NFAT Transcription Factor Regulator-1

Name: NFAT Transcription Factor Regulator-1
Brand: MedChemExpress
SKU: HY-112778
Rating: 4.5 (1 reviews)

Cat. No.: HY-112778 Purity: 98.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 245747-71-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 192	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 192	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 295	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1500	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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•Related Screening Libraries:

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View All Interleukin Related Isoform Specific Products:

View All Isoforms

IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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.

245747-71-1

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
10 mM	0.2402 mL	1.2011 mL	2.4022 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (249 KB) HNMR (185 KB) LCMS (430 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

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

[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. [Content Brief]

Complete Stock Solution Preparation Table

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