Oxyphenbutazone
(Synonyms: 羟布宗) 目录号 : GC40651
An NSAID
Cas No.:129-20-4
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
Oxyphenbutazone is a metabolite of phenylbutazone . Both compounds were identified as having anti-inflammatory effects in early studies, and, as a result, are considered NSAIDs. Interestingly, the effects of the two compounds in animal models differ, with phenylbutazone having anti-inflammatory effects in rheumatic diseases and oxyphenbutazone reducing edema in certain types of acute inflammation. Oxyphenbutazone is a poor inhibitor of prostaglandin synthesis, but, like other NSAIDs, it inhibits organic anion transporter 1 (Ki = 32 µM). It inhibits the growth of MH60/BSF-2 cells induced by IL-6 (IC50 = 7.5 µM). Oxyphenbutazone stimulates neurite outgrowth at 1.5 µM and sensitizes M. tuberculosis to antimicrobials.
| Cas No. | 129-20-4 | SDF | |
| 别名 | 羟布宗 | ||
| Canonical SMILES | O=C(C1CCCC)N(C2=CC=CC=C2)N(C3=CC=C(O)C=C3)C1=O | ||
| 分子式 | C19H20N2O3 | 分子量 | 324.4 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 50 mg/ml,PBS (pH 7.2): 0.5 m/ml,Water: 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。 |
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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 | 3.0826 mL | 15.4131 mL | 30.8261 mL |
| 5 mM | 0.6165 mL | 3.0826 mL | 6.1652 mL |
| 10 mM | 0.3083 mL | 1.5413 mL | 3.0826 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。
Oxyphenbutazone-induced goitre
Postgrad Med J 1977 Feb;53(616):93-5.PMID:141661DOI:10.1136/pgmj.53.616.93.
A woman who had taken Oxyphenbutazone for 4 years because of back pain presented with goitre and hypothyroidism. This was shown to be due to an organification defect, caused or aggravated by Oxyphenbutazone.
Oxyphenbutazone (tandearil) in rhinoplasty. A clinical evaluation of effectiveness
Calif Med 1966 Oct;105(4):271-5.PMID:5341676doi
To evaluate the effectiveness of Oxyphenbutazone as an anti-inflammatory agent, a double-blind study of Oxyphenbutazone and a placebo in a group of 42 patients who had nasal cosmetic operations involving osteotomy was carried out. The observations included direct objective measurement of the width of the palpebral fissure after operation, grading of the severity of postoperative edema and ecchymosis from photographs, and observations by the patients regarding the clearing of the postoperative discoloration. It appeared from the results of these observations that Oxyphenbutazone is not effective in preventing postoperative edema in such operations or in promoting more rapid resolution of postoperative edema. It did appear to enhance the clearing of postoperative periorbital ecchymosis.
The objective and timing of drug disposition studies, appendix II. Plasma concentrations of Oxyphenbutazone in dogs given Oxyphenbutazone or the calcium or sodium salts of its phosphate ester
Drug Metab Rev 1975;4(2):249-65.PMID:1222682DOI:10.3109/03602537508993759.
Plasma levels of Oxyphenbutazone were measured in beagle dogs following oral administration of Oxyphenbutazone and salts of Oxyphenbutazone phosphate. Dosage with sodium and calcium salts of Oxyphenbutazone phosphate produced higher Oxyphenbutazone plasma levels than dosage with Oxyphenbutazone itself. Oxyphenbutazone phosphate was not detected in plasma following oral dosing with salts of Oxyphenbutazone phosphate but was found in plasma following intramuscular administration of Oxyphenbutazone phosphate sodium salt. A metabolite, Oxyphenbutazone glucuronide, was found in plasma of dogs following administration of either Oxyphenbutazone or salts of Oxyphenbutazone phosphate.
Diffusion of Oxyphenbutazone into synovial fluid, synovial tissue, joint cartilage and cerebrospinal fluid
Eur J Clin Pharmacol 1983;25(1):107-12.PMID:6617711DOI:10.1007/BF00544025.
The diffusion of Oxyphenbutazone into synovial and cerebrospinal fluids and synovium and joint cartilage was investigated in 25 patients receiving short-term treatment. In the synovial fluid, the mean Oxyphenbutazone concentration, was 57.1 +/- 13.4% of the plasma level, due to its excellent diffusion into the joint cavity. In synovial tissue, the Oxyphenbutazone level was higher in patients with severe inflammation than in those with no or little inflammation. Penetration into joint cartilage is less than into synovial tissue. In cerebrospinal fluid the concentration was close to the level of free plasma Oxyphenbutazone. The findings show increased diffusion of Oxyphenbutazone towards its site of action in inflammation.
Phenylbutazone and Oxyphenbutazone distribution into tissue fluids in the horse
J Vet Pharmacol Ther 1986 Jun;9(2):204-12.PMID:3723663DOI:10.1111/j.1365-2885.1986.tb00031.x.
The clinically recommended dose rate of phenylbutazone (4.4 mg/kg) was administered intravenously as a single dose to five Welsh Mountain ponies. Distribution of phenylbutazone and its active metabolite Oxyphenbutazone into body fluids was studied by measuring concentrations in plasma, tissue-cage fluid, peritoneal fluid and acute inflammatory exudate harvested from a polyester sponge model of inflammation. The ready penetration of phenylbutazone into inflammatory exudate was demonstrated by the relatively high mean value for Cmax of 12.4 micrograms/ml occurring at a time of 4.6 h and a mean AUC0-24 of 128 microgram X h/ml. A high mean exudate:plasma AUC0-24 ratio of 0.83 was recorded. Plasma:exudate concentration ratios for phenylbutazone were initially greater than and subsequently less than one; the slower clearance from exudate was indicated by approximate t1/2 beta) values of 4.8 and 24 h for plasma and exudate, respectively. These findings may help to explain the relatively long duration of action of phenylbutazone, in spite of a plasma elimination half-life of less than 5 h. Lower values of Cmax and AUC0-24 for phenylbutazone passage into peritoneal fluid (6.3 micrograms/ml and 45 micrograms X h/ml) were recorded, and a limited number of sampling times indicated a similar degree of penetration as into tissue cage fluid. Mean concentrations of Oxyphenbutazone in all fluids were lower than phenylbutazone concentrations at all times, but ready penetration of the metabolite into body fluids, especially into inflammatory exudate, occurred suggesting that Oxyphenbutazone may contribute to the anti-inflammatory effect. The hyperaemia of acute inflammation and the high protein levels in inflammatory exudate may both assist passage of phenylbutazone and Oxyphenbutazone into exudate.