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95510-70-6生产厂家

95510-70-6价格

95510-70-6

95510-70-6结构式
95510-70-6结构式
  • 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)。

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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)
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
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.

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

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

海关编码 2933990090
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%