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盐酸苯氟雷司

盐酸苯氟雷司用途

Benfluorex hydrochloride (JP-992 hydrochloride) 是一个肝核因子 4α (HNF4α) 激活剂。

盐酸苯氟雷司名称

[ CAS 号 ]:
23642-66-2

[ 中文名 ]:
盐酸苯氟雷司

[ 英文名 ]:
Benfluorex hydrochloride

[中文别名 ]:

盐酸苯氟雷司生物活性

[ 描述 ]:

Benfluorex hydrochloride (JP-992 hydrochloride) 是一个肝核因子 4α (HNF4α) 激活剂。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 其他 >> 其他

研究领域 >> 代谢疾病

[ 靶点 ]

HNF4α[1]

[体外研究]

当GFP阳性细胞数量增加时,盐酸苯氟醚持续激活胰岛素启动子活性。盐酸苯氟醚以剂量反应方式增加GFP阳性细胞数,增加内源性胰岛素mRNA水平。与HNF4α激活剂一致,盐酸苯氟醚刺激HNF4α的表达。盐酸苯氟醚改变了HNF4α蛋白酶的敏感性,而非活性对照化合物则没有[1]。盐酸苯氟醚以浓度依赖的方式减少油酸盐合成酸溶性产物和酮体,而盐酸苯氟醚显著增加了柠檬酸循环中14CO2的生成。盐酸苯氟醚以剂量依赖的方式抑制乳酸/丙酮酸的糖异生率(10/1nm)[2]。

[激酶实验]

以20μM或40μM的浓度用二甲基亚砜或盐酸苯氟醚处理HepG2细胞16小时。提取细胞总蛋白，用BCA蛋白测定。每一个样品被分成两个小份进行蛋白水解，不含或含有枯草杆菌肽。20微克细胞裂解物与或不与蛋白酶（20 ng/mL枯草杆菌素）在室温下孵育35分钟。然后用一级抗HNF4α多克隆抗体（1:1000稀释）和二级HRP结合抗山羊IgG（1:2000稀释）进行Western blot，用化学发光ECL试剂盒检测。

[细胞实验]

肝细胞用0.025%胶原酶原位灌注分离。肝细胞（1至2×106细胞/mL）在37°C下于2 mL含氧（O2:CO2；95:5）Krebs-Henseleit碳酸氢盐缓冲液（pH 7.4）中在旋转摇动水浴中孵育1 h。盐酸苯氟醚溶于二甲基亚砜中，以0.1或1nm的最终浓度（10μL）加入培养基中[2]。

[参考文献]

[1]. Lee SH, et al. Identification of alverine and benfluorex as HNF4α activators. ACS Chem Biol. 2013 Aug 16;8(8):1730-6.

[2]. Kohl C, et al. Effects of benfluorex on fatty acid and glucose metabolism in isolated rat hepatocytes: from metabolic fluxes to gene expression. Diabetes. 2002 Aug;51(8):2363-8.

盐酸苯氟雷司物理化学性质

[ 密度 ]:
1.183g/cm3

[ 沸点 ]:
420.5ºC at 760mmHg

[ 熔点 ]:
158-159?C

[ 分子式 ]:
C₁₉H₂₁ClF₃NO₂

[ 分子量 ]:
387.82400

[ 闪点 ]:
208.1ºC

[ 精确质量 ]:
387.12100

[ PSA ]:
38.33000

[ LogP ]:
5.27590

[ 蒸汽压 ]:
2.81E-07mmHg at 25°C

[ 储存条件 ]:
Refrigerator

盐酸苯氟雷司MSDS

详细MSDS(安全技术说明书)

盐酸苯氟雷司毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KL8526000

CHEMICAL NAME :: Ethanol, 2-((1-methyl-2-(3-(trifluoromethyl)phenyl)ethyl)amino )-, benzoate (ester), hydrochloride

CAS REGISTRY NUMBER :: 23642-66-2

LAST UPDATED :: 199509

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C19-H20-F3-N-O2.Cl-H

MOLECULAR WEIGHT :: 387.86

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 :: 108 mg/kg

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

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 195,252,1972

盐酸苯氟雷司安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;

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

[ WGK德国 ]:
2

[ RTECS号 ]:
KL8275000

盐酸苯氟雷司文献

[Benfluorex and valvular heart disease].

Presse Med. 40(11) , 1008-16, (2011)

Benfluorex is responsible of restrictive organic valvular regurgitations via one of its metabolites, the norfenfluramine. It has been withdrawn from the european market in June 2010. In France, about ...

[About the settlement of litigations concerning the harm caused by benfluorex (Mediator®)].

Presse Med. 42(4 Pt 1) , 411-8, (2013)

Since September 1st 2011, the National Bureau for Compensation of Medical Accidents represents a unique portal for out-of-court settlement of litigations concerning the harm caused by benfluorex. In D...

[Reform Act on safety of drug and health products in France: announcement effect, strengthening or upheaval?].

Therapie. 67(1) , 1-10, (2012)

In France, the Médiator(®) scandal and the trauma it has created, are the source of Law n° 2011-2012 of 29 December 2011 on strengthening safety of drug and health products, intended by the Ministry o...

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