| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
NFAT Inhibitor-2 targets the calcineurin-NFAT signaling pathway. Calcineurin is a serine/threonine protein phosphatase that is activated by Ca2+ and calmodulin. Activated calcineurin dephosphorylates nuclear factor of activated T-cells (NFAT) transcription factors, allowing them to translocate to the nucleus and regulate gene expression. NFAT signaling plays a central role in immune cell activation, differentiation, and cytokine production. By inhibiting calcineurin NFAT signaling, NFAT Inhibitor-2 blocks NFAT-mediated gene expression, modulating immune responses, inflammation, and cell proliferation.
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| ln Vitro |
In vitro, NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signaling. In cell-based assays, the compound inhibits NFAT-mediated transcriptional activity, as measured by NFAT-responsive reporter gene assays. Its activity is concentration-dependent, with effective concentrations typically in the nanomolar to micromolar range. The compound's inhibition of calcineurin NFAT signaling makes it a valuable tool for studying immune cell function, inflammation, and cell proliferation. It may be used for studying inflammatory diseases, autoimmune diseases, cardiovascular diseases, neurodegenerative diseases, and other conditions involving dysregulated NFAT signaling.
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| ln Vivo |
In vivo, NFAT Inhibitor-2 has been studied in preclinical models of inflammatory diseases, autoimmune diseases, and other conditions involving NFAT signaling. The compound's ability to inhibit calcineurin NFAT signaling may reduce inflammation and modulate immune responses. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying NFAT signaling and immune function. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro NFAT signaling inhibition assay for NFAT Inhibitor-2 typically uses cells transfected with an NFAT-responsive luciferase reporter construct. Cells are seeded in 96-well plates and treated with varying concentrations of the test compound (typically 0.1 nM to 10 µM) and stimulated with a calcium ionophore (e.g., ionomycin) and phorbol ester (e.g., PMA) to activate NFAT signaling. Luciferase activity is measured using a luminescence plate reader. The compound's ability to inhibit NFAT-mediated transcriptional activity is calculated, and IC50 values are determined from dose-response curves using nonlinear regression. For calcineurin activity assays, purified calcineurin enzyme is used with a phosphopeptide substrate. Positive controls (e.g., cyclosporine A, FK506) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, immune cells (e.g., T cells, B cells, macrophages) or other cell types are treated with NFAT Inhibitor-2 at concentrations ranging from 0.1 nM to 10 µM for 1-24 hours, followed by stimulation with calcium ionophore and PMA. NFAT nuclear translocation is assessed by immunofluorescence or cell fractionation followed by Western blotting. NFAT target gene expression (e.g., IL-2, TNF-α) is assessed by qRT-PCR or ELISA. Cytokine production is measured by ELISA or multiplex cytokine assay. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell proliferation is assessed by [³H]-thymidine incorporation or CFSE dilution. All experiments include appropriate controls (vehicle, known calcineurin inhibitors) and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, rodent models of inflammatory diseases (e.g., colitis, arthritis), autoimmune diseases (e.g., EAE, lupus), or transplantation are used. NFAT Inhibitor-2 is administered orally or intraperitoneally at doses ranging from 1 to 50 mg/kg, typically once or twice daily, for 7-28 days. Disease severity is assessed by clinical scoring, histology, and measurement of inflammatory markers. Immune cell populations and cytokine levels are assessed in blood and tissues. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of NFAT Inhibitor-2 have been partially characterized. The compound has a molecular weight of 446.47 and a molecular formula of C22H20F2N2O4S. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-3 hours. Plasma half-life is estimated to be 4-8 hours. The compound distributes into tissues including immune organs (spleen, lymph nodes). Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of NFAT Inhibitor-2 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signaling. It is used to study inflammatory diseases, autoimmune diseases, cardiovascular diseases, and neurodegenerative diseases. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use only. Its inhibition of calcineurin NFAT signaling makes it a valuable tool for studying immune function, inflammation, and cell proliferation.
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| Molecular Formula |
C22N2O4F2SH20
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| Molecular Weight |
446.467
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| Exact Mass |
446.111
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| CAS # |
422546-87-0
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| PubChem CID |
15995931
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
694
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(C(NC2C=CC(C)=C(F)C=2)=O)=CC=1S(=O)(=O)NCC1C=CC(OC)=CC=1
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| InChi Key |
UILNVCFXMNSVLA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20F2N2O4S/c1-14-3-7-17(12-20(14)24)26-22(27)16-6-10-19(23)21(11-16)31(28,29)25-13-15-4-8-18(30-2)9-5-15/h3-12,25H,13H2,1-2H3,(H,26,27)
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| Chemical Name |
4-fluoro-N-(3-fluoro-4-methylphenyl)-3-[(4-methoxyphenyl)methylsulfamoyl]benzamide
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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 : ~125 mg/mL (~279.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.66 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 20.8 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: ≥ 2.08 mg/mL (4.66 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 20.8 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 | 2.2398 mL | 11.1990 mL | 22.3979 mL | |
| 5 mM | 0.4480 mL | 2.2398 mL | 4.4796 mL | |
| 10 mM | 0.2240 mL | 1.1199 mL | 2.2398 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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