Loxoprofen
(Synonyms: 洛索洛芬) 目录号 : GC36482
An NSAID and a prodrug form of loxoprofen-SRS
Cas No.:68767-14-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Loxoprofen is a non-steroidal anti-inflammatory drug (NSAID) and prodrug form of loxoprofen-SRS.1 It inhibits COX-1 and COX-2 in isolated human whole blood (IC50s = 6.5 and 13.5 ?M, respectively). Loxoprofen reduces acetic acid-induced writhing in mice and carrageenan-induced paw edema and LPS-induced fever in rats (ED30s = 20.1, 0.7, and 2.79 mg/kg, respectively).2 Formulations containing loxoprofen have been used in the treatment of pain associated with osteoarthritis, myalgia, and post-traumatic swelling.
1.Riendeau, D., Salem, M., Styhler, A., et al.Evaluation of loxoprofen and its alcohol metabolites for potency and selectivity of inhibition of cyclooxygenase-2Bioorg. Med. Chem. Lett.14(5)1201-1203(2004) 2.Futaki, N., Yoshikawa, K., Hamasaka, Y., et al.NS-398, a novel non-steroidal anti-inflammatory drug with potent analgesic and antipyretic effects, which causes minimal stomach lesionsGen. Pharmacol.24105-110(1993)
| Cas No. | 68767-14-6 | SDF | |
| 别名 | 洛索洛芬 | ||
| Canonical SMILES | O=C1C(CCC1)CC2=CC=C(C(C)C(O)=O)C=C2 | ||
| 分子式 | C15H18O3 | 分子量 | 246.3 |
| 溶解度 | DMSO: ≥ 100 mg/mL (406.01 mM) | 储存条件 | Store at RT |
| 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 | 4.0601 mL | 20.3004 mL | 40.6009 mL |
| 5 mM | 0.812 mL | 4.0601 mL | 8.1202 mL |
| 10 mM | 0.406 mL | 2.03 mL | 4.0601 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。
Loxoprofen: A Review in Pain and Inflammation
Clin Drug Investig 2016 Sep;36(9):771-781.PMID:27444038DOI:10.1007/s40261-016-0440-9.
Loxoprofen (Loxonin(®), Loxonin(®) Pap, Loxonin(®) Tape) is a prodrug-type NSAID that is available in several formulations, including 60 mg tablets, 100 mg hydrogel patches and 50 or 100 mg tape. In active comparator-controlled trials, oral Loxoprofen therapy (ranging from 2 days to 6 weeks' duration depending on the pain type) provided analgesic efficacy that generally did not significantly differ from that of celecoxib for postoperative pain or frozen shoulder, ibuprofen for knee osteoarthritis or naproxen for lumbar pain. In double-blind, double-dummy, multicentre trials, Loxoprofen hydrogel patches were noninferior to oral Loxoprofen with regard to rates of final overall symptomatic improvement over 1-4 weeks in patients with knee osteoarthritis, myalgia or trauma-induced swelling and pain. Loxoprofen hydrogel patches were also noninferior to other commercially available patches (ketoprofen and indometacin) over 2 or 4 weeks in patients with knee osteoarthritis or myalgia in open-label studies. Oral and topical Loxoprofen were generally well tolerated in clinical trials. Thus, Loxoprofen is a useful analgesic option for patients with pain and inflammation, with topical Loxoprofen potentially reducing the risk of gastrointestinal, cardiovascular and renal complications associated with oral NSAID use.
Loxoprofen-induced bullous fixed drug eruption
J Gen Fam Med 2019 Dec 6;21(2):21-22.PMID:32161698DOI:10.1002/jgf2.288.
A 49-year-old housewife with a long-standing migraine presented with "spells" of intensely itchy, well-circumscribed, erythematous patches over the flexor aspect of her left wrist and palm repeatedly for the last 15 years. Detailed history revealed her oral Loxoprofen use for migraine headaches preceding rash development. Although a patch test was negative, inadvertent ingestion of the drug by the patient reproduced the rash within a few hours, thereby establishing the diagnosis of loxoprofen-induced bullous fixed drug eruption.
Identification of sulfonyl-loxoprofen as novel phase 2 conjugate in rat
Biopharm Drug Dispos 2019 Jul;40(7):234-241.PMID:31242324DOI:10.1002/bdd.2196.
Loxoprofen is a prodrug that exerts strong analgesic and anti-inflammatory effects through its active trans-alcohol metabolite, which is produced in the liver by carbonyl reductase. Previous metabolic studies have evaluated Loxoprofen, but its sulfate and taurine conjugates have not yet been studied. We characterized the metabolomic profile of Loxoprofen in rat plasma, urine, and feces using high-resolution mass spectrometry. We identified 17 metabolites of Loxoprofen in the three different biological matrices, 13 of which were detected in plasma and feces and 16 in urine. Amongst these metabolites, two novel taurine conjugates (M12 and M13) and two novel acyl glucuronides (M14, M15) were identified for the first time in rats. In addition, we detected three novel sulfate conjugates (M9, M10, and M11) of Loxoprofen. Further study of these metabolites of Loxoprofen is essential in order to assess their potency and toxicity.
Pharmacokinetics of Loxoprofen in a self-administered overdose in a Japanese patient admitted to hospital
J Pharm Health Care Sci 2021 Sep 7;7(1):33.PMID:34488903DOI:10.1186/s40780-021-00216-9.
Background: Loxoprofen is a propionic acid derivative and is the most widely prescribed non-steroidal anti-inflammatory drug in Japan. Loxoprofen is generally considered to be relatively nontoxic. Case presentation: A 33-year-old man (body weight, 55 kg) who intentionally took an overdose of 100 tablets of Loxoprofen (6000 mg) as a suicide attempt was emergently admitted to Kyoto Medical Center. On arrival, the patient was suffering disorders of consciousness. His plasma concentrations of Loxoprofen and its reduced trans-alcohol metabolite were 52 and 24 μg/mL, 3.7 and 2.3 μg/mL, 0.81 and 0.54 μg/mL, and 0.015 and 0.011 μg/mL, respectively, at 4, 26, 50, and 121 h after the oral overdose. The observed apparent terminal elimination half-life of Loxoprofen during days 1 and 2 of hospitalization was in the range 6-12 h, which is several times longer than the reported normal value. This finding implied nonlinearity of Loxoprofen pharmacokinetics over the current 100-fold dose range, which could affect the accuracy of values simulated by a simplified physiologically based pharmacokinetic (PBPK) model founded on data from a normal dose of 60 mg. The reasons for the delayed eliminations from plasma of Loxoprofen and its trans-alcohol metabolite in this case are uncertain, but slight renal impairment (low eGFR values) developed on the second and third hospital days and could be a causal factor. Conclusions: Because the patient's level of consciousness had gradually improved, he was discharged on the fourth day of hospitalization. The virtual plasma exposures of Loxoprofen and its reduced trans-alcohol metabolite estimated using the current simplified PBPK model were lower than the measured values in the overdose case. The present results based on drug monitoring data and pharmacokinetic predictions could serve as a useful guide in cases of Loxoprofen overdose.
Antinociception by fluoro-loxoprofen, a novel non-steroidal anti-inflammatory drug with less ulcerogenic effects, in rat models of inflammatory pain
Eur J Pharmacol 2019 Feb 5;844:253-258.PMID:30529473DOI:10.1016/j.ejphar.2018.12.008.
The use of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammatory pain is limited by gastrointestinal complications. The rapid action of NSAIDs is associated with better pain relief. Previously, we demonstrated that fluoro-loxoprofen, a novel NSAID, has less ulcerogenic potential than other NSAIDs, attributable to its gastroprotective properties. The aim of this study was to investigate and compare the effects of fluoro-loxoprofen on inflammatory pain in rats with those of other NSAIDs. Oral administration of fluoro-loxoprofen, Loxoprofen, and celecoxib resulted in equivalent analgesic action against yeast-induced inflammatory pain. The antinociceptive effect of fluoro-loxoprofen was maximized within 1 h after administration, which is less time than that observed for Loxoprofen (2 h) and celecoxib (3 h). We confirmed that both fluoro-loxoprofen and Loxoprofen suppressed the increases in prostaglandin E2 in inflamed paws. In addition to yeast-induced pain, fluoro-loxoprofen produced a similar effect against adjuvant-induced inflammatory pain, with faster peak analgesic effects than those observed for Loxoprofen and celecoxib. Taken together, these results suggest that the analgesic effect of fluoro-loxoprofen is equivalent to that of Loxoprofen and celecoxib. Moreover, the analgesic effect of fluoro-loxoprofen against inflammatory pain was more rapid than that of other NSAIDs, and this may be associated with its rapid absorption property.