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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

😃Good
Purity: 98.93%
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.
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Purity:98.93%
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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
ColorWhite
AppearanceSolid
Storage & Solubility Information
Storagekeep away from moisture | 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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