丁双胍盐酸盐

丁双胍盐酸盐用途

Buformin hydrochloride (1-Butylbiguanide hydrochloride) 是一种有效的,具有口服活性的降血糖试剂 (antidiabetic agent),是一种 AMPK 活化剂。Buformin 降低肝糖异生并降低血糖生成。Buformin 也具有抗癌活性,可以应用于癌症研究,如宫颈癌、乳腺癌等。

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丁双胍盐酸盐名称

[ CAS 号 ]:
1190-53-0

[ 中文名 ]:
盐酸丁福明

[ 英文名 ]:
Buformin hydrochloride

[中文别名 ]:

盐酸丁二胍

[英文别名 ]:

EINECS 214-723-6
butyl-biguanide hydrochloride

丁双胍盐酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> AMPK

研究领域 >> 癌症

信号通路 >> PI3K/Akt/mTOR 信号通路 >> AMPK

[体外研究]

盐酸二甲双胍(0-10 mM；5天)以浓度依赖的方式抑制SKBR3和BT474细胞生长,对erbB-2过度表达的SKBR3和BT474细胞的IC50值分别为246.7μM和 98.6μM[1]。盐酸二甲双胍(0-3mm；48h)增加G0/G1期细胞百分率,降低S期细胞百分率,尤其是SKBR3细胞[1]。盐酸二甲双胍(0-3 mM；24小时)抑制RTK激活,包括下游的erbB-2和IGF1R信号传导,并且SKBR3和BT474细胞中的Akt激活/磷酸化受到抑制[1]。细胞活力测定[1]细胞系：ErbB-2-过度表达SKBR3和BT474细胞浓度：0μM、1μM、3μM、10μM、30μM、100μM、300μM、1、3或10 mM孵育时间：5天结果：ErbB-2-过度表达乳腺细胞的细胞活力降低。细胞周期分析[1]细胞系：ErbB-2-过度表达的SKBR3和BT474细胞浓度：0.5毫米；1毫米；3毫米孵育时间：48小时结果：细胞数增加,停滞在G0/G1期。Western Blot分析[1]细胞系：ErbB-2-过度表达的SKBR3和BT474细胞浓度：0 mM、0.1 mM、0.3 mM、1 mM或3 mM孵育时间：24小时结果：p-AMPK、p-p706S、p-ERK1/2的表达呈浓度依赖性降低。

[体内研究]

盐酸二甲双胍(口服；7.6 mmol/kg chow；7天)在MMTV-erbB-2转基因小鼠中显示出显著减少的肿瘤体积和重量,并阻碍乳腺的形态发生和增殖[1]。动物模型：雌性MMTV-erbB-2转基因小鼠[1]剂量：7.6 mmol/kg给药：口服；7天结果：抑制MMTV-erbB-2转基因小鼠乳腺同基因肿瘤生长。

[参考文献]

[1]. Amanda B Parris, et al. Buformin hydrochloride Inhibits the Stemness of erbB-2-overexpressing Breast Cancer Cells and Premalignant Mammary Tissues of MMTV-erbB-2 Transgenic Mice. J Exp Clin Cancer Res

[2]. Jing Li, et al. Buformin hydrochloride Suppresses Proliferation and Invasion via AMPK/S6 Pathway in Cervical Cancer and Synergizes With Paclitaxel. Cancer Biol Ther. 2018 Jun 3;19(6):507-517.

丁双胍盐酸盐物理化学性质

[ 沸点 ]:
322.7ºC at 760 mmHg

[ 熔点 ]:
174-177ºC

[ 分子式 ]:
C₆H₁₆ClN₅

[ 分子量 ]:
193.67800

[ 闪点 ]:
148.9ºC

[ 精确质量 ]:
193.10900

[ PSA ]:
97.78000

[ LogP ]:
2.27750

[ 蒸汽压 ]:
0.000275mmHg at 25°C

[ 储存条件 ]:
库房通风低温干燥,与食品原料类分开存放

丁双胍盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DU1135000

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

CAS REGISTRY NUMBER :: 1190-53-0

LAST UPDATED :: 199707

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C6-H15-N5.Cl-H

MOLECULAR WEIGHT :: 193.72

WISWESSER LINE NOTATION :: MUYZMYUM&M4 &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 :: 320 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 :: 380 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 - mouse

DOSE/DURATION :: 74 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 105 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 - guinea pig

DOSE/DURATION :: 58 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 :: 23 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Embryo

DOSE/DURATION :: 1900 ug/L

REFERENCE :: SNSHBT Senshokutai. Chromosome. (Sensyokutai Gakkai, Kaokusai Kirisutokyo Daigaku, Mitaka, Tokyo-to, Japan) No.1- 1946- Adopted new numbering in 1976. Volume(issue)/page/year: (20),574,1980

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丁双胍盐酸盐安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H315-H318-H335

[ 警示性声明 ]:
P280-P301 + P312 + P330-P305 + P351 + P338 + P310

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
22-43-36

[ 安全声明 (欧洲) ]:
36/39-46

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

[ 海关编码 ]:
2925290090

丁双胍盐酸盐海关

[ 海关编码 ]: 2925290090

[ 中文概述 ]:
2925290090 其他亚胺及其衍生物，以及它们的盐。监管条件:无。增值税率:17.0%。退税率:9.0%。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

[ Summary ]:
2925290090 other imines and their derivatives; salts thereof。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%