Carbutamide
(Synonyms: 氨磺丁脲,BZ-55) 目录号 : GC39547
A first generation sulfonylurea
Cas No.:339-43-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Carbutamide is a first generation sulfonylurea.1 It inhibits ATP-sensitive potassium (KATP) channels in β-cells with an IC50 value of 173 ?M.2 It reduces blood glucose levels in anesthetized dogs when administered at a dose of 50 mg/kg.3 Carbutamide also increases ventricular fibrillation in a rat model of cardiac ischemia induced by left anterior descending (LAD) coronary artery ligation.1 Formulations containing carbutamide have previously been used in the treatment of diabetes.
1.Ballagi-Pordány, G., K?szeghy, A., Koltai, M.Z., et al.Divergent cardiac effects of the first and second generation hypoglycemic sulfonylurea compoundsDiabetes Res. Clin. Pract.8(2)109-114(1990) 2.Schwanstecher, C., Meyer, M., Schwanstecher, M., et al.Interaction of N-benzoyl-D-phenylalanine and related compounds with the sulphonylurea receptor of β-cellsBr. J. Pharmacol.123(6)1023-1030(1998) 3.Pozza, G., Galansino, G., and Foà, P.P.Insulin secretion following carbutamide injections in normal dogsProc. Soc. Exp. Biol. Med.93(3)539-542(1956)
| Cas No. | 339-43-5 | SDF | |
| 别名 | 氨磺丁脲,BZ-55 | ||
| Canonical SMILES | O=S(C1=CC=C(N)C=C1)(NC(NCCCC)=O)=O | ||
| 分子式 | C11H17N3O3S | 分子量 | 271.34 |
| 溶解度 | DMSO: 50 mg/mL (184.27 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6854 mL | 18.4271 mL | 36.8541 mL |
| 5 mM | 0.7371 mL | 3.6854 mL | 7.3708 mL |
| 10 mM | 0.3685 mL | 1.8427 mL | 3.6854 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。
Carbutamide--the first oral antidiabetic. A retrospect
Exp Clin Endocrinol Diabetes 1998;106(2):149-51.PMID:9628248DOI:10.1055/s-0029-1211968.
This work describes the history of the first oral antidiabetic in East and West Germany. M. Janbon and A. Loubatières reported experimental and clinical findings about a blood sugar-decreasing effect of a sulphonamide derivate, sulphoisopropyl thiodiazol (1942). These findings, however, did not prove to be useful in the treatment of diabetes. In 1952 the author found a series of hypoglycemic shocks with the sulfonamid-urea derivate carbutamdide during clinical tests of infectious diseases. These were reported to the pharmaceutical company Von Heyden in Dresden. The head chemist E. Haack went with my files from East to West Germany, to Boehringer Mannheim. Without mentioning the synthesis in Dresden, he synthesized Carbutamide in Mannheim. The hypoglycemic effect was rediscovered by his friend H. Franke together with J. Fuchs. It took twenty years until the results of the author's research were officially acknowledged.
The effect of human plasma on the glucose uptake of the rat diaphragm before and after administration of Carbutamide
Br J Pharmacol Chemother 1957 Dec;12(4):475-8.PMID:13489177DOI:10.1111/j.1476-5381.1957.tb00168.x.
The glucose uptake of the rat diaphragm has been determined in the presence of the plasma of young volunteers before and after administration of Carbutamide without and with added insulin. The increase in the glucose uptake of the rat diaphragm due to the added plasma above that in the medium alone has been termed plasma effect. The increase in the glucose uptake of the rat diaphragm with plasma and added insulin above that with only insulin in the medium has been termed plasma+insulin effect. There was a significant increase in the plasma effect and the plasma+insulin effect after Carbutamide administration. The increase in the plasma+insulin effect was significantly greater than the increase in the plasma effect. From these observations it has been suggested that Carbutamide potentiates the action of insulin peripherally. Observed facts about Carbutamide do not contradict this mechanism of action.
Treatment of diabetic patients; observations on the use of Carbutamide and tolbutamide
Calif Med 1956 Nov;85(5):285-8.PMID:13364673doi
Of a group of 32 patients with diabetes, 26 had a favorable modification of the disease in response to administration of butyl-sulfonyl-urea. All but one of the patients who had good response were past the age of 38. All diabetic patients included in this group were those with little or no tendency to ketosis after cessation of insulin administration. No toxic manifestations were noted except for a slight decrease in leukocytes in one case.
Effects of various hypoglycaemic sulphonylureas on the cardiotoxicity of glycosides
Eur J Clin Pharmacol 1985;28(4):367-70.PMID:3928386DOI:10.1007/BF00544351.
In diabetic patients it has been shown that tolbutamide and Carbutamide enhanced and glibenclamide did not influence the incidence of digitalis intoxication, or that of multifocal ectopic beats or coupling due to premature ectopic ventricular beats during digitalis therapy. In rabbits glibenclamide decreased and tolbutamide and Carbutamide increased strophanthidin toxicity in a dose dependent manner. It was concluded that glibenclamide should be preferred to tolbutamide or Carbutamide in digitalis-treated diabetics, when satisfactorily metabolic control is not achieved with a dietary regime alone.