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苯扎贝特

苯扎贝特用途

Bezafibrate 是 PPAR 的激动剂,对人和鼠 PPARα,PPARγ 和 PPARδ 的 EC50 分别为 50 μM,60 μM,20 μM 和 90 μM,55 μM,110 μM；Bezafibrate 是一种降血脂剂。

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苯扎贝特名称

[ CAS 号 ]:
41859-67-0

[ 中文名 ]:
苯扎贝特

[ 英文名 ]:
Bezafibrate

[中文别名 ]:

[英文别名 ]:

Difaterol
bezafibric acid
bezafibrato
bezafibratum [INN_la]
CEDUR
Bezalip
MFCD00078970
Bezafibrate
Befizal
bezafibrat

苯扎贝特生物活性

[ 描述 ]:

Bezafibrate 是 PPAR 的激动剂,对人和鼠 PPARα,PPARγ 和 PPARδ 的 EC50 分别为 50 μM,60 μM,20 μM 和 90 μM,55 μM,110 μM；Bezafibrate 是一种降血脂剂。

[ 相关类别 ]:

研究领域 >> 代谢疾病

研究领域 >> 心血管疾病

[ 靶点 ]

hPPARδ:20 μM (EC50)

hPPARα:50 μM (EC50)

hPPARγ:60 μM (EC50)

[体外研究]

苯扎贝特是PPAR的激动剂,对于小鼠PPARα,PPARγ和PPARδ,EC50分别为90μM,55μM,110μM,对于人PPARα,PPARγ和PPARδ分别为50μM,60μM,20μM[1]。苯扎贝特(>200μM)显示出对人视网膜微血管内皮细胞(HRMEC)和人视网膜色素上皮ARPE-19细胞的显着细胞毒性。苯扎贝特(30-100μM)抑制肿瘤坏死因子(TNF)α诱导的炎症因子并调节HRMEC中TNFα诱导的核因子(NF)-κB反式激活。苯扎贝特抑制VEGF诱导的HRMECs迁移,并抑制白细胞介素(IL)-1β诱导的ARPE-19细胞VEGF分泌[2]。

[体内研究]

苯扎贝特(0.5％)显着降低血浆脂质和葡萄糖水平,并增加TallyHo小鼠胰腺中的胰岛面积。苯扎贝特还可以改善能量消耗和代谢灵活性。此外,苯扎贝特可改善脂肪变性,改善脂质成分,增加肝脏线粒体质量[3]。

[细胞实验]

使用CCK-8试剂盒评估细胞活力。将人类视网膜微血管内皮细胞（HRMEC）或ARPE-19细胞以5000个细胞/孔接种在96孔板中含有10％血清的培养基中。孵育24小时后，将培养基用1％FBS血清饥饿6小时，加入CCK-8试剂，并在三个时间点使用酶标仪在450nm处测量所得溶液的吸光度。用苯扎贝特（0,10,50,100,200,500和1000μM）治疗后24,48和72小时[2]。

[动物实验]

TallyHo小鼠在我们的动物设施中繁殖。在该研究中仅使用雄性小鼠，并且小鼠接受标准饮食（SD），其为苯扎贝特组补充0.5％（w / w）苯扎贝特8周。通过异氟醚过量杀死动物，并如下所述制备解剖的组织。所有数据均代表苯扎贝特（或SD）治疗8周后取样，除非另有说明[3]。

[参考文献]

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.

[2]. Usui-Ouchi A, et al. The peroxisome proliferator-activated receptor pan-agonist bezafibrate suppresses microvascular inflammatory responses of retinal endothelial cells and vascular endothelial growth factor production in retinal pigmented epithelial cells. Int Immunopharmacol. 2017 Nov;52:70-76.

[3]. Franko A, et al. Bezafibrate ameliorates diabetes via reduced steatosis and improved hepatic insulin sensitivity in diabetic TallyHo mice. Mol Metab. 2017 Jan 6;6(3):256-266.

[相关活性小分子]

苯扎贝特物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
572.1±45.0 °C at 760 mmHg

[ 熔点 ]:
184 °C

[ 分子式 ]:
C₁₉H₂₀ClNO₄

[ 分子量 ]:
361.819

[ 闪点 ]:
299.8±28.7 °C

[ 精确质量 ]:
361.108093

[ PSA ]:
75.63000

[ LogP ]:
3.46

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±1.7 mmHg at 25°C

[ 折射率 ]:
1.583

[ 储存条件 ]:
Refrigerator

[ 水溶解性 ]:
DMF: soluble

苯扎贝特MSDS

详细MSDS(安全技术说明书)

苯扎贝特毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UE8755000

CHEMICAL NAME :: Propionic acid, 2-(4-(2-((4-chlorobenzoyl)amino)ethyl)phenoxy)-2-meth yl-

CAS REGISTRY NUMBER :: 41859-67-0

LAST UPDATED :: 199806

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C19-H20-Cl-N-O4

MOLECULAR WEIGHT :: 361.85

WISWESSER LINE NOTATION :: QVX1&1&OR D2MVR DG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 514 mg/kg/60D-I

TOXIC EFFECTS :: Peripheral Nerve and Sensation - sensory change involving peripheral nerve

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 309,929,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1326 mg/kg/37W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,371,1993

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1082 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - tumors

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4293,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 505 mg/kg

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

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 15,215,1979

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1580 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Gastrointestinal - tumors

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4293,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 723 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4293,1988

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

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

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 15,215,1979

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1635 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,1226,1995

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - chronic pulmonary edema Gastrointestinal - other changes Liver - other changes

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4337,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 27300 mg/kg/13W-C

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Endocrine - changes in adrenal weight

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4301,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/kg/7D-I

TOXIC EFFECTS :: Liver - changes in liver weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases

REFERENCE :: ARTODN Archives of Toxicology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.32- 1974- Volume(issue)/page/year: 66,327,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 45500 mg/kg/13W-C

TOXIC EFFECTS :: Liver - other changes Kidney, Ureter, Bladder - other changes Blood - normocytic anemia

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4337,1988 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8800 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - sex ratio

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4415,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4415,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/kg

SEX/DURATION :: female 17-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - other neonatal measures or effects

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4433,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 450 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 4 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4433,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3900 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 22,4453,1988

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苯扎贝特安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
1

[ RTECS号 ]:
UE8755000

[ 海关编码 ]:
2924299090

苯扎贝特海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

苯扎贝特文献

Environmental friendly method for urban wastewater monitoring of micropollutants defined in the Directive 2013/39/EU and Decision 2015/495/EU.

J. Chromatogr. A. 1418 , 140-9, (2015)

The fate and removal of organic micropollutants in the environment is a demanding issue evidenced by the recent European policy. This work presents an analytical method for the trace quantification of...

BFCOD activity in fish cell lines and zebrafish embryos and its modulation by chemical ligands of human aryl hydrocarbon and nuclear receptors.

Environ. Sci. Pollut. Res. Int. 22 , 16393-404, (2015)

Assessment of exposure and effect of fish to pharmaceuticals that contaminate aquatic environment is a current major issue in ecotoxicology and there is a need to develop specific biological marker to...

Determination of selected pharmaceuticals in tap water and drinking water treatment plant by high-performance liquid chromatography-triple quadrupole mass spectrometer in Beijing, China.

Environ. Sci. Pollut. Res. Int. 22(3) , 1854-67, (2015)

A simultaneous determination method of 14 multi-class pharmaceuticals using solid-phase extraction (SPE) followed by high-performance liquid chromatography-tandem mass spectrometer (HPLC-MS/MS) was es...

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