Hydroxyhexamide ((±)-Hydroxyhexamid)
(Synonyms: 乙酸己脲) 目录号 : GC32482
Hydroxyhexamide is a pharmacologically active metabolite of acetohexamide, which is a sulfonylurea hypoglycemic agent.
Cas No.:3168-01-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Hydroxyhexamide is a pharmacologically active metabolite of acetohexamide, which is a sulfonylurea hypoglycemic agent.
| Cas No. | 3168-01-2 | SDF | |
| 别名 | 乙酸己脲 | ||
| Canonical SMILES | O=S(C1=CC=C(C(O)C)C=C1)(NC(NC2CCCCC2)=O)=O | ||
| 分子式 | C15H22N2O4S | 分子量 | 326.41 |
| 溶解度 | DMSO : ≥ 300 mg/mL (919.09 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 | 3.0636 mL | 15.3182 mL | 30.6363 mL |
| 5 mM | 0.6127 mL | 3.0636 mL | 6.1273 mL |
| 10 mM | 0.3064 mL | 1.5318 mL | 3.0636 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。
GLC determination of acetohexamide and Hydroxyhexamide in biological fluids
J Pharm Sci 1977 May;66(5):635-8.PMID:874743DOI:10.1002/jps.2600660507.
A sensitive and specific GLC assay was developed for acetohexamide and Hydroxyhexamide, its major metabolite, in plasma and urine. The assay uses tolbutamide as a mass internal standard. Compounds are extracted from acidified plasma or urine with toluene, converted to methylated derivatives with dimethyl sulfate, and measured by GLC using a flame-ionization detector. With GLC-mass spectrometry, the compounds measured are the N-methylsulfonamides resulting from GLC pyrolysis. Plasma and urine data are presented from a bioavailability study to demonstrate the utility of this method.
Comparative pharmacokinetics of acetohexamide and its metabolite, Hydroxyhexamide in laboratory animals
Chem Pharm Bull (Tokyo) 1989 Mar;37(3):760-5.PMID:2752490DOI:10.1248/cpb.37.760.
The pharmacokinetic profiles of the hypoglycemic agent, acetohexamide (AH) and its major active metabolite, Hydroxyhexamide (HH) were studied in three species of laboratory animals after intraperitoneal (ipl) administration in comparison with those after intravenous (iv) administration of AH and of the preformed metabolite HH. Reductive biotransformation of AH to HH was reversible in rats and guinea pigs, while it was irreversible in rabbits. The parameters of reversible drug-metabolite pharmacokinetics were calculated, including essential clearances of reversible and irreversible elimination, volumes of distribution at the steady state and sojourn times or turnover rates of the metabolite pair. An interconversion model, which incorporated a first-pass metabolism, was applied to the disposition kinetics of AH and HH, and the available fractions of AH and generated metabolite HH in each species were elucidated.
Acetohexamide hypoglycemia: treatment by peritoneal dialysis
South Med J 1977 Oct;70(10):1240-1.PMID:910178doi
Acetohexamide hypoglycemia in a patient with renal failure has been successfully treated by peritoneal dialysis. Peritoneal dialysis was done in such a patient, and specimens of serum were collected to measure levels of acetohexamide and its main active metabolite, Hydroxyhexamide. During dialysis, hypoglycemia was corrected. After 17 1/2 hours of dialysis, serum acetohexamide level was essentially unchanged. Serum Hydroxyhexamide level had decreased at a slower rate than the rate of decrease previously measured in a uremic patient not on dialysis. Although peritoneal dialysis may correct the hypoglycemia, the data suggest that acetohexamide and Hydroxyhexamide are not dialyzable. Due to these problems this drug should not be used in patients with chronic renal failure. The drug of choice to control hyperglycemia in patients with renal insufficiency is insulin. If for any reason insulin cannot be used, tolbutamide is the oral hypoglycemic agent of choice.
Individual Variability of Carbonyl Reductase Activity for Acetohexaminde in Human Erythorcytes
Am J Ther 1995 Jan;2(1):47-49.PMID:11850647doi
Acetohexamide, an oral antidiabetic agent, is metabolized by carbonyl reductase to Hydroxyhexamide, which has a higher hypoglycemic potency than the parent compound. In the present study, interindividual variability of carbonyl reductase activity in erythrocyte was examined. Enzyme activity in 31 healthy subjects (23.9 plus minus 3.4 years, mean plus minus SD) was monitored by measuring formation of Hydroxyhexamide using HPLC methods. Using 0.5 mM acetohexamide as substrate, reductase activity of 6.06 plus minus 0.06 nmol min(minus sign1) gHb(minus sign1) (range: 5.9--6.2) with a coefficient of variation of 15% was observed in erythrocytes. Acetohexamide-reducing activity in erythrocytes showed a normal distribution and the interindividual variability of the reductase activity was found to be small, implying that the large variability reported for the acetohexamide plasma half-life is not caused by the amount of reductase enzyme in erythrocytes.
Carbonyl reductase activity for acetohexamide in human erythrocytes
Drug Metab Dispos 1994 May-Jun;22(3):367-70.PMID:8070312doi
Acetohexamide is an oral antidiabetic agent and is metabolized by the reductive conversion of the acetoxy group to a secondary alcohol metabolite. In vivo, many drugs are metabolized by reductase enzymes; however, the characteristics of the enzymes that reduce carbonyl compounds need to be clarified. We tested whether reductase activity for acetohexamide can be found in human erythrocytes. Enzyme activity was monitored by formation of Hydroxyhexamide using HPLC methods. In human erythrocytes, reductase activity (6.10 +/- 1.20 nmol/min/g hemoglobin) (mean +/- SD) was indeed observed, when 0.5 mM acetohexamide was used as a substrate. KM values and Vmax at the physiologically important pH 7.4 were 0.70 +/- 0.13 mM and 9.19 +/- 0.88 nmol/min/g hemoglobin, respectively. Separation of protein by gel filtration gave one major peak fraction with reductase activity whose molecular weight was estimated to be 31,000. Known substrates of carbonyl reductase such as menadione, daunorubicin, and ethacrynic acid inhibited the acetohexamide reduction. The acetohexamide reductase in erythrocyte showed characteristics of carbonyl reductase. Furthermore, acetohexamide reductase activity in erythrocyte was approximately 30% activity of that of human liver (0.17 +/- 0.05 nmol/min/mg cytosolic protein). The pattern of inhibitors in human liver was essentially the same as that in erythrocytes. It is plausible that the activity in erythrocytes may predict the activity in the liver. It was concluded that carbonyl reductase in human erythrocyte plays an important role in acetohexamide metabolism.