米屈肼

米屈肼用途

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。

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米屈肼名称

[ CAS 号 ]:
76144-81-5

[ 中文名 ]:
米屈肼二水合物

[ 英文名 ]:
Mildronate

[中文别名 ]:

[英文别名 ]:

MET88
Meldonium
3-(2,2,2-Trimethyldiazan-2-ium-1-yl)propanoate
MFCD00876389
Quaterin
Mildronate
UNII-73H7UDN6EC

米屈肼生物活性

[ 描述 ]:

[ 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.

米屈肼物理化学性质

[ 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

米屈肼毒性和生态

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

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米屈肼安全信息

[ 海关编码 ]:
2928000090

米屈肼上下游产品

米屈肼上游产品

米屈肼下游产品

米屈肼海关

[ 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%

米屈肼