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| 250mg |
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Purity: ≥98%
Celecoxib (formerly SC58635; YM-177; SC-58635; YM 177; trade name Celebrex; Xilebao), an anti-inflammatory agent of the NSAID class, is a potent and selective COX-2 inhibitor of the non-steroidal anti-inflammatory drug (NSAID) class with an IC50 of 40 nM in Sf9 cells. In vitro, celecoxib not only reduced the production of PGE2 but also inhibited the downstream effects of PGE2. Celecoxib blocked migration and invasion of A549 cells increased by PGE2 in the wound healing and transwell assays.
| ln Vitro |
Celecoxib (10-75 μM), a selective cyclooxygenase-2 (COX-2) inhibitor, suppresses nasopharyngeal cancer cell line proliferation in a dose-dependent manner. In NPC cell lines, celecoxib (25 and 50 μM) caused apoptosis and cell cycle arrest at the G0/G1 checkpoint, which was linked to a notable reduction in STAT3 phosphorylation. Genes downstream of STAT3, including Survivin, Mcl-1, Bcl-2, and Cyclin D1, were markedly downregulated following exposure to Celecoxib (25 and 50 μM) [2]. Celecoxib, which targets the transcriptional target cyclooxygenase 2 (COX-2), reduces the growth and carcinogenesis of NF2 mutant cells [6]. Combining TTNPB (3 μM) with celecoxib (5 μM, 28 days) causes fibroblasts to become articular chondrocytes [7]. Mesenchymal cells generated from Wharton's jelly are encouraged to transdifferentiate into endothelial progenitor cells by celecoxib (10 μM, 7–14 days) [8]. Human aortic valve interstitial cells undergo transdifferentiation into myofibroblasts when exposed to celecoxib (5 μM) for 14 days [9].
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| ln Vivo |
Oral celecoxib exhibits strong anti-inflammatory properties. In an adjuvanted arthritis model, celecoxib reduces chronic inflammation with an ED50 of 0.37 mg/kg/day, and it reduces acute inflammation in the carrageenan edema test with an ED50 of 7.1 mg/kg. With an ED50 of 34.5 mg/kg, celecoxib additionally demonstrated analgesic efficacy in the Hargreaves hyperalgesia model. Despite being just as effective as conventional NSAIDs, celecoxib did not cause acute gastrointestinal toxicity in rats when administered at doses as high as 200 mg/kg. Furthermore, no chronic gastrointestinal damage was observed in rats even dosages as high as 600 mg/kg/day for 10 days [1]. Tumor weight was 66% lower in KpB mice given an obese, high-fat diet when treated with celecoxib than in control animals. Celecoxib treatment reduced tumor weight by 46% in KpB mice fed a low-fat (non-obesogenic) diet [3]. For two weeks, either an intramuscular injection of Fasudil (10 mg/kg) or oral Celecoxib (20 mg/kg) was given to the rat model. The findings demonstrate that in rats with spinal cord injury, the combination of celecoxib and facudil can dramatically reduce the expression of COX-2 and Rho kinase II surrounding the lesion site, improve the pathological morphology of the injured spinal cord, and aid in the promotion of motor function recovery [4].
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| References |
[1]. Penning TD, et al. Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib). J Med Chem. 1997
[2]. Liu DB, et al. Celecoxib induces apoptosis and cell-cycle arrest in nasopharyngeal carcinoma cell lines via inhibition of STAT3 phosphorylation. Acta Pharmacol Sin. 2012 May;33(5):682-90. [3]. Suri A, et al. The effect of celecoxib on tumor growth in ovarian cancer cells and a genetically engineered mouse model of serous ovarian cancer. Oncotarget. 2016 Apr 8. [4]. Hou XL, et al. Combination of fasudil and celecoxib promotes the recovery of injured spinal cord in rats better than celecoxib or fasudil alone. Neural Regen Res. 2015 Nov;10(11):1836-40. [5]. Liu C, et al. Celecoxib alleviates nonalcoholic fatty liver disease by restoring autophagic flux. Sci Rep. 2018 Mar 7;8(1):4108. [6]. Pobbati AV, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635. |
| Molecular Formula |
C17H14F3N3O2S
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|---|---|
| Molecular Weight |
381.37
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| CAS # |
169590-42-5
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| Related CAS # |
Celecoxib;169590-42-5;Celecoxib;169590-42-5
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])N1C(=C([H])C(C(F)(F)F)=N1)C1C([H])=C([H])C(C([H])([H])[H])=C([H])C=1[H])(N([H])[H])(=O)=O
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| Synonyms |
SC 58635; YM177. Celecoxib; SC58635; YM-177; SC-58635; YM 177; trade name Celebrex; Xilebao.
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| 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)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6221 mL | 13.1106 mL | 26.2213 mL | |
| 5 mM | 0.5244 mL | 2.6221 mL | 5.2443 mL | |
| 10 mM | 0.2622 mL | 1.3111 mL | 2.6221 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.
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