1. Immunology/Inflammation
  2. Interleukin Related
  3. NFAT Transcription Factor Regulator-1

NFAT Transcription Factor Regulator-1 

Cat. No.: HY-112778 Purity: 98.98%
COA Handling Instructions

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.

For research use only. We do not sell to patients.

NFAT Transcription Factor Regulator-1 Chemical Structure

NFAT Transcription Factor Regulator-1 Chemical Structure

CAS No. : 245747-71-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 192 In-stock
Solution
10 mM * 1 mL in DMSO USD 192 In-stock
Solid
1 mg USD 83 In-stock
5 mg USD 175 In-stock
10 mg USD 295 In-stock
50 mg USD 880 In-stock
100 mg USD 1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC50 of 182 nM.

IC50 & Target[1]

IL-2

182 nM (IC50)

In Vitro

NFAT Transcription Factor Regulator-1 (compound example 19) inhibits IL-2 synthesis with an IC50 of 182 nM. NFAT Transcription Factor Regulator-1 inhibits human and rat PBMC proliferation with IC50s of 82 and 146 nM, respectively. NFAT Transcription Factor Regulator-1 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NFAT Transcription Factor Regulator-1 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-1 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-1 has potential similar to that of cyclosporine for use in transplantation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

416.28

Formula

C17H10F6N4O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3OC(F)F)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (12.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (12.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.37%

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4022 mL 12.0111 mL 24.0223 mL 60.0557 mL
5 mM 0.4804 mL 2.4022 mL 4.8045 mL 12.0111 mL
10 mM 0.2402 mL 1.2011 mL 2.4022 mL 6.0056 mL
15 mM 0.1601 mL 0.8007 mL 1.6015 mL 4.0037 mL
20 mM 0.1201 mL 0.6006 mL 1.2011 mL 3.0028 mL
25 mM 0.0961 mL 0.4804 mL 0.9609 mL 2.4022 mL
30 mM 0.0801 mL 0.4004 mL 0.8007 mL 2.0019 mL
40 mM 0.0601 mL 0.3003 mL 0.6006 mL 1.5014 mL
50 mM 0.0480 mL 0.2402 mL 0.4804 mL 1.2011 mL
60 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0009 mL
80 mM 0.0300 mL 0.1501 mL 0.3003 mL 0.7507 mL
100 mM 0.0240 mL 0.1201 mL 0.2402 mL 0.6006 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

NFAT Transcription Factor Regulator-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NFAT Transcription Factor Regulator-1
Cat. No.:
HY-112778
Quantity:
MCE Japan Authorized Agent: