Imrecoxib
(Synonyms: 艾瑞昔布; BAP-909) 目录号 : GC36305
Imrecoxib（BAP-909）艾瑞昔布是选择性环氧合酶 2 (COX-2) 抑制剂，IC50 值为 18 nM，也可以抑制 COX1 活性，IC50 值为 115 nM。Imrecoxib（BAP-909) 艾瑞昔布具有抗炎作用。
Cas No.:395683-14-4
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
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect[1]. Human COX-1|115 nM (IC50)|Human COX-2|18 nM (IC50)
Imrecoxib (BAP-909) (0.1-10 µM; 24 hours) decreases COX-2 mRNA level induced by PMA+LPS at a dose dependent manner in U937 cells[1]. RT-PCR[1] Cell Line: U937 cells
Imrecoxib (BAP-909) (gastrointestinal administration; 5-20 mg/kg; 1 hour before carrageenan injection) inhibits carrageenan-induced acute inflammation, and the inhibitory effect is maximal at 4 hours[1].Imrecoxib (BAP-909) (gastrointestinal administration; 5-20 mg/kg; started on day 7; 26 days) diminishes the secondary paw swelling and inhibits heat-inactivated BCG induced-inflammtory polyarthritis[1]. Animal Model: Rat carrageenan-induced edema model[1]
[1]. Chen XH, et al. Imrecoxib: a novel and selective cyclooxygenase 2 inhibitor with anti-inflammatory effect. Acta Pharmacol Sin. 2004 Jul;25(7):927-31.
| Cas No. | 395683-14-4 | SDF | |
| 别名 | 艾瑞昔布; BAP-909 | ||
| Canonical SMILES | O=C1N(CCC)CC(C2=CC=C(S(=O)(C)=O)C=C2)=C1C3=CC=C(C)C=C3 | ||
| 分子式 | C21H23NO3S | 分子量 | 369.48 |
| 溶解度 | DMSO: 100 mg/mL (270.65 mM) | 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 | 2.7065 mL | 13.5325 mL | 27.0651 mL |
| 5 mM | 0.5413 mL | 2.7065 mL | 5.413 mL |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 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。
Inhibition of Imrecoxib on mRNA and protein expression of CYP2C11 enzyme in rats
Biomed Chromatogr 2022 Oct;36(10):e5439.PMID:35778888DOI:10.1002/bmc.5439.
To evaluate the effect of Imrecoxib on CYP2C11 enzyme activity, mRNA, and protein expression, a UPLC method was established. Tolbutamide was selected as the CYP2C11 enzyme-specific probe drug and incubated with Imrecoxib in rat liver microsomes. The yield of 4-hydroxytolbutamide was measured using UPLC to investigate the effect of Imrecoxib on CYP2C11 enzyme activity. Imrecoxib (10 mg/kg) was administered intragastrically twice daily. After 1, 7, and 14 days of administration, the liver tissues were analyzed. The expression of CYP2C11 enzyme mRNA was determined using reverse transcription-polymerase chain reaction, and its protein expression was determined using Western blot analysis. Imrecoxib concentration was inversely proportional to the production of 4-hydroxytolbutamide in liver microsomes. Imrecoxib demonstrated a dose-dependent inhibitory effect on CYP2C11 activity with IC50 = 74.77 μM. After administration, reverse transcription-polymerase chain reaction showed CYP2C11 enzyme mRNA expressions were 65% (P < 0.05), 35%, and 34% of the control group, respectively (P < 0.01). Western blot analysis showed CYP2C11 enzyme protein expressions were 80, 37, and 34% of the control group, respectively (P < 0.01). Imrecoxib can reduce mRNA and protein expression of CYP2C11 enzyme in rat liver and inhibit the activity of CYP2C11 enzyme in a dose-dependent manner. However, it does not produce clinically significant drug interactions.
Imrecoxib Inhibits Paraquat-Induced Pulmonary Fibrosis through the NF- κ B/Snail Signaling Pathway
Comput Math Methods Med 2020 Oct 13;2020:6374014.PMID:33123215DOI:10.1155/2020/6374014.
Objective: In recent years, pulmonary fibrosis caused by paraquat poisoning is still concerned. However, no effective drugs have been developed yet to treat paraquat-induced pulmonary fibrosis. The aim of our research is to investigate whether Imrecoxib can inhibit paraquat-induced pulmonary fibrosis and its possible mechanism. Methods: Extraction of primary pulmonary fibrosis cells (PPF cells) in vitro by the method of trypsin digestion. RT-qPCR and western blot were employed to measure the transcription level and protein expression of EMT related markers in paraquat-induced A549 cells. MTT, wound-healing, and Transwell experiments were used to verify the effect of Imrecoxib on the proliferation, migration, and invasion of PPF and HFL1 cells. Results: Firstly, our results confirmed that paraquat can induce EMT and activate the NF-κB/snail signal pathway in lung epithelial cell A549. Furthermore, experimental results showed that Imrecoxib could repress the proliferation, migration, and invasion of PPF and HFL1 cells. Finally, our study found that Imrecoxib can inhibit EMT of paraquat-induced A549 cells by the NF-κB/snail signal pathway. Conclusion: Imrecoxib can inhibit EMT of paraquat-induced A549 cells and alleviate paraquat-caused pulmonary fibrosis through the NF-κB/snail signal pathway. Therefore, Imrecoxib is a drug worthy of study in the treatment of paraquat-induced pulmonary fibrosis.
Imrecoxib versus celecoxib as postoperative analgesia for patients receiving arthroscopic knee surgery: a randomized, controlled, non-inferiority study
Inflammopharmacology 2022 Jun;30(3):875-881.PMID:35445990DOI:10.1007/s10787-022-00938-8.
Objective: Imrecoxib is a novel cyclooxygenase-2 inhibitor independently developed in China, which exhibits a good efficacy and tolerance in orthopedic disorders. The current study aimed to further compare its efficacy and safety with celecoxib as postoperative analgesia in arthroscopic knee surgery (AKS). Methods: Patients receiving AKS were enrolled and randomly assigned to Imrecoxib (n = 64) and celecoxib (n = 62) group to receive analgesia for 72 h after surgery. Pain at rest and movement, pethidine consumption, patient's satisfaction, Lysholm score, and adverse events were assessed after AKS. Meanwhile the upper limit of 95% CI of pain-score mean difference (MD) between Imrecoxib and celecoxib was calculated, then, the non-inferiority was defined if the all-time-point upper limits of 95% CI less than 1. Results: Imrecoxib was non-inferior to celecoxib for alleviating pain at rest (upper limit of 95% CI of MD ranging from 0.443 to 0.782, all time-point values less than 1); as well as for attenuating pain at movement (upper limit of 95% CI of MD ranging from 0.398 to 0.582, all time-point values less than 1). Moreover, rescue analgesia rate (P = 0.583), pethidine consumption (P = 0.454), patient's satisfaction at 72 h (P = 0.408), and Lysholm score at M3 (P = 0.776) were of no difference between Imrecoxib group and celecoxib group. Additionally, the main adverse events in two groups were nausea (P = 0.425), constipation (P = 1.000), vomiting (P = 0.715), headache (P = 1.000), and dizziness (P = 0.667), which were mild and manageable. Conclusion: Imrecoxib is non-inferior to celecoxib in postoperative analgesia and exhibits an acceptable tolerance in patients undergoing AKS.
Cost-utility analysis of Imrecoxib compared with diclofenac for patients with osteoarthritis
Cost Eff Resour Alloc 2021 Apr 20;19(1):22.PMID:33879168DOI:10.1186/s12962-021-00275-7.
Background: To estimate the cost -utility of Imrecoxib compared with diclofenac, as well as the addition of a proton pump inhibitor to both two treatment strategies, for patients with osteoarthritis, from a Chinese healthcare perspective. Methods: A Markov model was built. Costs of managing osteoarthritis and initial adverse events were collected from a Medical Database which collected information from 170 hospitals. Other parameters were obtained from the literature. Subgroup analyses were conducted for people at high risk of gastrointestinal or cardiovascular adverse events. Deterministic and probabilistic sensitivity analyses were performed. Results: Imrecoxib was highly cost-effective than diclofenac (the ICER was $401.58 and $492.77 in patients at low and high gastrointestinal and cardiovascular risk, respectively). The addition of a proton pump inhibitor was more cost -effective compared with single drug for both treatment strategies. Findings remained robust to sensitivity analyses. 59.04% and 57.16% probability for the co-prescription of Imrecoxib and a proton pump inhibitor to be the most cost-effective strategy in all patients considered using the cost-effectiveness threshold of $30,000. Conclusions: The addition of a proton pump inhibitor to both Imrecoxib and diclofenac was advised. Imrecoxib provides a valuable option for patients with osteoarthritis. Uncertainties existed in the model, and the suggestions can be adopted with caution.
Cost-utility analysis of Imrecoxib compared with celecoxib for patients with osteoarthritis
Ann Transl Med 2021 Apr;9(7):575.PMID:33987273DOI:10.21037/atm-21-290.
Background: The objective of this study is to compare the long-term cost-utility of Imrecoxib and celecoxib for patients with osteoarthritis (OA) from the perspective of the Chinese healthcare system. Methods: An economic model was built based on the model from the National Institute for Health and Care Excellence (NICE). The simulation was carried out initially for 100 cycles of 3 months each, starting with 10,000 patients. A discount rate of 5% was applied both for cost and utility. Quality-adjusted life years (QALYs) were adopted as the utility indicator, and real-world data from the hospital information systems of 170 hospitals was collected to indicate cost. The relative incidence rates of adverse events (AEs) with Imrecoxib and celecoxib were collected from randomized controlled trials. Sensitivity analysis was performed to validate the robustness of the model. Results: In the base case analysis (6-month treatment duration, 55 years old and above), Imrecoxib was the more cost-effective option compared to celecoxib, with an incremental cost-effectiveness ratio (ICER) of $3,041.14. This finding remained unchanged after varying the treatment duration and the age of the patients. The main drivers of the results were the relative incidence of myocardial infarction (MI), the cost of Imrecoxib, and the utility of OA patients without any AEs. Probability sensitivity analysis (PSA) showed that there was a 59.02% probability of Imrecoxib as the more cost-effective option, with a threshold of $30,000. Conclusions: Although there were uncertainties, Imrecoxib was the more cost-effective option compared to celecoxib, with a definite possibility. Due to the limitations of the original model and this study, the results of this study should be adopted with caution.