在Hep3B细胞中，orphenibuta可以提高甲氨蝶呤（MTX）的抗癌功效[1]。 Hep3B 细胞可能会因羟保泰松（2.5–7.5 µM；48 小时）和 MTX (0.25–1.0 µM) 联合治疗而受到细胞毒性影响 [1]。 Orphenibuta 可以修复肝细胞 [1]。

将羟保泰松（70 mg/kg/周；口服；分两次剂量；持续 13 周）与 MTX（5.0 或 2.5 mg/kg/周；腹腔注射）联合使用可能具有抗癌作用 [1]。

细胞毒性测定[1]
细胞类型： Hep3B 细胞
测试浓度： 2.5 µM、5 µM、7.5 µM
孵育时间： 48小时
实验结果：MTX的细胞毒性增强。

Animal/Disease Models: Wistar strain albino male rats (5-6 weeks; 150-220 g) [1]
Doses: 70 mg/kg/week (co-treatment with MTX 5.0 or 2.5 mg/kg/week)
Route of Administration: Oral ; once a week; taken in two divided doses; for 13 weeks.
Experimental Results: When combined with MTX, it has potential anti-cancer activity in rats.

Absorption, Distribution and Excretion
...OXYPHENBUTAZONE IS EXTENSIVELY BOUND TO PLASMA PROTEINS & HAS PLASMA HALF-TIME OF SEVERAL DAYS. ...ONLY SLOWLY EXCRETED IN URINE, SINCE BINDING TO PLASMA PROTEIN LIMITS...GLOMERULAR FILTRATION, &...RELATIVELY HIGH PKA, WHICH FAVORS PASSIVE REABSORPTION IN DISTAL TUBULE.

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Metabolism / Metabolites
OXIDN OF PHENYLBUTAZONE DURING CHRONIC DOSING BY MEASURING URINARY EXCRETION OF 3 METABOLITES, OXYPHENBUTAZONE GAMMA-HYDROXYPHENBUTAZONE & P,GAMMA-HYDROXYPHENBUTAZONE DURING INFUSION OF HYDROCORTISONE SODIUM SUCCINATE IS REPORTED.

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Biological Half-Life
IN MAN, OXYPHENBUTAZONE HAS BIOLOGICAL HALF-LIFE OF ABOUT 2 DAYS.

Interactions
SOME TRICYCLIC COMPD HAVE BEEN SHOWN TO DELAY OXYPHENYLBUTAZONE ABSORPTION IN RAT BY INCR GASTRIC EMPTYING TIME.
...OXYPHENBUTAZONE MAY PROLONG PROTHROMBIN TIME IN PT RECEIVING COUMARIN ANTICOAGULANTS CONCOMITANTLY & MAY INCR HYPOGLYCEMIC EFFECT OF INSULIN & ORAL HYPOGLYCEMIC AGENTS.
WHEN OXYPHENBUTAZONE & METHANDROSTENOLONE ARE ADMIN CONCURRENTLY IN HUMANS, SERUM OXYPHENBUTAZONE LEVELS MAY BE ELEVATED. PT TREATED WITH THESE CONCURRENTLY SHOULD BE MONITORED FOR SIGNS OF OXYPHENBUTAZONE-INDUCED ADVERSE EFFECTS.
OXYPHENBUTAZONE ABSORPTION...IS DECR BY DESIPRAMINE.
For more Interactions (Complete) data for OXYPHENBUTAZONE (6 total), please visit the HSDB record page.

[1]. Oxyphenbutazone promotes cytotoxicity in rats and Hep3B cellsvia suppression of PGE2 and deactivation of Wnt/β-catenin signaling pathway. Mol Cell Biochem. 2018 Jul;444(1-2):187-196.

[2]. Nonsteroidal anti-inflammatory drug sensitizes Mycobacterium tuberculosis to endogenous and exogenous antimicrobials. Proc Natl Acad Sci U S A. 2012 Oct 2;109(40):16004-11.

Oxyphenbutazone is a metabolite of phenylbutazone obtained by hydroxylation at position 4 of one of the phenyl rings. Commonly used (as its hydrate) to treat pain, swelling and stiffness associated with arthritis and gout, it was withdrawn from the market 1984 following association with blood dyscrasis and Stevens-Johnson syndrome. It has a role as a non-steroidal anti-inflammatory drug, a non-narcotic analgesic, an antipyretic, a gout suppressant, a drug metabolite, a xenobiotic metabolite, an antineoplastic agent and an antimicrobial agent. It is a member of pyrazolidines and a member of phenols. It is functionally related to a phenylbutazone.
Oxyphenbutazone was withdrawn from the Canadian market in March 1985 due to concerns regarding bone marrow suppression.
A non-steroidal anti-inflammatory drug. Oxyphenbutazone eyedrops have been used abroad in the management of postoperative ocular inflammation, superficial eye injuries, and episcleritis. (From AMA, Drug Evaluations Annual, 1994, p2000) It had been used by mouth in rheumatic disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis but such use is no longer considered justified owing to the risk of severe hematological adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p27)

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Mechanism of Action
...HAS PROMINENT ANTI-INFLAMMATORY EFFECTS IN ANIMALS, & COMPARABLE EFFECTS... IN PT WITH RHEUMATOID ARTHRITIS & RELATED DISORDERS. ...INHIBITS BIOSYNTHESIS OF PROSTAGLANDINS, UNCOUPLES OXIDATIVE PHOSPHORYLATION, & INHIBITS ATP-DEPENDENT BIOSYNTHESIS OF MUCOPOLYSACCHARIDE SULFATES IN CARTILAGE. /PHENYLBUTAZONE/

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Therapeutic Uses
Anti-Inflammatory Agents, Non-Steroidal; Anti-Inflammatory Agents, Topical
EPISCLERITIS & UVEITIS ASSOC WITH RHEUMATOID ARTHRITIS HAVE SOMETIMES BEEN TREATED SUCCESSFULLY WITH...OXYPHENBUTAZONE.
...HAS MILD URICOSURIC EFFECT IN EXPTL ANIMALS & MAN, PROBABLY ATTRIBUTABLE TO ONE OF ITS METABOLITES.
...HAS MILD URICOSURIC EFFECT IN EXPTL ANIMALS & MAN... URICOSURIC EFFECT RESULTS FROM DIMINISHED TUBULAR REABSORPTION OF URIC ACID. ...CAUSES SIGNIFICANT RETENTION OF SODIUM & CHLORIDE, ACCOMPANIED BY REDN IN URINE VOL... REDUCES UPTAKE OF IODINE BY THYROID GLAND...ALSO INHIBITS ENZYMES OF KREBS CYCLE... /PHENYLBUTAZONE/
For more Therapeutic Uses (Complete) data for OXYPHENBUTAZONE (7 total), please visit the HSDB record page.

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Drug Warnings
...40-YR OLD MAN RECEIVED TOTAL DOSE OF 1 G OXYPHENBUTAZONE OVER APPROX 5 DAYS, 2 MO BEFORE ADMISSION TO HOSPITAL WITH SEVERE ANEMIA & LEUCOCYTOSIS; HE DIED ON THIRD DAY AFTER DEVELOPING THIS CONDITION.
...WHITE-BLOOD CELL DISORDER CONCERNED 47-YR-OLD MAN WHO, 13 MO BEFORE ADMISSION WITH TEMP, HAD BEEN GIVEN 1.9 G OXYPHENBUTAZONE OVER 2-WK PERIOD. ON ADMISSION, HE WAS GIVEN 0.6 G OF DRUG; BLOOD EXAM SHOWED THAT HE HAD LEUKEMIA, OF WHICH HE DIED APPROX 4 MO LATER.
IT SHOULD ALWAYS BE TAKEN IMMEDIATELY AFTER MEALS OR WITH FULL GLASS OF MILK, TO MINIMIZE GASTRIC IRRITATION.
OXYPHENBUTAZONE IS SAID TO CAUSE SOMEWHAT LESS GASTRIC IRRITATION /THAN PHENYLBUTAZONE/. ... IT SHOULD BE TAKEN IN 3 OR 4 DIVIDED PORTIONS AFTER MEALS TO LESSEN GASTRIC IRRITATION.
For more Drug Warnings (Complete) data for OXYPHENBUTAZONE (8 total), please visit the HSDB record page.

C19H20N2O3

324.38

324.147

129-20-4

Oxyphenbutazone monohydrate;7081-38-1;Oxyphenbutazone-d9;1189693-23-9;Oxyphenbutazone-13C6

4641

White to off-white solid powder

1.241g/cm3

485.6ºC at 760mmHg

109-111°C

247.5ºC

4.7E-10mmHg at 25°C

1.61

3.623

60.85

1

3

5

24

454

0

HFHZKZSRXITVMK-UHFFFAOYSA-N

InChI=1S/C19H20N2O3/c1-2-3-9-17-18(23)20(14-7-5-4-6-8-14)21(19(17)24)15-10-12-16(22)13-11-15/h4-8,10-13,17,22H,2-3,9H2,1H3

4-butyl-1-(4-hydroxyphenyl)-2-phenylpyrazolidine-3,5-dione

G 29701. Oxyphenbutazone; G29701; G-29701

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~308.29 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.71 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (7.71 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。
*20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (7.71 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。