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帕苯达唑

帕苯达唑用途

Parbendazole 是一种有效的 microtubule 重组抑制剂,能够破坏微管蛋白,EC50 值为 8.79 nM,具有广谱的驱虫作用。
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帕苯达唑名称

[ CAS 号 ]:
14255-87-9

[ 中文名 ]:
帕苯达唑

[ 英文名 ]:
Parbendazole

[中文别名 ]:

[英文别名 ]:

帕苯达唑生物活性

[ 描述 ]:

Parbendazole 是一种有效的 microtubule 重组抑制剂,能够破坏微管蛋白,EC50 值为 8.79 nM,具有广谱的驱虫作用。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白
信号通路 >> 细胞骨架 >> 微管/微管蛋白
研究领域 >> 感染

[ 靶点 ]

EC50: 8.79 nM (tubulin)[1]


[体外研究]

Parbendazole是一种微管蛋白去稳定剂,EC50为8.79 nM,可诱导DNA损伤[1]。帕潘哒唑(2-10μM)剂量依赖性地抑制微管组装,IC50为3μM。 Parbendazole(2-20μM)处理的细胞显示Vero细胞中完全没有微管[2]。 Parbendazole(高达10μM)抑制CLd-AX myxamoebae的生长。帕潘哒唑(2-5μM)有效抑制从野生型粘液瘤中纯化的微管蛋白[3]。

[激酶实验]

纯的微管蛋白通过体外装配和拆卸的2个循环从绵羊脑中获得。在即将使用之前,将蛋白质以130000g离心30分钟以除去任何聚集物。其在0.025M管式缓冲液,0-5mM EGTA,0-25mM Mg 2 SO 4> 0.1mM GTP中以0-2mg / mL的蛋白质浓度使用。使用0.1μM和4μM之间的帕苯达唑浓度和2%(v / v)DMF(二甲基甲酰胺)作为载体,通过平衡透析测定药物结合。通过在26℃下持续搅拌2小时来实现平衡,使用牛血清白蛋白作为标准。在25-200B液体闪烁计数器[2]中,在PCS中计数200μL等分试样。

[细胞实验]

将来自猴肾的已建立的细胞系Vero细胞接种在补充有10%(v / v)胎牛血清的DMEM中,置于多孔培养皿中的玻璃盖玻片上。使它们沉降,并在37℃的潮湿气氛中铺展2-5小时。此后,将培养基更换为含有2,10或20μM帕苯达唑和1%(v / v)DMSO对照的DMEM,其含有1%(v / v)DMSO或不添加[2]。

[参考文献]

[1]. Lo YC, et al. Computational Cell Cycle Profiling of Cancer Cells for Prioritizing FDA-Approved Drugs with Repurposing Potential. Sci Rep. 2017 Sep 12;7(1):11261.

[2]. Lo YC, et al. Computational Cell Cycle Profiling of Cancer Cells for Prioritizing FDA-Approved Drugs with Repurposing Potential. Sci Rep. 2017 Sep 12;7(1):11261.

[3]. Havercroft JC, et al. Binding of parbendazole to tubulin and its influence on microtubules in tissue-culture cells as revealed by immunofluorescence microscopy. J Cell Sci. 1981 Jun;49:195-204.

[4]. Havercroft JC, et al. Binding of parbendazole to tubulin and its influence on microtubules in tissue-culture cells as revealed by immunofluorescence microscopy. J Cell Sci. 1981 Jun;49:195-204.

[5]. Foster KE, et al. A mutant beta-tubulin confers resistance to the action of benzimidazole-carbamate microtubule inhibitors both in vivo and in vitro. Eur J Biochem. 1987 Mar 16;163(3):449-55.

[6]. Foster KE, et al. A mutant beta-tubulin confers resistance to the action of benzimidazole-carbamate microtubule inhibitors both in vivo and in vitro. Eur J Biochem. 1987 Mar 16;163(3):449-55.


[相关活性小分子]

诺考达唑 | 一甲基澳瑞他汀E | VcMMAE | Mertansine(DM1化合物) | 甲磺酸艾瑞布林 | 埃博霉素 | 酒石酸长春瑞滨 | 埃博霉素B | McMMAF | MMAF盐酸盐 | 伊沙匹隆 | N,BETA,BETA-三甲基-L-苯基丙氨酰基-N-[(1S,2E)-3-羧基-1-(1-甲基乙基)-2-丁烯基]-N,3-二甲基-L-缬氨酰胺 | 雌莫司汀磷酸钠 | 安丝菌素P3 | 康普瑞汀磷酸二钠

帕苯达唑物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 熔点 ]:
255-257°C

[ 分子式 ]:
C13H17N3O2

[ 分子量 ]:
247.293

[ 精确质量 ]:
247.132080

[ PSA ]:
67.01000

[ LogP ]:
3.57

[ 外观性状 ]:
固体

[ 折射率 ]:
1.632

[ 储存条件 ]:
库房通风低温干燥

[ 稳定性 ]:
Stable. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
<0.1 g/100 mL at 18 ºC

帕苯达唑MSDS

帕苯达唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DD6495000
CHEMICAL NAME :
2-Benzimidazolecarbamic acid, 5-butyl-, methyl ester
CAS REGISTRY NUMBER :
14255-87-9
LAST UPDATED :
199306
DATA ITEMS CITED :
23
MOLECULAR FORMULA :
C13-H17-N3-O2
MOLECULAR WEIGHT :
247.33
WISWESSER LINE NOTATION :
T56 BM DNJ CMVO1 G4

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 :
>40 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1700 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Bird - chicken
DOSE/DURATION :
>40 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - domestic
DOSE/DURATION :
660 mg/kg
TOXIC EFFECTS :
Gastrointestinal - ulceration or bleeding from stomach
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Mammal - cattle
DOSE/DURATION :
>1200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Mammal - cattle
DOSE/DURATION :
450 mg/kg/6D-I
TOXIC EFFECTS :
Gastrointestinal - other changes
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1200 mg/kg
SEX/DURATION :
female 7-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - gastrointestinal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
80 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
80 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
150 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
80 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
4 gm/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - respiratory system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
90 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
400 mg/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
10 gm/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
16 gm/kg
SEX/DURATION :
female 6-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - urogenital system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
130 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - abortion Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
780 mg/kg
SEX/DURATION :
female 6-18 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
60 mg/kg
SEX/DURATION :
female 21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - physical
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
30 mg/kg
SEX/DURATION :
female 12 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - other measures of fertility

MUTATION DATA

TYPE OF TEST :
Mutation test systems - not otherwise specified
TEST SYSTEM :
Mammal - domestic Leukocyte
DOSE/DURATION :
1 mg/L
REFERENCE :
THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 31,505,1976
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帕苯达唑安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R20/21/22:Harmful by inhalation, in contact with skin and if swallowed . R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36/37/39

[ 危险品运输编码 ]:
2811

[ RTECS号 ]:
DD6495000

[ 海关编码 ]:
2933990090

帕苯达唑海关

[ 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%

帕苯达唑文献

Microtubule disruption synergizes with oncolytic virotherapy by inhibiting interferon translation and potentiating bystander killing.

Nat. Commun. 6 , 6410, (2015)

In this study, we show that several microtubule-destabilizing agents used for decades for treatment of cancer and other diseases also sensitize cancer cells to oncolytic rhabdoviruses and improve ther...

Development and validation of an ultra high performance liquid chromatography tandem mass spectrometry method for simultaneous determination of sulfonamides, quinolones and benzimidazoles in bovine milk.

J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 962 , 20-9, (2014)

A simple, sensitive and reliable analytical method was developed for the simultaneous determination of 38 veterinary drugs (18 sulfonamides, 11 quinolones and 9 benzimidazoles) and 8 metabolites of be...

Controlled tests of activity of several antiparasitic compounds against natural infections of Haemonchus contortus and other helminths in lambs from a flock established in 1962.

Am. J. Vet. Res. 54(3) , 406-10, (1993)

Antiparasitic activity of several compounds was evaluated over a long period (about 25 years) in the same flock of sheep. Haemonchus contortus was of special interest, including its relation to drug r...


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产品详情:5-丁基-2-苯并咪唑氨基甲酸甲酯


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¥1166.0/100mg ¥4636.0/1g ¥1856.0/250mg ¥12166.0/5g

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¥需询单/1g

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产品详情:Parbendazole


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产品详情:[Perfemiker]Parbendazole,≥98%


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产品详情:Parbendazole


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相关化合物

【帕苯达唑】化源网提供帕苯达唑CAS号14255-87-9,帕苯达唑MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询帕苯达唑上化源网,专业又轻松。>>电脑版:帕苯达唑

标题:帕苯达唑_MSDS_用途_密度_帕苯达唑CAS号【14255-87-9】_化源网 地址:https://m.chemsrc.com/mip/cas/14255-87-9_826632.html