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| ln Vitro |
Temacoxib (JTE-522) is a new selective cyclooxygenase (COX)-2 inhibitor. Its mechanism of action and inhibitory activity on human COX-1 and COX-2 were investigated and compared with reference drugs. Tilmacoxib inhibited yeast-expressed human recombinant COX-2 in enzymatic tests, having an IC50 of 0.085 μM. On the other hand, at doses as high as 100 μM, temacoxib did not inhibit human COX-1 that was generated from human platelets. Tilmacoxib decreased prostaglandin E2 synthesis produced by lipopolysaccharide in human peripheral blood mononuclear cells (COX-2) in a cell-based experiment (IC50=15.1 nM). Conversely, telmacoxib's ability to prevent the generation of thromboxane B2 in response to calcium ionophore in human platelets that have been cleaned (COX-1) was reduced (IC50=6.21 μM). When compared to other COX-2 inhibitors (NS-398 and SC-58635), telmacoxib shows a more specific inhibition of human COX-2. Temacoxib reduces the activity of human recombinant COX-2 in a time- and dose-dependent way [1]. A PGE2-independent mechanism also plays a role in the suppression of gastric epithelial cell proliferation by the cyclooxygenase 2 inhibitor Tilmacoxib (JTE522). While Tilmacoxib did not totally prevent the rise in cellular PGE2 concentration following the addition of arachidonic acid, the combination of Tilmacoxib and arachidonic acid produced a considerable delay in wound healing when compared with the control [2].
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| ln Vivo |
The purpose of this study was to assess temacoxib (JTE-522), a new selective cyclooxygenase 2 inhibitor, on colonic aberrant crypt lesions (ACF) caused by 1,2-dimethylhydrazine (DMH). possible qualities that prevent chemotherapy. Signs of colon cancer development in rats. A total of 80 male F344 rats were gavaged five times a week orally with a dose of 3 or 10 mg/kg body weight of temacoxib or a vehicle from the start of the experiment. A week later, the rats received four weeks of subcutaneous injections of either saline or 20 mg/kg body weight of DMH once a week. Twelve weeks after the trial began, all of the rats were killed, and the colonic ACF was measured. Total ACF/colon was considerably decreased by temacib at a dose of 10 mg/kg. In the group treated with 3 mg/kg temacoxib, no inhibitory effects were seen. The administration of 10 mg/kg temacoxib effectively prevented the development of ACF, resulting in a 30% reduction in total ACF/colon (p<0.01). Furthermore, lesions with one to three crypts formed at a considerably lower rate with 10 mg/kg temacoxib, but not with lesions with four or more crypts, according to data on crypt multiplicity. Temacoxib administered at a modest dose (3 mg/kg) did not diminish total ACF or crypt multiplicity [3].
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| References |
[1]. Wakitani K, et al. Profile of JTE-522 as a human cyclooxygenase-2 inhibitor. Jpn J Pharmacol. 1998 Nov;78(3):365-71.
[2]. Hirose M, et al. Inhibition of proliferation of gastric epithelial cells by a cyclooxygenase 2 inhibitor, JTE522, is also mediated by a PGE2-independent pathway. Aliment Pharmacol Ther. 2002 Apr;16 Suppl 2:83-9. [3]. Wei M, et al. Chemopreventive effect of JTE-522, a selective cyclooxygenase-2 inhibitor, on 1, 2-dimethylhydrazine-induced rat colon carcinogenesis. Cancer Lett. 2003 Dec 8;202(1):11-6 |
| Additional Infomation |
Tilmacoxib is a member of the class of 1,3-oxazoles that is that is 1,3-oxazole which is substituted at positions 2, 4 and 5 by methyl, cyclohexyl, and 3-fluoro-4-sulfamoylphenyl groups, respectively. It has a role as a cyclooxygenase 2 inhibitor. It is a member of 1,3-oxazoles, an organofluorine compound and a sulfonamide.
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| Molecular Formula |
C16H19FN2O3S
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| Molecular Weight |
338.39
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| Exact Mass |
338.11
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| CAS # |
180200-68-4
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| PubChem CID |
159271
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.294g/cm3
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| Boiling Point |
500.6ºC at 760mmHg
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| Flash Point |
256.5ºC
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| Vapour Pressure |
3.75E-10mmHg at 25°C
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| Index of Refraction |
1.56
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| LogP |
5.265
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
504
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=CC=C(C2=C(C3CCCCC3)N=C(C)O2)C=C1F)(N)=O
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| InChi Key |
MIMJSJSRRDZIPW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19FN2O3S/c1-10-19-15(11-5-3-2-4-6-11)16(22-10)12-7-8-14(13(17)9-12)23(18,20)21/h7-9,11H,2-6H2,1H3,(H2,18,20,21)
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| Chemical Name |
4-(4-cyclohexyl-2-methyl-1,3-oxazol-5-yl)-2-fluorobenzenesulfonamide
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| Synonyms |
RWJ-57504; JTP-19605; Tilmacoxib
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| HS Tariff Code |
2934.99.9001
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9552 mL | 14.7759 mL | 29.5517 mL | |
| 5 mM | 0.5910 mL | 2.9552 mL | 5.9103 mL | |
| 10 mM | 0.2955 mL | 1.4776 mL | 2.9552 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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