Vedaprofen
(Synonyms: 维达洛芬,,Quadrisol; CERM 10202; PM 150) 目录号 : GC45141An NSAID used in animals
Cas No.:71109-09-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >95.00%
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Vedaprofen is a non-steroidal anti-inflammatory drug (NSAID) commonly used in veterinary medicine to combat pain, inflammation, and fever associated with acute and chronic musculoskeletal disorders in horses and dogs. In addition to inhibiting COX and reducing prostaglandin H2 synthesis, vedaprofen is reported to block the activity of the E. coli DNA polymerase III β subunit, preventing DNA replication and repair.
Cas No. | 71109-09-6 | SDF | |
别名 | 维达洛芬,,Quadrisol; CERM 10202; PM 150 | ||
Canonical SMILES | CC(C(O)=O)C(C1=C2C=CC=C1)=CC=C2C3CCCCC3 | ||
分子式 | C19H22O2 | 分子量 | 282.4 |
溶解度 | DMF: 25 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.5411 mL | 17.7054 mL | 35.4108 mL |
5 mM | 0.7082 mL | 3.5411 mL | 7.0822 mL |
10 mM | 0.3541 mL | 1.7705 mL | 3.5411 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 | ||||||||||
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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 pharmacokinetics of Vedaprofen and its enantiomers in dogs after single and multiple dosing
J Vet Pharmacol Ther 2005 Jun;28(3):305-12.PMID:15953205DOI:10.1111/j.1365-2885.2005.00659.x.
Vedaprofen is a chiral nonsteroidal anti-inflammatory drug that has been developed as a gel formulation for oral administration to dogs and horses. The pharmacokinetics of Vedaprofen and its enantiomers were studied in beagle dogs after single (intravenous solution and oral gel) and multiple (oral gel) dosing at a dosage of 0.5 mg/kg body weight. Plasma concentrations of Vedaprofen and its enantiomers were analysed by HPLC. The plasma protein binding of Vedaprofen was studied by ultrafiltration. The absorption of Vedaprofen was rapid (tmax 0.63 +/- 0.14 h) and almost complete after oral administration (bioavailability 86 +/- 7%). The terminal half-lives after intravenous and oral administration, 16.8 +/- 2.2 and 12.7 +/- 1.7 h respectively, were of the same order of magnitude. Enantioselective analysis showed that the R(-) enantiomer predominated in plasma. The change in the plasma time course of the plasma R(-)/S(+) enantiomer concentration ratio over time was similar after single intravenous and oral dosing, with R(-)/S(+) ratios in the AUC of 1.7 +/- 0.5 and 1.9 +/- 0.2 respectively. Plasma protein binding of Vedaprofen and its enantiomers was high (> 99.5%). Vedaprofen is absorbed rapidly from the gastrointestinal tract, has a high bioavailability and does not accumulate in plasma in dogs following repeated oral administration.
Vedaprofen therapy in cats with upper respiratory tract infection or following ovariohysterectomy
J Small Anim Pract 2007 Feb;48(2):70-5.PMID:17286658DOI:10.1111/j.1748-5827.2006.00211.x.
Objectives: The antipyretic and analgesic efficacy of Vedaprofen (at a dose of 0.5 mg/kg) was evaluated after repeated once-daily administration (for three or five days) to 80 cats with upper respiratory tract disease or 302 cats undergoing ovariohysterectomy. Methods: Both clinical trials were randomised, double blinded and placebo controlled. Results: In the upper respiratory tract disease trial, Vedaprofen produced a significant reduction in rectal temperature when compared with cats administered antimicrobial treatment only. This antipyretic activity lasted at least four hours after administration on the first day of treatment (day 0) and at least eight hours on day 1 and day 2. Significantly more cats in the treatment group were classified as having returned to normal on day 5, day 6 and day 7 compared with the placebo group. In the ovariohysterectomy trial, scores for behaviour (on day 1, day 2 and day 3) and appetite (on day 1 and day 2) were significantly better in the Vedaprofen group than in the placebo-treated cats. Clinical significance: Vedaprofen produced a clinically relevant reduction in body temperature and a more rapid return to normality in cats with upper respiratory tract disease. Vedaprofen treatment also resulted in more rapid recovery, presumably through the relief of pain and inflammation, in cats that had undergone soft tissue surgery.
A pharmacodynamic and pharmacokinetic study with Vedaprofen in an equine model of acute nonimmune inflammation
J Vet Pharmacol Ther 1999 Apr;22(2):96-106.PMID:10372594DOI:10.1046/j.1365-2885.1999.00173.x.
The pharmacodynamics and enantioselective pharmacokinetics of Vedaprofen were studied in six ponies in a two period cross-over study, in which a mild acute inflammatory reaction was induced by carrageenan soaked sponges implanted subcutaneously in the neck. Vedaprofen, administered intravenously at a dosage of 1 mg/kg, produced significant and prolonged inhibition of ex vivo serum thromboxane B2 (TXB2) synthesis and short-lived inhibition of exudate prostaglandin E2 (PGE2) and TXB2 synthesis. Vedaprofen also partially inhibited oedematous swelling and leucocyte infiltration into exudate. Vedaprofen displayed enantioselective pharmacokinetics, plasma concentrations of the R(-) enantiomer exceeding those of S(+) Vedaprofen. The plasma concentration ratio, R:S, increased from 69:31 at 5 min to 96:4 at 3 h and plasma mean AUC values were 7524 and 1639 ng x h/mL, respectively. Volume of distribution was greater for S(+) Vedaprofen, whilst elimination half-life (t(1/2beta)) and mean residence time were greater for R(-) Vedaprofen. The penetration of Vedaprofen into inflammatory exudate was also enantioselective. For R(-) and S(+) Vedaprofen maximum concentration (Cmax) values were 2950 and 1534 ng/mL, respectively, and corresponding AUC values were 9755 and 4400 ng x h/mL. Vedaprofen was highly protein bound (greater than 99%) in both plasma and exudate. The significance of these data for the therapeutic use of Vedaprofen is discussed.
A comparison of pre and post-operative Vedaprofen with ketoprofen for pain control in dogs
BMC Vet Res 2015 Feb 7;11:24.PMID:25880775DOI:10.1186/s12917-015-0338-4.
Background: This prospective randomized blinded clinical study aimed to investigate the potential of Vedaprofen for preventive analgesia, comparing its analgesic effects with ketoprofen administered post-operatively in dogs undergoing maxillectomy or mandibulectomy. Results: Pain control was effective and rescue analgesia was not necessary in any group. Pain scores were not significantly different between groups. The respiratory rate and rectal temperature were decreased in all groups at extubation until 6 hours post-extubation compared to baseline. Cortisol and epinephrine levels were increased only at 0.5 hours after extubation in all groups compared to baseline. Conclusions: Vedaprofen did not present any preventive analgesic effect. Pre- and postoperative Vedaprofen were as effective as ketoprofen for postoperative pain control.
Comparison of Vedaprofen and meloxicam in dogs with musculoskeletal pain and inflammation
J Small Anim Pract 2002 May;43(5):208-12.PMID:12038853DOI:10.1111/j.1748-5827.2002.tb00059.x.
In this randomised, multicentre clinical study, dogs with musculoskeletal pain and inflammation were treated with either Vedaprofen or meloxicam administered orally at the recommended dose rates. Clinical examinations were carried out regularly and clinical severity scores assigned. In total, 214 cases (73 acute, 141 chronic) were evaluated. Treatment with Vedaprofen and meloxicam was continued for 14 and 17 days, respectively, in the acute cases, and 38 and 39 days in the chronic cases. NSAID treatment resulted in a significant improvement in clinical scores. The overall response to treatment ('responders') at the final clinical examination was 89 per cent and 87 per cent in the acute cases and 72 per cent and 65 per cent in the chronic cases in the Vedaprofen and meloxicam groups, respectively. Mild transient gastrointestinal signs were observed in both groups (11 per cent Vedaprofen, 12 per cent meloxicam). Adverse effects related to NSAIDs resulted in treatment cessation in 5 per cent of the dogs in each group. Vedaprofen and meloxicam were efficacious in, and well tolerated by, most of the dogs in the study.