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刀豆素A

刀豆素A用途

Concanamycin A (Antibiotic X 4357B; Concanamycin; X 4357B) 是一种大环内酯类抗生素,也是特异的空泡状 H+- ATP 酶 (V-ATPase) 抑制剂。

刀豆素A名称

[ CAS 号 ]:
80890-47-7

[ 中文名 ]:
伴刀球霉素A

[ 英文名 ]:
concanamycin A

[中文别名 ]:

刀豆素A

[英文别名 ]:

antibioticx4357b
S-45A
MFCD00210037
Antibiotic A661I
FOLIMYCIN,STREPTOMYCES SP
A661-I
FOLIMYCIN
Antibiotic S-45A
x4357b
CONCANAMYCIN A

刀豆素A生物活性

[ 描述 ]:

Concanamycin A (Antibiotic X 4357B; Concanamycin; X 4357B) 是一种大环内酯类抗生素,也是特异的空泡状 H+- ATP 酶 (V-ATPase) 抑制剂。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 跨膜转运 >> 质子泵

[ 靶点 ]

Vacuolar type H+-ATPase[1]

[参考文献]

[1]. Togashi K, et al. Concanamycin A, a vacuolar type H(+)-ATPase inhibitor, induces cell death in activated CD8(+) CTL. Cytotechnology. 1997 Nov;25(1-3):127-35.

[2]. Eswarappa SM, et al. Folimycin (concanamycin A) inhibits LPS-induced nitric oxide production and reduces surface localization of TLR4 in murine macrophages. Innate Immun. 2008 Feb;14(1):13-24.

刀豆素A物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
966.4±65.0 °C at 760 mmHg

[ 熔点 ]:
179-180℃ (dichloromethane ethanol )

[ 分子式 ]:
C₄₆H₇₅NO₁₄

[ 分子量 ]:
866.09

[ 闪点 ]:
538.3±34.3 °C

[ 精确质量 ]:
865.518738

[ PSA ]:
225.92000

[ LogP ]:
3.88

[ 蒸汽压 ]:
0.0±0.6 mmHg at 25°C

[ 折射率 ]:
1.555

[ 储存条件 ]:
−20°C

刀豆素A毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CB9732000

CHEMICAL NAME :: Antibiotic X 4357 B

CAS REGISTRY NUMBER :: 80890-47-7

LAST UPDATED :: 199712

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C46-H75-N-O14

MOLECULAR WEIGHT :: 866.22

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 :: 21 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4076802

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2450 ug/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4076802

刀豆素A安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H300 + H310 + H330-H319

[ 警示性声明 ]:
P260-P264-P280-P284-P301 + P310-P302 + P350

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T+

[ 风险声明 (欧洲) ]:
26/27/28-36

[ 安全声明 (欧洲) ]:
26-36/37/39-45

[ 危险品运输编码 ]:
UN 3462 6.1/PG 2

[ WGK德国 ]:
3

[ RTECS号 ]:
CB9732000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

刀豆素A文献

2,4-Dichlorophenoxyacetic acid alters intracellular pH and ion transport in the outer mantle epithelium of the bivalve Anodonta cygnea.

Aquat. Toxicol. 154 , 12-8, (2014)

Bivalve molluscs, due to their sedentary mode of life and filter-feeding behavior, are very susceptible to pollutant bioaccumulation and used as sentinel organisms in the assessment of environment pol...

Inhibitors of vacuolar ATPase proton pumps inhibit human prostate cancer cell invasion and prostate-specific antigen expression and secretion.

Int. J. Cancer 132(2) , E1-10, (2013)

Vacuolar ATPases (V-ATPases) comprise specialized and ubiquitously distributed pumps that acidify intracellular compartments and energize membranes. To gain new insights into the roles of V-ATPases in...

Functional characterization of the Plasmodium falciparum chloroquine-resistance transporter (PfCRT) in transformed Dictyostelium discoideum vesicles.

PLoS ONE 7(6) , e39569, (2012)

Chloroquine (CQ)-resistant Plasmodium falciparum malaria has been a global health catastrophe, yet much about the CQ resistance (CQR) mechanism remains unclear. Hallmarks of the CQR phenotype include ...

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