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盐酸苯乙双胍

盐酸苯乙双胍用途

Phenformin hydrochloride 是一种双胍类的抗糖尿病药,能够使 AMPK 活化。

盐酸苯乙双胍名称

[ CAS 号 ]:
834-28-6

[ 中文名 ]:
盐酸苯乙福明

[ 英文名 ]:
Phenformin (hydrochloride)

[中文别名 ]:

[英文别名 ]:

Phenformin hydrochloride
Phenformini Hydrochloride
Insora
meltrol
phenforminhclno.9113
Glucopostin
Phenformine HCL
dbi-td
β-PEBG HCl
DBI monohydrochloride

盐酸苯乙双胍生物活性

[ 描述 ]:

Phenformin hydrochloride 是一种双胍类的抗糖尿病药,能够使 AMPK 活化。

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> AMPK

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AMPK

研究领域 >> 癌症

[ 靶点 ]

AMPK

[体外研究]

苯乙双胍刺激AMPKalpha1和AMPKalpha2的磷酸化和活化而不改变LKB1活性[1]。苯乙双胍增加分离心脏的AMPK活性和磷酸化,AMPK活性的增加总是先于细胞溶质[AMP]增加并与其相关[2]。苯乙双胍是一种比二甲双胍更有效的线粒体复合物I抑制剂50倍。苯乙双胍在LKB1缺陷的NSCLC细胞系中强烈诱导细胞凋亡。 2mM的苯乙双胍类似地诱导AMPK信号传导,如P-AMPK和P-Raptor水平增加所示。苯乙双胍诱导较高水平的细胞应激,引发P-Ser51eIF2α及其下游靶CHOP的诱导,以及后期细胞凋亡的标志物。在长期治疗后,苯乙双胍诱导KLluc小鼠的存活率和治疗反应显着增加[3]。苯乙双胍和AICAR以剂量依赖的方式增加H441细胞中的AMPK活性,分别在5-10mm和2mm处刺激激酶。与对照组相比,苯乙双胍显着降低H441单层的基础离子转运(以短路电流测量)约50％。与对照相比,苯乙双胍和AICAR显着降低阿米洛利敏感的跨上皮Na +转运。苯乙双胍和AICAR通过一种途径抑制阿米洛利敏感的Na +转运穿过H441细胞,该途径包括激活AMPK和通过ENaC抑制顶端Na +进入和通过Na +,K + -ATP酶抑制基底外Na +挤压[4]。苯乙双胍治疗的大鼠显示出血胰岛素水平降低的趋势(放射免疫测定)[5]。

[体内研究]

苯乙双胍增加正常肺以及小鼠肺肿瘤中P-eIF2α及其靶BiP/Grp78的水平[3]。

[激酶实验]

使用Dagher等人的方法测量总AMPK活性。在重悬的沉淀中定量AMPK活性，如将来自[γ-32P] ATP（10GBq / mmol）的32P掺入具有AMPK特异性靶序列SAMS肽的合成肽中。使用液体闪烁计数器测量放射性。使用Bradford方法测定含有重悬的（NH 4）2 SO 4沉淀的溶液中的蛋白质含量。

[参考文献]

[1]. Sakamoto K, et al. Activity of LKB1 and AMPK-related kinases in skeletal muscle: effects of contraction, phenformin, and AICAR. Am J Physiol Endocrinol Metab.?2004 Aug;287(2):E310-7.

[2]. Zhang L, et al. Metformin and phenformin activate AMP-activated protein kinase in the heart by increasing cytosolic AMP concentration. Am J Physiol Heart Circ Physiol. 2007 Jul;293(1):H457-66.

[3]. Moreira AL, et al. Thalidomide exerts its inhibitory action on tumor necrosis factor alpha by enhancing mRNA degradation. J Exp Med. 1993 Jun 1;177(6):1675-80.

[4]. Woollhead AM, et al. Phenformin and 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) activation of AMP-activated protein kinase inhibits transepithelial Na+ transport across H441 lung cells. J Physiol. 2005 Aug 1;566(Pt 3):781-92. Epub 2005

[5]. Dilman VM, et al. Inhibition of DMBA-induced carcinogenesis by phenformin in the mammary gland of rats. Arch Geschwulstforsch. 1978;48(1):1-8.

[相关活性小分子]

盐酸苯乙双胍物理化学性质

[ 密度 ]:
1.24 g/cm3

[ 沸点 ]:
413.7ºC at 760 mmHg

[ 熔点 ]:
175-178ºC

[ 分子式 ]:
C₁₀H₁₆ClN₅

[ 分子量 ]:
241.721

[ 闪点 ]:
204ºC

[ 精确质量 ]:
241.109421

[ PSA ]:
97.78000

[ LogP ]:
2.72010

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
>=10 g/100 mL at 21 ºC

盐酸苯乙双胍毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DU2200000

CHEMICAL NAME :: Biguanide, 1-phenethyl-, monohydrochloride

CAS REGISTRY NUMBER :: 834-28-6

LAST UPDATED :: 199706

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C10-H15-N5.Cl-H

MOLECULAR WEIGHT :: 241.76

WISWESSER LINE NOTATION :: MUYZMYUM&M2R &GH

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 :: 938 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 140 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 :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17500 ug/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 407 mg/kg

TOXIC EFFECTS :: Endocrine - hypoglycemia

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 150 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 200 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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17800 ug/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 - guinea pig

DOSE/DURATION :: 47 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 19 mg/kg

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

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Rodent - rat Liver

DOSE/DURATION :: 1 mmol/L

REFERENCE :: EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 24,181,1994

盐酸苯乙双胍安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 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 ]:
2811.0

[ WGK德国 ]:
3

[ RTECS号 ]:
DU2200000

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2942000000

盐酸苯乙双胍上下游产品

盐酸苯乙双胍上游产品

盐酸苯乙双胍下游产品

盐酸苯乙双胍海关

[ 海关编码 ]: 2942000000

盐酸苯乙双胍文献

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