阿西莫司

阿西莫司用途

Acipimox是烟酸衍生物,可降血脂。

阿西莫司作用

1.作用于肝脏和脂肪组织，抑制脂肪组织的脂解作用，从而使血浆总胆固醇、甘油三酯、低密度脂蛋白、极低密度脂蛋白降低。
2.增加血浆中高密度脂蛋白，有利于胆固醇的转运和清除。
3.增加肝糖原合成，使血糖水平降低。本药可作为治疗各种高脂血症的首选降脂药物，尤其适用于糖尿病伴高脂血症者。

阿西莫司名称

[ CAS 号 ]:
51037-30-0

[ 中文名 ]:
阿西莫司

[ 英文名 ]:
Acipimox

[中文别名 ]:

[英文别名 ]:

5-methyl-2-pyrazinoic-4-oxide
2-Pyrazinecarboxylic acid, 5-methyl-, 4-oxide
5-Carboxy-2-methylpyrazine 1-oxide
5-methyl-4-oxy-pyrazine-2-carboxylic acid
5-methylpyrazine-2-carboxylic acid 4-oxide
2-carboxy-5-methylpyrazine 4-oxide
Acipimox
K-9321
Olbetam
5-Methylpyrazinecarboxylic acid 4-oxide

阿西莫司生物活性

[ 描述 ]:

Acipimox是烟酸衍生物,可降血脂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

天然产物 >> 生物碱

研究领域 >> 心血管疾病

[参考文献]

[1]. http://en.wikipedia.org/wiki/Acipimox

[相关活性小分子]

阿西莫司物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
539.0±45.0 °C at 760 mmHg

[ 熔点 ]:
177-180 °C

[ 分子式 ]:
C₆H₆N₂O₃

[ 分子量 ]:
154.123

[ 闪点 ]:
279.8±28.7 °C

[ 精确质量 ]:
154.037842

[ PSA ]:
75.65000

[ LogP ]:
-1.38

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.608

[ 储存条件 ]:
2-8°C

阿西莫司MSDS

阿西莫司毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ2453000

CHEMICAL NAME :: 2-Pyrazinecarboxylic acid, 5-methyl-, 4-oxide

CAS REGISTRY NUMBER :: 51037-30-0

BEILSTEIN REFERENCE NO. :: 0777471

LAST UPDATED :: 199710

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C6-H6-N2-O3

MOLECULAR WEIGHT :: 154.14

WISWESSER LINE NOTATION :: T6N DNJ AO B1 EVQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3500 mg/kg

TOXIC EFFECTS :: Biochemical - Metabolism (Intermediary) - lipids including transport

REFERENCE :: EJMCA5 European Journal of Medicinal Chemistry--Chimie Therapeutique. (Editions Scientifiques Elsevier, 29 rue Buffon, F-75005, Paris, France) V.9- 1974- Volume(issue)/page/year: 15,157,1980

阿西莫司安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H319

[ 警示性声明 ]:
P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36

[ 安全声明 (欧洲) ]:
S26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
UQ2453000

[ 海关编码 ]:
2942000000

阿西莫司合成路线

阿西莫司上下游产品

阿西莫司上游产品

阿西莫司下游产品

阿西莫司制备

在冷却和搅拌下，往78g马来酸酐溶于60ml氯仿的溶液中，加入40ml30%的过氧化氢。2h后再加入4.8g的5-甲基吡嗪-2-羧酸，在0-5℃保持2d。滤去马来酸。浓缩至剩微小体积，加入乙酸乙酯，过滤可得1.1g的阿西莫司，熔点178-180℃。

阿西莫司海关

[ 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%

阿西莫司文献

Kinetics and utilization of lipid sources during acute exercise and acipimox.

Am. J. Physiol. Endocrinol. Metab. 307(2) , E199-208, (2014)

Overweight is associated with abnormalities of lipid metabolism, many of which are reversed by exercise. We investigated the impact of experimental antilipolysis and acute exercise on lipid kinetics a...

The lowering of hepatic fatty acid uptake improves liver function and insulin sensitivity without affecting hepatic fat content in humans.

Am. J. Physiol. Endocrinol. Metab. 295(2) , E413-9, (2008)

Lipolysis may regulate liver free fatty acid (FFA) uptake and triglyceride accumulation; both are potential causes of insulin resistance and liver damage. We evaluated whether 1) systemic FFA release ...

ECG-triggered 18F-fluorodeoxyglucose positron emission tomography imaging of the rat heart is dramatically enhanced by acipimox.

Eur. J. Nucl. Med. Mol. Imaging 37(9) , 1745-50, (2010)

18F-Fluorodeoxyglucose (FDG) imaging, provided by current positron emission tomography (PET) systems dedicated to small animals,might provide a precise functional assessment of the left ventricle (LV)...

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