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| 10mg |
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| 50mg |
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| 100mg |
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SC-236 is a novel, oral and potent inhibitor of COX-2 (IC50 = 10 nM) and a PPARγ agonist with anti-inflammatory and potent antimetastatic activity.
| ln Vitro |
NSAID reactions are inhibited and vEC factors are prevented in ALSS by SC-236 (15 μM, 30 minutes) [1]. In HSCs, SC-236 strongly upregulates the expression of PPARγ and modulates the luciferase reporter gene. In a manner that affects both time and concentration, SC-236 potently suppresses macrophage activity [2]. Using an activation assay, SC-236 functions as a strong PPARγ agonist in cultured HSCs either by itself or in conjunction with 15d-PGJ2 [2]. SC-236 controls AP-1 signaling to affect tumor transduction [3].
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| ln Vivo |
SC-236 (6 mg/kg, gavage) exhibits anti-fibrotic properties in CCl4-treated animals [2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: vECs. Induces significant pro-inflammatory effects[2]. Tested Concentrations: 15 μM Incubation Duration: 30 minutes. Experimental Results: COX-2 levels were Dramatically diminished and IκBα levels were increased, thereby preventing ALSS-induced NFκB activation and inflammation in vECs. Western Blot Analysis[2] Cell Types: COS 7 cells. Tested Concentrations: 3 and 10 μM. Incubation Duration: 18 hrs (hours) (combined with 15d-PGJ2). Experimental Results: Acts as a PPARγ agonist in a concentration-dependent manner. |
| Animal Protocol |
Animal/Disease Models: 76 male adult Wistar rats, weighing 200-220 g (CCl4 treatment) [2] ].
Doses: 6 mg/kg. Route of Administration: Orally, 3 times a week. Experimental Results: Immunohistochemistry detected significant induction of COX-2 protein expression in the liver of CCl4-treated rats. Dramatically reduce the degree of liver fibrosis. α-SMA expression was Dramatically inhibited in CCl4-treated rats. |
| ADME/Pharmacokinetics |
Biological Half-Life
Long plasma half-life. |
| References |
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| Additional Infomation |
SC-236 is a potent, selective, orally active inhibitor of cyclooxygenase-2 (COX-2) that has been studied in cancer therapy, lower back pain, and inflammation,,,.
Mechanism of Action This drug is a selective inhibitor of the COX-2 enzyme,. COX-2 is expressed in the brain, in the kidney, in bone, and likely in the female reproductive system. Its expression at other sites is increased during inflammation, experimentally, in response to mitogenic stimuli. Growth factors, phorbol esters, and interleukin (IL)-1 stimulate the expression of COX-2 in fibroblasts, while endotoxin serves the same function in monocytes/macrophages. SC-236 works also directly through suppressing the nuclear translocation of RelA/p65, a transcription factor. SC-236 directly targets proteins that facilitate the nuclear translocation of NF-κB, an inflammatory signaling pathway,. |
| Molecular Formula |
C16H11CLF3N3O2S
|
|---|---|
| Molecular Weight |
401.78
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| Exact Mass |
401.021
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| CAS # |
170569-86-5
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| PubChem CID |
9865808
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
543.4±60.0 °C at 760 mmHg
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| Flash Point |
282.4±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.625
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| LogP |
4.32
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
583
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NSQNZEUFHPTJME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11ClF3N3O2S/c17-11-3-1-10(2-4-11)14-9-15(16(18,19)20)22-23(14)12-5-7-13(8-6-12)26(21,24)25/h1-9H,(H2,21,24,25)
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| Chemical Name |
4-[5-(4-chlorophenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
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| Synonyms |
SC236 SC 236 SC-236
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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 (~248.89 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.22 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 (6.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4889 mL | 12.4446 mL | 24.8892 mL | |
| 5 mM | 0.4978 mL | 2.4889 mL | 4.9778 mL | |
| 10 mM | 0.2489 mL | 1.2445 mL | 2.4889 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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