Buformin (hydrochloride)
(Synonyms: 盐酸丁双胍; 1-Butylbiguanide hydrochloride) 目录号 : GC42987
An antihyperglycemic biguanide
Cas No.:1190-53-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Buformin is a biguanide derivative with antihyperglycemic activity. It delays absorption of glucose from the gastrointestinal tract, increases insulin sensitivity and glucose utilization in peripheral cells, and inhibits hepatic gluconeogenesis. It can also deactivate the glycolytic pathway by suppressing glyceraldehyde 3-phosphate dehydrogenase gene expression, which can lead to lactic acidosis. Biguanides, such as buformin, are reported to inhibit the mitochondrial respiratory complex I by inhibiting ubiquinone reduction and by stimulating reactive oxygen species production via the complex I flavin. Some biguanides, including buformin, can also inhibit the mitochondrial ATP synthase. Buformin has also been examined for antitumor activity due to its ability to disrupt the unfolded protein response transcription program during glucose deprivation, which induces cell death in glucose-deprived tumor cells.
| Cas No. | 1190-53-0 | SDF | |
| 别名 | 盐酸丁双胍; 1-Butylbiguanide hydrochloride | ||
| Canonical SMILES | NC(NC(NCCCC)=N)=N.Cl | ||
| 分子式 | C6H15N5•HCl | 分子量 | 193.7 |
| 溶解度 | PBS (pH 7.2): 1 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 5.1626 mL | 25.8131 mL | 51.6262 mL |
| 5 mM | 1.0325 mL | 5.1626 mL | 10.3252 mL |
| 10 mM | 0.5163 mL | 2.5813 mL | 5.1626 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
[The use of natural and synthetic hydrophilic polymers in the formulation of metformin hydrochloride tablets with different profile release]
Polim Med 2012;42(3-4):167-84.PMID:23457958doi
Aim of study: Metformin hydrochloride after Buformin and phenformin belongs to the group of biguanid derivatives used as oral anti-diabetic drugs. The object of the study is the technological analysis and the potential effect of biodegradable macromolecular polymers on the technological and therapeutic parameters of oral anti-diabetic medicinal products with metformin hydrochloride: Siofor, Formetic, Glucophage, Metformax in doses of 500mg and 1000mg and Glucophage XR in a dose of 500 mg of modified release. Materials and methods: Market therapeutic products containing 500 and 1000 mg of metformin hydrochloride in a normal formulation and 500 mg of metformin hydrochloride in a formulation of modified release were analyzed. Following research methods were used: technological analysis of tablets, study of disintegration time of tablets, evaluation of pharmaceutical availability of metformin hydrochloride from tested therapeutic products, mathematical and kinetic analysis of release profiles of metformin hydrochloride, statistical analysis of mean differences of release coefficients. Results: The percentage of excipients in the XR formulation is higher and constitutes 50.5% of a tablet mass. However, in standard formulations the percentage is lower, between 5.5% and 12.76%. On the basis of the results of disintegration time studies, the analysed therapeutic products can be divided into two groups, regardless the dose. The first one are preparations with faster (not fast!) disintegration: Glucophage i Metformax. The second group are preparations with slower disintegration, more balanced in the aspect of a high dose of the biologically active substance: Formetic and Siofor. Products with a lower content of excipients (Metformax, Glucophage) disintegrate in a faster way. The disintegration rate of the products with a higher content of excipients (Formetic, Siofor) is slower. The appearance of metformin hydrochloride concentration in the gastrointestinal contents, balanced in time, caused by a slower disintegration-dissolving of a tablet, is conducive to the reduction of gastrointestinal side effects and better tolerance of the therapeutic product by a patient. The study on pharmaceutical availability indicated relevant kinetic differences between tested therapeutic products. They are particularly visible between standard formulations and the one with prolonged release (Glucophage XR500). Its release profile bears features of kinetics similar to zero-order reactions. Conclusions: Tested therapeutic products contain a large amount of the biologically active substance in relation to the content of excipients. A higher content of excipients in a single tablet mass distinguishes Siofor in comparison with Glucophage i Metformax. The excipients used in the formulations of tested preparations are comparable. A higher percentage of binding agents (HPMC, PVP) is observed, but there is a lack of typical disintegrants which results in a longer disintegration time up to 15 minutes. Siofor disintegrates at the same time as Formetic, but longer than Glucophage i Metformax. Considering the large content of the active substance and pharmacological properties of metformin hydrochloride, such a disintegration might have beneficial consequences, because the amount of the free active substance in the gastrointestinal tract will increase over the longer time period what will reduce the level of gastrointestinal side effects. The release profiles of metformin hydrochloride from tested therapeutic products are comparable. The Glucophage XR 500 formulation with the release kinetics of metformin hydrochloride similar to the zero-order kinetics is completely different from the others. The above is confirmed by the mathematical analysis of release profiles of metformin hydrochloride from tested preparations where equations of lines describing the release profile are characterized by similar values of correlation coefficients.
[Concentration of 14C-1-butylbiguanide in plasma of diabetic patients and its elimination after administration of a new Galenical formulation (author's transl)]
Arzneimittelforschung 1976;26(6):1227-9.PMID:989423doi
The time course of 1-butylbiguanide concentration in plasma and the urinary and fecal elimination of the substance were measured in six female elimination of the substance were measured in six female diabetic patients after oral administration of 100 mg of 14C-1-butylibiguanide hydrochloride as Sindiatil. The mean maximum plasma concentration was 37 mug/100 ml and was reached after about 2 1/2 h. At least semi-maximum plasma concentrations (greater than or equal 18 mug/100 ml) were maintained between the 1st and 8th h after administration. Within 24 h 64% of the administered dose were eliminated (36% via the kidneys, 28% with the faeces). After 3 days a total of 80% had been eliminated, one-half each in urine and faeces, respectively. The average time taken for 50% of maximum renal elimination, and thus of the absorbed quantity, to be excreted was 7.2 h.