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Icotrokinra

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Catalog No. T89073Cas No. 2763602-16-8
Alias PN-235, PN235, JNJ-77242113, JNJ77242113, JNJ-2113, JNJ2113

Icotrokinra is an orally bioavailable and highly selective antagonist of the interleukin-23 receptor (IL-23R), thereby interfering with IL-23-mediated signaling cascades. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 value of 5.6 pM, and it suppresses IL-23-induced interferon-gamma production in natural killer cells with an IC50 value of 18.4 pM. Icotrokinra further demonstrates anti-inflammatory effects in a rat TNBS-induced colitis model, making it a compound of interest in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.

Icotrokinra

Icotrokinra

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Purity: 99.93%
Catalog No. T89073Alias PN-235, PN235, JNJ-77242113, JNJ77242113, JNJ-2113, JNJ2113Cas No. 2763602-16-8
Icotrokinra is an orally bioavailable and highly selective antagonist of the interleukin-23 receptor (IL-23R), thereby interfering with IL-23-mediated signaling cascades. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 value of 5.6 pM, and it suppresses IL-23-induced interferon-gamma production in natural killer cells with an IC50 value of 18.4 pM. Icotrokinra further demonstrates anti-inflammatory effects in a rat TNBS-induced colitis model, making it a compound of interest in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$275-In Stock
10 mg$975-In Stock
50 mg$2,235-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.93%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Icotrokinra is an orally bioavailable and highly selective antagonist of the interleukin-23 receptor (IL-23R), thereby interfering with IL-23-mediated signaling cascades. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 value of 5.6 pM, and it suppresses IL-23-induced interferon-gamma production in natural killer cells with an IC50 value of 18.4 pM. Icotrokinra further demonstrates anti-inflammatory effects in a rat TNBS-induced colitis model, making it a compound of interest in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease.
Targets&IC50
IL-23:7.1 pM (Kd)
In vivo
In the TNBS-induced rat colitis model, oral administration of Icotrokinra at doses ≥0.3 mg/kg/day significantly reduced body weight loss and the colon weight/length ratio. In the IL-23-induced skin inflammation model, Icotrokinra at doses ≥10 mg/kg BID markedly suppressed IL-17A, IL-17F, and IL-22 gene expression and alleviated skin thickness.[1]
SynonymsPN-235, PN235, JNJ-77242113, JNJ77242113, JNJ-2113, JNJ2113
Chemical Properties
Molecular Weight1898.17
FormulaC90H120N20O22S2
Cas No.2763602-16-8
SmilesN(C([C@H](CC1=CC2=C(C=C1)C=CC=C2)NC([C@H](CC3=CC=C(OCCN)C=C3)NC(=O)[C@H]4NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](CC=5C=6C(NC5)=C(C)C=CC6)NC(=O)[C@]([C@@H](C)O)(NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(C)=O)C(C)(C)SSC4(C)C)[H])=O)=O)C7(C(N[C@H](C(N[C@H](C(N[C@@H](CC=8C=CC=NC8)C(N(CC(N)=O)C)=O)=O)CC(N)=O)=O)CCC(O)=O)=O)CCOCC7
SequenceAc-Pen-Asn-Thr-Trp(7-Me)-Lys(Ac)-Pen-Phe(4-amino ethoxy)-2Nal-ThpGly-Glu-Asn-3Pal-Sar-NH2 (Pen1&Pen6 bridge)
Sequence ShortTWKGEN
Storage & Solubility Information
Storagekeep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (42.15 mM), Sonication is recommended.
H2O: ≥ 80 mg/mL, Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.5268 mL2.6341 mL5.2682 mL26.3412 mL
5 mM0.1054 mL0.5268 mL1.0536 mL5.2682 mL
10 mM0.0527 mL0.2634 mL0.5268 mL2.6341 mL
20 mM0.0263 mL0.1317 mL0.2634 mL1.3171 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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