NFAT Transcription Factor Regulator |
| Catalog No.GC31934 |
NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 245747-71-1
Sample solution is provided at 25 µL, 10mM.
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NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
NFAT Transcription Factor Regulator is compound example 19. NFAT Transcription Factor Regulator inhibits IL-2 synthesis with an IC50 of 182 nM. It inhibits human and rat PBMC proliferation with IC50s of 82 and 146 nM, respectively. It is able to inhibit IL-4 and IL-5 production in human T-cell lines with similar potency to its effects on IL-2 release[1].
NFAT Transcription Factor Regulator is found to have an inhibitory potency approximately 10-fold better than that of cyclosporine. Comparable inhibitory effects on T-cell IL-2 production are obtained with NFAT Transcription Factor Regulator and cyclosporine at doses of 3.0 and 30 mg/kg, po, respectively. The efficacies achieved in monkeys in vivo for blocking T-cell cytokine production suggest that NFAT Transcription Factor Regulator has potential similar to that of cyclosporine for use in transplantation[1].
[1]. Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug 10;43(16):2975-81.
Animal experiment: | Monkey[1]Cynomolgus monkeys are bled to obtain heparinized baseline samples for measuring predrug cytokine production and then briefly intubated for intragastric dosing. Cyclosporine is administered in the Neoral formulation. Compound 19 is given. Postdrug blood samples are similarly obtained 2 h later. The samples are stimulated by spiking undiluted blood with PMA (50 ng/mL) and ionomycin (1µg/mL) and incubating for 24 h. Plasma samples are collected by centrifugation, and IL-2 concentrations are determined by ELISA using recombinant human IL-2 as standard[1]. |
References: [1]. Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug 10;43(16):2975-81. | |
| Cas No. | 245747-71-1 | SDF | |
| Canonical SMILES | O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3OC(F)F)C=C2 | ||
| Formula | C17H10F6N4O2 | M.Wt | 416.28 |
| Solubility | DMSO : ≥ 150 mg/mL (360.33 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4022 mL | 12.0111 mL | 24.0223 mL |
| 5 mM | 0.4804 mL | 2.4022 mL | 4.8045 mL |
| 10 mM | 0.2402 mL | 1.2011 mL | 2.4022 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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