是不可预测的。反复给药后,血浆浓度-时间曲线(AUC)下面积显著增加。奥美拉唑(H 16868)在反复给药后增加自身的相对可用性。这可能是由于奥美拉唑(一种不耐酸的化合物)抑制胃酸分泌所致[2]。奥美拉唑钠是一种有效的脑渗透剂中性鞘磷脂酶(N-SMase)抑制剂(外显体抑制剂)[3]。
• 参考文献:

  [1]. Li XQ, et al. Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. Drug Metab Dispos. 2004 Aug;32(8):821-7.

  [2]. Jonkers D, et al. Omeprazole inhibits growth of gram-positive and gram-negative bacteria including Helicobacter pylori in vitro. J Antimicrob Chemother. 1996 Jan;37(1):145-50.

  [3]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DD9088500 CHEMICAL NAME : 1H-Benzimidazole, 5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)met hyl)sulfinyl)-, sodium salt, hydrate CAS REGISTRY NUMBER : 95510-70-6 LAST UPDATED : 199512 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C17-H18-N3-O3-S.Na.H2-O MOLECULAR WEIGHT : 385.45 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 278 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,479,1995 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 400 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,497,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 4550 mg/kg/13W-I TOXIC EFFECTS : Gastrointestinal - other changes Skin and Appendages - dermatitis, other (after systemic exposure) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,479,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 328 mg/kg/13W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in bladder weight REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,497,1995 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 8400 mg/kg SEX/DURATION : male 9 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,573,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 83200 ug/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 49,573,1995

安全

• 海关编码: 2933990090

海关

海关编码	2933990090
中文概述	2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
申报要素	品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%