| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g | |||
| Other Sizes |
Purity: =99.63%
| Targets |
Imrecoxib targets cyclooxygenase 2 (COX-2), an enzyme responsible for the production of prostaglandins in response to inflammation. By selectively inhibiting COX-2, Imrecoxib reduces the production of prostaglandins, thereby decreasing pain and inflammation. It has anti-inflammatory effect. Its selectivity for COX-2 over COX-1 may reduce the risk of gastrointestinal side effects associated with non-selective NSAIDs.
|
|---|---|
| ln Vitro |
In U937 cells, imrecoxib (BAP-909) (0.1–10 µM; 24 hours) dose-dependently lowers COX-2 mRNA levels generated by PMA+LPS [1].
Imrecoxib is a selective cyclooxygenase 2 (COX-2) inhibitor with anti-inflammatory effect. Its activity has been confirmed in various in vitro and in vivo studies. It has been used in trials studying the treatment of knee osteoarthritis. It is indicated for the relief of pain symptoms of osteoarthritis. |
| ln Vivo |
Irecoxib (BAP-909) (gastrointestinal administration; 5-20 mg/kg; 1 hour before carrageenan injection) can decrease carrageenan-induced acute inflammation, with the strongest inhibitory effect at 4 hours [1]. Imrecoxib (BAP-909) (GI; 5-20 mg/kg; starting on day 7; day 26) decreases secondary paw swelling and prevents heat-inactivated BCG-induced inflammatory polyarthritis [ 1].
Imrecoxib has been used in trials studying the treatment of knee osteoarthritis. It is indicated for the relief of pain symptoms of osteoarthritis, applicable to men and women without fertility requirements during treatment. It has been evaluated in preclinical studies for its anti-inflammatory effects. |
| Enzyme Assay |
The primary in vitro assay for Imrecoxib is a COX-2 enzyme activity assay using purified COX-2. The enzyme is incubated with arachidonic acid, and the production of prostaglandins is measured in the presence of the compound. The IC50 for COX-2 inhibition is determined. The selectivity for COX-2 over COX-1 is assessed using COX-1 in parallel assays.
|
| Cell Assay |
RT-PCR[1]
Cell Types: U937 Cell Tested Concentrations: 0.1 µM; 1µM; 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished COX-2 mRNA levels. In vitro cellular experiments for Imrecoxib involve treating inflammatory cells, such as macrophages, with the compound and measuring its effects on prostaglandin production and inflammatory cytokine expression. The inhibition of PGE2 production is measured by ELISA. The effects on COX-2 expression and activity are assessed. |
| Animal Protocol |
Animal/Disease Models: Rat carrageenan edema model [1]
Doses: 5 mg/kg, 10 mg/kg, 20 mg/kg Administration route: gastrointestinal administration; 5-20 mg/kg; carrageenan injection Results in the first 1 hour: Different doses can inhibit the edema reaction. Animal/Disease Models: Rat adjuvant-induced arthritis (AIA) model [1] Doses: 5 mg/kg, 10 mg/kg, 20 mg/kg Route of Administration: gastrointestinal administration; 5-20 mg/kg; Starting on day 7; day 26 Experimental Results: 10 and 20 mg/kg doses inhibited adjuvant-induced chronic inflammation. In vivo animal experiments for Imrecoxib have been conducted in models of acute inflammation, where it was administered orally at doses of 5, 10, and 20 mg/kg. Its effects on inflammation are assessed. It could also be evaluated in animal models of osteoarthritis or other inflammatory conditions to assess its efficacy in reducing pain and inflammation. |
| ADME/Pharmacokinetics |
Imrecoxib has a molecular weight of 369.48 and a molecular formula of C21H23NO3S. It is also known as BAP-909. The compound has a CAS number of 395683-14-4. It is a selective COX-2 inhibitor. It has a purity of 98%.
|
| Toxicity/Toxicokinetics |
Imrecoxib is a research compound that is not intended for human use. Its toxicological profile is characteristic of COX-2 inhibitors. Common adverse effects may include gastrointestinal disturbances, cardiovascular effects, and renal effects. Its safety has been evaluated in clinical trials for the treatment of knee osteoarthritis.
|
| References | |
| Additional Infomation |
Imexicob has been used in trials investigating the treatment of knee osteoarthritis.
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with anti-inflammatory effect. It has been used in trials studying the treatment of knee osteoarthritis. It is indicated for the relief of pain symptoms of osteoarthritis. Imrecoxib has a molecular weight of 369.48 and a molecular formula of C21H23NO3S. |
| Molecular Formula |
C21H23NO3S
|
|---|---|
| Molecular Weight |
369.479
|
| Exact Mass |
369.139
|
| CAS # |
395683-14-4
|
| PubChem CID |
11682175
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
604.1±55.0 °C at 760 mmHg
|
| Flash Point |
319.1±31.5 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.590
|
| LogP |
3.57
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
26
|
| Complexity |
645
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AXMZZGKKZDJGAZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H23NO3S/c1-4-13-22-14-19(16-9-11-18(12-10-16)26(3,24)25)20(21(22)23)17-7-5-15(2)6-8-17/h5-12H,4,13-14H2,1-3H3
|
| Chemical Name |
4-(4-methylphenyl)-3-(4-methylsulfonylphenyl)-1-propyl-2H-pyrrol-5-one
|
| Synonyms |
BAP909 BAP 909 BAP-909
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~270.65 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 5.4130 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA