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草多索

草多索用途

Endothall(Endothal)是一种蛋白质磷酸酶2A(PP2A)抑制剂,PP2A和PP1的IC50分别为90 nM和5µM。它可以用作除草剂。内皮素在癌症化疗中也很有用[1]。

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草多索名称

[ CAS 号 ]:
145-73-3

[ 中文名 ]:
茵多酸

[ 英文名 ]:
Endothall

[中文别名 ]:

[英文别名 ]:

aquatholplus
7-oxa-bicyclo[2.2.1]heptane-2,3-dicarboxylic acid
7-Oxabicyclo[2.2.1]heptane-2,3-dicarboxylicacid
Aquathol
Hydout
7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid
ENDOTHAL
ACCELERATE
MFCD00137362
Niagrathal

草多索生物活性

[ 描述 ]:

Endothall(Endothal)是一种蛋白质磷酸酶2A(PP2A)抑制剂,PP2A和PP1的IC50分别为90 nM和5µM。它可以用作除草剂。内皮素在癌症化疗中也很有用[1]。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸酶

[体外研究]

内毒素是一种有机酸,是斑蝥素毒性最小的结构类似物,仍然抑制PP2A[2]。内皮素优先抑制肝细胞癌(HCC)的生长,这些新的大鼠肝细胞癌细胞株可能有助于PP2A抑制剂的进一步生化和药理学研究,以及测试肝细胞癌的新治疗形式。HR-2、HR-3、HR-4和Zajdela肝细胞癌对内毒素最敏感(IC50分别为1.7、1.2、0.9和1.7µg/mL),而新生大鼠肝细胞在原代培养(IC50=6.2µg/mL)、大鼠DHD/K12结肠癌细胞(IC50=3.6µg/mL)中呈指数增长,或人类HT-29结肠癌细胞(IC50=4.9微克/毫升)的敏感性较低[2]。与正常肝细胞或结肠癌相比,内毒素对培养的肝癌细胞系的生长抑制作用更强,导致有丝分裂停止,随后导致细胞死亡。内毒素会在G2/M中引起剂量和时间依赖性细胞停滞[2]。内毒素(3µg/mL)抑制G2/M时的细胞周期和随后的凋亡细胞死亡[2]。

[体内研究]

在小鼠中,内毒素血症表现出14 mg/kg的急性LD50[2]。

[参考文献]

[1]. Janetti R Signorelli, et al. Protein phosphatases decrease their activity during capacitation: a new requirement for this event. PLoS One. 2013 Dec 2;8(12):e81286.

[2]. J P Thièry, et al. Hepatocellular carcinoma cell lines from diethylnitrosamine phenobarbital-treated rats. Characterization and sensitivity to endothall, a protein serine/threonine phosphatase-2A inhibitor. Hepatology. 1999 May;29(5):1406-17.

草多索物理化学性质

[ 密度 ]:
1.431

[ 沸点 ]:
350ºC(e)

[ 熔点 ]:
144ºC

[ 分子式 ]:
C₈H₁₀O₅

[ 分子量 ]:
186.16200

[ 闪点 ]:
190.5ºC

[ 精确质量 ]:
186.05300

[ PSA ]:
83.83000

[ 蒸汽压 ]:
2.88E-09mmHg at 25°C

[ 折射率 ]:
1.568

草多索MSDS

详细MSDS(安全技术说明书)

草多索毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RN7875000

CHEMICAL NAME :: 7-Oxabicyclo(2.2.1)heptane-2,3-dicarboxylic acid

CAS REGISTRY NUMBER :: 145-73-3

LAST UPDATED :: 199701

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C8-H10-O5

MOLECULAR WEIGHT :: 186.18

WISWESSER LINE NOTATION :: T55 A AOTJ CVQ DVQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 571 uL/kg

TOXIC EFFECTS :: Cardiac - other changes Kidney, Ureter, Bladder - urine volume decreased Nutritional and Gross Metabolic - metabolic acidosis

REFERENCE :: AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 6,509,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38 mg/kg

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

REFERENCE :: PCOC** Pesticide Chemicals Official Compendium, Association of the American Pesticide Control Officials, Inc., 1966. (Topeka, KS) Volume(issue)/page/year: -,471,1966

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

ROUTE OF EXPOSURE :: Administration onto the skin

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 7,299,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14 mg/kg

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

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 35,823,1987 *** U.S. STANDARDS AND REGULATIONS *** EPA FIFRA 1988 PESTICIDE SUBJECT TO REGISTRATION OR RE-REGISTRATION FEREAC Federal Register. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) V.1- 1936- Volume(issue)/page/year: 54,7740,1989

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草多索安全信息

[ 危害码 (欧洲) ]:
T

[ 风险声明 (欧洲) ]:
21-25-36/37/38

[ 安全声明 (欧洲) ]:
S45;S36/S37/S39

[ 危险品运输编码 ]:
UN 2811 6.1/PG 2

[ WGK德国 ]:
1

[ RTECS号 ]:
RN7875000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
2932190013

草多索合成路线

详细合成路线

草多索上下游产品

草多索上游产品

草多索下游产品

草多索海关

[ 海关编码 ]: 2932190013

[ 中文概述 ]:
2932190013 呋氧草醚,环庚草醚,呋草酮等〔包括茵多酸〕。监管条件:S(进出口农药登记证明)。增值税率:17.0%。退税率:9.0%。最低关税:6.5%。普通关税:20.0%

[ Summary ]:
2932190013 7-oxabicyclo[2.2.1]heptane-2,3-dicarboxylic acid。supervision conditions:s(import or export registration certificate for pesticides)。VAT:17.0%。tax rebate rate:9.0%。MFN tarrif:6.5%。general tariff:20.0%

草多索