| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
In CHO cells transfected stably with human COX isoenzyme, SC57666 inhibits COX2 with an IC50 of 3.2±0.8 nM and a selectivity 1000 times greater than that of COX1 (IC50=6000±1900 nM) [2].
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| ln Vitro |
In CHO cells transfected stably with human COX isoenzyme, SC57666 inhibits COX2 with an IC50 of 3.2±0.8 nM and a selectivity 1000 times greater than that of COX1 (IC50=6000±1900 nM) [2].
In CHO cells stably transfected with human COX isozymes, SC57666 inhibited arachidonic acid-dependent PGE₂ production with an IC₅₀ of 3.2 ± 0.8 nM for COX-2 and 6000 ± 1900 nM for COX-1, representing a selectivity ratio (COX-1/COX-2) of approximately 2000-fold. [2] In a human whole blood assay for COX-2 (LPS-induced PGE₂ production), the IC₅₀ value for SC57666 is not provided, but it is mentioned as one of the compounds for which more sensitive assays are required to discriminate their relative effects on COX-1. [2] In human platelets stimulated by calcium ionophore A23187, SC57666 inhibited COX-1 mediated TXB₂ production with an IC₅₀ of 2.1 ± 0.2 μM. [2] In a sensitive assay using U937 cell microsomes at a low arachidonic acid concentration (0.1 μM), SC57666 inhibited COX-1 activity with an IC₅₀ of approximately 3300 nM. [2] |
| ln Vivo |
An adjuvant-induced arthritis model has demonstrated the oral activity of SC57666 (ED50=1.7 mpk). Intragastrically given SC57666 for 5 hours at 600 mpk, no gastric damage was seen in the mice. The administration of SC57666 orally to rats at 200 mpk for 72 hours did not result in any intestinal harm [1].
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| References |
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| Additional Infomation |
SC-57666 is a stilbene compound. SC57666 (1-[2-(4-fluorophenyl)cyclopenten-1-yl]-4-(methanesulfonyl)benzene) is described as a selective cyclooxygenase-2 (COX-2) inhibitor belonging to a new class of 1,2-diarylcyclopentene compounds. In this study, it was used as a reference compound to compare the biochemical and pharmacological properties of various COX inhibitors. [2] In the COX-1 assay of U937 cell microsomes, the potency order of the various inhibitors was: diclofenac > indomethacin ~ naproxen > nimesulide ~ meloxicam ~ piroxicam > NS-398 ~ SC57666 > SC-58125 > CGP 28238 ~ etodoxacin > L-745,337 > DFU. [2]
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| Molecular Formula |
C18H17FO2S
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|---|---|
| Molecular Weight |
316.38978
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| Exact Mass |
316.093
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| CAS # |
158959-32-1
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| PubChem CID |
443373
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| Appearance |
White to off-white solid powder
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| LogP |
5.404
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
516
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GJGZQTGPOKPFES-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H17FO2S/c1-22(20,21)16-11-7-14(8-12-16)18-4-2-3-17(18)13-5-9-15(19)10-6-13/h5-12H,2-4H2,1H3
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| Chemical Name |
1-fluoro-4-[2-(4-methylsulfonylphenyl)cyclopenten-1-yl]benzene
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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) |
DMSO : ≥ 100 mg/mL (~316.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.90 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 25.0 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: ≥ 2.5 mg/mL (7.90 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 25.0 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 | 3.1607 mL | 15.8033 mL | 31.6066 mL | |
| 5 mM | 0.6321 mL | 3.1607 mL | 6.3213 mL | |
| 10 mM | 0.3161 mL | 1.5803 mL | 3.1607 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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