76144-81-5

• 常用中文名：米屈肼
• 常用英文名：Mildronate
• CAS号：76144-81-5
• 分子式：C₆H₁₄N₂O₂
• 分子量：146.188
• 相关类别： 原料药 循环系统用药 抗充血性心力衰竭药
• 发布时间：2018-03-29 08:00:00
• 更新时间：2024-01-02 19:47:13
• Mildronate (Meldonium) 是一种心血管保护药,可竞争性的抑制 BBOX1 和OCTN2。Mildronate (Meldonium) 对人重组 BBOX 的 IC50 值为 34-62 μM,对人OCTN2 的 EC50 值为 21 μM。Mildronate (Meldonium) 可诱导长链脂肪酸代谢从线粒体向过氧化物酶体的重定向。

名称

• 中文名: 米屈肼二水合物
• 英文名: Mildronate dihydrate
• 中文别名: 美度铵; 米屈肼
• 英文别名: Diazanium, 2-(2-carboxyethyl)-1,1,1-trimethyl-, inner salt; MET88; Meldonium; 3-(2,2,2-Trimethyldiazan-2-ium-1-yl)propanoate; MFCD00876389; Quaterin; Mildronate; UNII-73H7UDN6EC

物化性质

• 熔点: 85-90ºC
• 分子式: C₆H₁₄N₂O₂
• 分子量: 146.188
• 精确质量: 146.105530
• PSA: 52.16000
• 外观性状: 白色结晶粉末
• 折射率: 1.598
• 储存条件: Refrigerator
• 稳定性: Hygroscopic

生物活性

• 描述: Mildronate (Meldonium) 是一种心血管保护药,可竞争性的抑制 BBOX1 和OCTN2。Mildronate (Meldonium) 对人重组 BBOX 的 IC50 值为 34-62 μM,对人OCTN2 的 EC50 值为 21 μM。Mildronate (Meldonium) 可诱导长链脂肪酸代谢从线粒体向过氧化物酶体的重定向。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
• 靶点:

  IC50: 34-62 μM (human recombinant BBOX). EC50: 21 μM (human OCTN2).

• 参考文献:

  [1]. Dambrova M, et al. Pharmacological effects of meldonium: Biochemical mechanisms and biomarkers of cardiometabolic activity. Pharmacol Res. 2016 Nov;113(Pt B):771-780.

  [2]. Schobersberger W, et al. Story behind meldonium-from pharmacology to performance enhancement: a narrative review. Br J Sports Med. 2017 Jan;51(1):22-25.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : MW0333620 CHEMICAL NAME : Hydrazinium, 2-(2-carboxyethyl)-1,1,1-trimethyl-, hydroxide, inner salt CAS REGISTRY NUMBER : 76144-81-5 LAST UPDATED : 199703 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C6-H14-N2-O2 MOLECULAR WEIGHT : 146.22 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >20 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 12 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory stimulation REFERENCE : EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 18500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 7850 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2105992 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 4430 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : BAXXDU British UK Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #2105992 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Mammal - cat DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 8 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Lungs, Thorax, or Respiration - other changes REFERENCE : EKFMA7 Eksperimental'naya i Klinicheskaya Farmakoterapiya. (Izdatel'stvo Zinantne, Riga, USSR) No.1- 1970- Volume(issue)/page/year: 19,67,1991

安全

• 海关编码: 2928000090

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海关

海关编码	2928000090
中文概述	2928000090 其他肼（联氨）及胲（羟胺）的有机衍生物。监管条件:无。增值税率:17.0%。退税率:9.0%。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
Summary	2928000090 other organic derivatives of hydrazine or of hydroxylamine VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%