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寡霉素A

寡霉素A用途

Oligomycin A 是从链霉菌属中得到的一种线粒体 F0F1-ATPase 抑制剂,Ki 值为 1 μM；Oligomycin A 具有抗真菌的功能。

寡霉素A名称

[ CAS 号 ]:
579-13-5

[ 中文名 ]:
寡霉素A

[ 英文名 ]:
Oligomycin A

[中文别名 ]:

[英文别名 ]:

Oligomycin A
MCH 32
MFCD00065705
OLIGOMYCIN,STREPTOMYCES DIASTATOCHROMOGENES
EINECS 209-473-3
OLIGOMYCIN A,STREPTOMYCES DIASTATOCHROMOGENES

寡霉素A生物活性

[ 描述 ]:

Oligomycin A 是从链霉菌属中得到的一种线粒体 F0F1-ATPase 抑制剂,Ki 值为 1 μM；Oligomycin A 具有抗真菌的功能。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> ATP合成酶

研究领域 >> 癌症

研究领域 >> 感染

天然产物 >> 其他

[ 靶点 ]

Ki: 1 μM (F0F1-ATPase)[1]

[体外研究]

Oligomycin A是线粒体F0F1-ATP酶抑制剂,Ki为1μM。 Oligomycin A对NCI-60细胞系显示出细胞毒性,GI50为10nM。 Oligomycin A也抑制Triton X-100溶解的ATP酶的活性,Ki为0.1μM。此外,Oligomycin A具有抗真菌活性[1]。 Oligomycin A(2.4μM)抑制精子实现可行的体外获能(IVC)的能力,并抑制黄体酮诱导的体外顶体胞吐(IVAE)以及伴随的O2消耗和ATP水平峰[2]。

[细胞实验]

将药物（Oligomycin A等）稀释液一式三份加入96孔板中的单层或悬浮细胞中不同时间。然后将MTT加入到孔中，终浓度为0.5mg / mL。在制备还原的MTT晶体后除去上清液。将晶体完全溶解在40mM HCl的异丙醇溶液中。将板在595nm的酶标仪上扫描[1]。

[参考文献]

[1]. Salomon AR, et al. Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase. Chem Biol. 2001 Jan;8(1):71-80.

[2]. Ramió-Lluch L, et al. Oligomycin A-induced inhibition of mitochondrial ATP-synthase activity suppresses boar sperm motility and in vitro capacitation achievement without modifying overall sperm energy levels. Reprod Fertil Dev. 2014;26(6):883-97.

[相关活性小分子]

BTB06584

寡霉素A物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
886.3±65.0 °C at 760 mmHg

[ 熔点 ]:
150-151ºC

[ 分子式 ]:
C₄₅H₇₄O₁₁

[ 分子量 ]:
791.063

[ 闪点 ]:
252.0±27.8 °C

[ 精确质量 ]:
790.523132

[ PSA ]:
180.05000

[ LogP ]:
6.17

[ 外观性状 ]:
white to off-white

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.543

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
Soluble in DMSO, ethanol or acetone

寡霉素A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RK3328000

CHEMICAL NAME :: Oligomycin A

CAS REGISTRY NUMBER :: 579-13-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C45-H74-O11

MOLECULAR WEIGHT :: 791.19

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1500 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JACSAT Journal of the American Chemical Society. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1879- Volume(issue)/page/year: 80,6092,1958

寡霉素A安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 危害码 (欧洲) ]:
Xn,T

[ 风险声明 (欧洲) ]:
22-68/20/21/22-20/21/22

[ 安全声明 (欧洲) ]:
36/37

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
RK3325000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
29419090

寡霉素A文献

Modulators of hepatic lipoprotein metabolism identified in a search for small-molecule inducers of tribbles pseudokinase 1 expression.

PLoS ONE 10 , e0120295, (2015)

Recent genome wide association studies have linked tribbles pseudokinase 1 (TRIB1) to the risk of coronary artery disease (CAD). Based on the observations that increased expression of TRIB1 reduces se...

Functional characterization of CYP107W1 from Streptomyces avermitilis and biosynthesis of macrolide oligomycin A.

Arch. Biochem. Biophys. 575 , 1-7, (2015)

Streptomyces avermitilis contains 33 cytochrome P450 genes in its genome, many of which play important roles in the biosynthesis process of antimicrobial agents. Here, we characterized the biochemical...

Moles of a Substance per Cell Is a Highly Informative Dosing Metric in Cell Culture.

PLoS ONE 10 , e0132572, (2015)

The biological consequences upon exposure of cells in culture to a dose of xenobiotic are not only dependent on biological variables, but also the physical aspects of experiments e.g. cell number and ...

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