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

NFAT Transcription Factor Regulator-1 

製品番号: HY-112778 純度: 99.37%
取扱説明書

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

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NFAT Transcription Factor Regulator-1 構造式

NFAT Transcription Factor Regulator-1 構造式

CAS 番号 : 245747-71-1

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 193 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 175 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 295 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 880 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1500 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

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)

体外実験

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].

体内実験

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].

分子量

416.28

分子式

C₁₇H₁₀F₆N₄O₂

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.
体内:
  • 1.

    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

  • 2.

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

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

*All of the co-solvents are provided by MCE.
参考文献
動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

純度: 99.37%

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Keywords:

NFAT Transcription Factor Regulator-1NFAT Transcription Factor Regulator1NFAT Transcription Factor Regulator 1Interleukin RelatedILInhibitorinhibitorinhibit

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製品名:
NFAT Transcription Factor Regulator-1
製品番号:
HY-112778
数量:
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