1. Immunology/Inflammation
  2. Interleukin Related

NFAT Transcription Factor Regulator 

Cat. No.: HY-112778
Handling Instructions

NFAT Transcription Factor Regulator 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 Chemical Structure

NFAT Transcription Factor Regulator Chemical Structure

CAS No. : 245747-71-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 182 nM (IL-2 synthesis)[1]

In Vitro

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].

In Vivo

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (360.33 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2402 mL 1.2011 mL 2.4022 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.01 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (6.01 mM); Clear solution

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
Molecular Weight

416.28

Formula

C₁₇H₁₀F₆N₄O₂

CAS No.

245747-71-1

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
NFAT Transcription Factor Regulator
Cat. No.:
HY-112778
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NFAT Transcription Factor Regulator

Cat. No.: HY-112778