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| Targets |
SC-236 targets cyclooxygenase-2 (COX-2), an enzyme that catalyzes the conversion of arachidonic acid to prostaglandins, which are key mediators of inflammation, pain, and fever. By selectively inhibiting COX-2 with an IC50 of 10 nM, SC-236 reduces the production of pro-inflammatory prostaglandins while sparing COX-1, which is responsible for maintaining gastric mucosal integrity and platelet function. SC-236 is also a PPARγ agonist, and it inhibits AP-1 activity through JNK inhibition and exerts anti-inflammatory effects by inhibiting ERK phosphorylation.
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| 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].
In vitro, SC-236 acts as a potent and selective COX-2 inhibitor with an IC50 of 10 nM for COX-2 and selectivity over COX-1. It is also a PPARγ agonist. The compound inhibits AP-1 activity through JNK inhibition. SC-236 has been shown to inhibit the nuclear translocation of NF-κB. Its anti-inflammatory activity has been demonstrated in various in vitro models. The compound's selectivity for COX-2 over COX-1 is important for minimizing gastrointestinal side effects associated with non-selective COX inhibitors. |
| ln Vivo |
SC-236 (6 mg/kg, gavage) exhibits anti-fibrotic properties in CCl4-treated animals [2].
In vivo, SC-236 has demonstrated anti-inflammatory effects in mouse models by inhibiting ERK phosphorylation. It is orally active and has been studied for its potential in treating inflammatory conditions. The compound's COX-2 selectivity and PPARγ agonist activity suggest potential therapeutic applications in inflammation, pain, and metabolic disorders. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SC-236 are COX-1 and COX-2 inhibition assays using purified ovine or recombinant COX-1 and COX-2 enzymes. The enzyme is incubated with arachidonic acid substrate and varying concentrations of SC-236, and prostaglandin production is measured by ELISA or radiometric methods. The IC50 for inhibition of COX-1 and COX-2 activity is determined from dose-response curves to confirm selectivity. PPARγ agonist activity can be assessed using PPARγ transactivation assays.
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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. In vitro cellular assays for SC-236 are performed using various cell types, including macrophages and other inflammatory cells. Cells are treated with SC-236 and stimulated with inflammatory agents such as lipopolysaccharide (LPS). Prostaglandin E2 (PGE2) production is measured by ELISA to assess COX-2 inhibition. NF-κB activation is assessed by measuring its nuclear translocation. AP-1 activity and ERK phosphorylation are assessed by Western blotting or reporter assays. Cell viability is evaluated using MTT assays to ensure that the observed effects are not due to cytotoxicity. |
| 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. In vivo animal experiments for SC-236 are conducted in mouse models of inflammation. Mice are administered SC-236 via oral administration, and inflammation is induced using agents such as carrageenan or complete Freund's adjuvant. Edema, inflammatory cytokine levels, and leukocyte infiltration are assessed. The compound's effects on ERK phosphorylation and AP-1 activity in tissues are evaluated. These studies confirm the compound's anti-inflammatory efficacy in vivo. |
| ADME/Pharmacokinetics |
Biological half-life
Plasma has a long half-life. SC-236 has a molecular weight of 401.79 g/mol and a molecular formula of C16H11ClF3N3O2S. The compound is orally active and is soluble in DMSO and other organic solvents. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a COX-2 inhibitor, SC-236 is expected to have favorable pharmacokinetic properties for oral administration. The compound is a crystalline solid. |
| Toxicity/Toxicokinetics |
SC-236 has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. As a selective COX-2 inhibitor, SC-236 may have a reduced risk of gastrointestinal side effects compared to non-selective COX inhibitors. However, COX-2 inhibitors have been associated with cardiovascular risks, which would need to be carefully evaluated. Comprehensive toxicology studies would be necessary to fully assess the compound's safety for clinical development.
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| References |
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| Additional Infomation |
SC-236 is a potent, selective, orally administered cyclooxygenase-2 (COX-2) inhibitor that has been studied in areas such as cancer treatment, 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, kidneys, bones, and possibly the female reproductive system. During inflammation, experiments have shown that COX-2 expression increases in other sites due to mitotic stimulation. Growth factors, phorbol esters, and interleukin (IL)-1 stimulate COX-2 expression in fibroblasts, while endotoxins play the same role in monocytes/macrophages. SC-236 also acts directly by inhibiting the nuclear translocation of the transcription factor RelA/p65. SC-236 directly targets proteins that promote the nuclear translocation of the NF-κB inflammatory signaling pathway.
SC-236 is a potent, orally active, and selective COX-2 inhibitor with an IC50 of 10 nM for COX-2 and selectivity over COX-1. It is also a PPARγ agonist. SC-236 inhibits AP-1 activity through JNK inhibition and exerts anti-inflammatory effects by inhibiting ERK phosphorylation. It also inhibits the nuclear translocation of NF-κB. SC-236 is a research compound with potential applications in inflammation, pain, and metabolic disorders. |
| Molecular Formula |
C16H11CLF3N3O2S
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|---|---|
| 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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