1. Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling
  2. Interleukin Related STAT IFNAR
  3. Icotrokinra

Icotrokinra  (Synonyms: JNJ-77242113; JNJ-2113; PN-235)

製品番号: HY-P10587 純度: 99.90%
COA 取扱説明書 Technical Support

Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.

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カスタムペプチド

Icotrokinra

Icotrokinra 構造式

CAS 番号 : 2763602-16-8

容量 価格(税別) 在庫状況 数量
1 mg $195 在庫あり
5 mg $345 在庫あり
10 mg $485 在庫あり
25 mg $770 在庫あり
50 mg $1180 在庫あり
100 mg $1770 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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製品説明

Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease[1].

IC50 & Target[1]

IL-23

7.1 pM (Kd)

体内実験

Icotrokinra (0.03-10 mg/kg; p.o.; once daily for 7 days) reduces the colon weight-to-length ratio and alleviates weight loss in rats with TNBS-induced colitis[1].
Icotrokinra (1-30 mg/kg; p.o.; twice daily for 3 days) prevents IL-23-induced upregulation of IL-17A and IL-22 in a rat skin inflammation model at doses greater than 10 mg/kg[1].

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

分子量

1898.17

分子式

C90H120N20O22S2

CAS 番号
Appearance

Solid

Color

White to off-white

Sequence

Ac-Pen-Asn-Thr-Trp(7-Me)-Lys(Ac)-Pen-Phe(4-amino ethoxy)-2Nal-ThpGly-Glu-Asn-3Pal-Sar-NH2 (Pen1&Pen6 bridge)

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Sealed storage, away from moisture
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : ≥ 100 mg/mL (52.68 mM)

DMSO : 100 mg/mL (52.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5268 mL 2.6341 mL 5.2682 mL
5 mM 0.1054 mL 0.5268 mL 1.0536 mL
10 mM 0.0527 mL 0.2634 mL 0.5268 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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: ≥ 2.5 mg/mL (1.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (1.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
純度とドキュメンテーション

純度: 99.90%

参考文献

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 0.5268 mL 2.6341 mL 5.2682 mL 13.1706 mL
5 mM 0.1054 mL 0.5268 mL 1.0536 mL 2.6341 mL
10 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3171 mL
15 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
20 mM 0.0263 mL 0.1317 mL 0.2634 mL 0.6585 mL
25 mM 0.0211 mL 0.1054 mL 0.2107 mL 0.5268 mL
30 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL
40 mM 0.0132 mL 0.0659 mL 0.1317 mL 0.3293 mL
50 mM 0.0105 mL 0.0527 mL 0.1054 mL 0.2634 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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.

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Inquiry Information

製品名:
Icotrokinra
製品番号:
HY-P10587
数量:
MCE 日本正規代理店: