Eltenac
(Synonyms: 依尔替酸) 目录号 : GC47287
A non-selective COX inhibitor
Cas No.:72895-88-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Eltenac is a non-selective COX inhibitor (IC50 = 0.03 µM for both COX-1 and COX-2 in isolated human whole blood) and a non-steroidal anti-inflammatory drug (NSAID).1 In vivo, eltenac (1 mg/kg) reduces lameness in horses with tendinitis, pododermatitis, navicular disease, non-infectious arthritis, degenerative joint disease, phalanx fracture, and osteochondrosis.2 It also reduces castration-induced edema in horses. Formulations containing eltenac have been used in the treatment of postoperative swelling in horses.
1.Klein, T., Dullweber, F., Brehm, C., et al.Characterization of eltenac and novel COX-2 selective thiopheneacetic acid analogues in vitro and in vivoBiochem. Pharmacol.76(6)717-725(2008) 2.PrÜgner, W., Huber, R., and LÜhmann, R.Eltenac, a new anti-inflammatory and analgesic drug for horses: clinical aspectsJ. Vet. Pharmacol. Ther.14(2)193-199(1991)
| Cas No. | 72895-88-6 | SDF | |
| 别名 | 依尔替酸 | ||
| Canonical SMILES | ClC1=C(NC2=CSC=C2CC(O)=O)C(Cl)=CC=C1 | ||
| 分子式 | C12H9Cl2NO2S | 分子量 | 302.2 |
| 溶解度 | DMF: soluble,DMSO: soluble,Methanol: soluble | 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 | 3.3091 mL | 16.5453 mL | 33.0907 mL |
| 5 mM | 0.6618 mL | 3.3091 mL | 6.6181 mL |
| 10 mM | 0.3309 mL | 1.6545 mL | 3.3091 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。
Eltenac, a new anti-inflammatory and analgesic drug for horses: clinical aspects
J Vet Pharmacol Ther 1991 Jun;14(2):193-9.PMID:1920607DOI:10.1111/j.1365-2885.1991.tb00822.x.
Two controlled studies to determine efficacy in the horse were performed with Eltenac, a new injectable, non-steroidal anti-inflammatory drug (NSAID). Clinical trials were carried out with a dose rate of 1 mg/kg body weight in a randomized, placebo-controlled, double-blind design to assess therapeutic efficacy in acute inflammatory disorders and in animals with orthopaedic conditions. In a preliminary pharmacokinetic investigation in six horses mean elimination half-life was 1.7 h after i.v. administration. In the first clinical study, analgesic activity on pain-related lameness was determined in a total of 64 horses. Pain was assessed using a rating scale. Compared with the placebo treatment, Eltenac produced significant pain relief after a single i.v. injection for a period of 24 h. In the second trial the anti-oedematous effect was determined in post-operative wound swelling following castration in two groups of 10 colts. After surgery, the horses received either an injection of 1 mg/kg Eltenac or a placebo injection on three consecutive days. Swelling was assessed by measuring the diameter of the external preputial fold using two methods: callipers and a rating scale of 0 to 3. Additionally, photographs were taken on days 1, 2 and 4. Compared with the placebo treatment, Eltenac inhibited pain and swelling significantly. The effect was maintained for up to 48 h after the last injection.
Effect of Eltenac in horses with induced endotoxaemia
Equine Vet J Suppl 2000 Jun;(32):26-31.PMID:11202378DOI:10.1111/j.2042-3306.2000.tb05330.x.
Ten horses were used in a crossover study to evaluate the effectiveness of Eltenac against endotoxaemia. Eltenac (0.5 mg/kg bwt) or saline control was given i.v. then 15 min later, intravenous infusion of endotoxin was begun and continued for 120 min (total dose 100 ng/kg bwt). Horses were monitored for heart and respiratory rates, pulmonary and carotid arterial pressure and core body temperature. Blood was sampled at intervals for measurement of haematological variables and plasma concentrations of lactate, prostanoid metabolites, tumour necrosis factor (TNF) and stress hormones. In comparison with saline-treatment, use of Eltenac significantly protected against endotoxin-induced changes in respiratory rate, core temperature, systemic arterial blood pressure (SAP), pulmonary arterial pressure, PCV, and plasma protein, 6-keto prostaglandin F1 alpha, thromboxane B2, epinephrine, and cortisol concentrations. Despite statistical effect of Eltenac on SAP, values in both treatment groups remained well above baseline throughout the evaluation period. Significant protective effect of Eltenac was not found for heart rate, white blood cell count, plasma lactate concentration or TNF activity. On the basis of these results, it is expected that use of Eltenac will provide clinical benefit in horses with naturally occurring endotoxaemia.
Efficacy and safety of Eltenac gel in the treatment of knee osteoarthritis
Osteoarthritis Cartilage 2001 Apr;9(3):273-80.PMID:11300751DOI:10.1053/joca.2000.0385.
Objective: A double-blind, placebo-controlled dose-finding study was performed in 237 patients with predominantly unilateral knee osteoarthritis (OA) evaluating efficacy and safety of a new topical NSAID. Design: The patients applied 3 g tid Eltenac gel 0.1%, 0.3%, 1% or placebo gel over a period of 4 weeks. The patients were supplied with paracetamol tablets as an escape analgesic. Primary efficacy end-point was mean global pain in the week preceding the examinatio ns, evaluated on a visual analog scale (VAS). Secondary criteria were Lequesne's score ISK, Jezek score, muscle strength and dolorimeter measurements, walking time, clinical examination results of the knee joint and patient's and investigator's overall efficacy estimates. Results: The graphical depiction of VAS and ISK suggested a dose-related efficacy, but the pre-planned statistical analysis did not show significant differences between treatments. In the patient subgroup with a higher degree of baseline severity of knee OA the ISK showed significant and relevant advantages of Eltenac gel 1% to placebo at different examination times. Two patients each of the Eltenac gel 1% group and the placebo group showed local intolerance reactions which subsided spontaneously. Conclusion: This study did not provide confirmatory proof of an efficacy of topical Eltenac in patients with knee OA. Methodological pitfalls and possible responder subgroups are described. Despite the difficulties, dose-finding studies seem to be feasible even with topical NSAIDs.
Determination of an effective dose of Eltenac and its comparison with that of flunixin meglumine in horses after experimentally induced carpitis
Am J Vet Res 1997 Mar;58(3):298-302.PMID:9055978doi
Objectives: To titrate a clinically effective Eltenac dosage (0.1, 0.5, and 1.0 mg/kg of body weight), compared with vehicle only, and to compare efficacy of the most effective Eltenac dosage with that of 1.1 mg of flunixin meglumine/kg. Animals: 40 healthy horses, ranked after model induction on the basis of lameness severity, were randomly assigned to 5 treatment groups, with 4 replicates of 10 horses each. Procedure: On day -5, after surgical preparation of the left carpal region, 0.7 ml of Freund's complete adjuvant was injected into the intercarpal space. Horses were observed daily, from the day of carpitis induction to day 0, when stride length was used as the method of ranking horses for randomization to treatment assignment. Treatments were administered i.v. once daily for 3 consecutive days, starting on day 0. Prior to carpitis induction on day -5, and at time 0 (pretreatment), 2, 4, 12, 24, 36, 48, 60, 72, and 96 hours after treatment initiation, resting respiratory rate and pulse, rectal temperature, carpal circumference, carpal flexion angle, stride length, carpal hyperthermia, and signs of carpal pain were recorded. Results: Compared with the vehicle and 0.1 mg of Eltenac/kg, 0.5 and 1.0 mg/kg caused statistically significant improvements (ie, reduction of carpal circumference, increase in carpal flexion angle, and increase in stride length of the affected limb), but values did not differ significantly between the 2 dosages. Thus, a dose-response plateau for Eltenac was reached at 0.5 mg/kg. Comparison with flunixin meglumine at a dosage of 1.1 mg/kg did not indicate significant differences between the 2 treatment groups at the pivotal time of 96 hours for carpal circumference, carpal flexion angle, stride length, carpal hyperthermia, and signs of carpal pain. Adverse reactions were not observed. Clinical relevance: Under conditions of this study, a dosage plateau for Eltenac was determined (0.5 mg/kg) that was statistically equivalent to Eltenac (1.0 mg/kg) and flunixin meglumine (1.1 mg/kg) in a 3-day i.v. dosing regimen.
Characterization of Eltenac and novel COX-2 selective thiopheneacetic acid analogues in vitro and in vivo
Biochem Pharmacol 2008 Sep 15;76(6):717-25.PMID:18674517DOI:10.1016/j.bcp.2008.06.025.
We assessed the effect of novel selective thiopheneacetic acids on cyclooxygenase isoenzymes in vitro and in vivo. Thiopheneacetic acid Eltenac and derivatives were investigated in this study. In human whole blood experiments these derivatives were potent inhibitors of COX-2 (IC(50)=0.02-0.4 microM) with less pronounced effect on COX-1 (IC(50)=0.15-5.6 microM). With COX-1/COX-2 ratios between 7.5- and 16-fold they are in the range of Celecoxib (13-fold). The parent drug Eltenac demonstrated no selectivity for COX-2. In a rat paw edema model, these compounds showed reduction of edema volume in the range of 36-45% at 10 mg/kg (Eltenac 52%, Diclofenac 51%). However, the compounds were superior to Diclofenac and Eltenac with respect to their ulcerogenic and gastrointestinal properties. Introduction of a nitrate-ester moiety to either Eltenac or a derivative did neither improve selectivity or potency in vitro, nor ulcerogenicity in vivo. Molecular modeling of selective thiopheneacetic acid derivatives to the active site of human COX-2 suggested similar binding properties as Lumiracoxib and Diclofenac. In summary, modification of Eltenac generates moderately selective COX-2 drugs in the range of Celecoxib with respect to potency and selectivity. The drugs showed potent anti-inflammatory properties and significant improvement of animal survival in a sub-chronical experimental set up. Thiopheneacetic derivatives are characterized by low pK(a) values, short microsomal half-lives and binding mode to COX-2 similar to Diclofenac and Lumiracoxib. These properties may also have an impact on the transient inhibition of COX-2-dependent prostacyclin, thereby being less associated with vascular complications.