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

Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate 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 acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease^[1].

Icotrokinra (0.03-10 mg/kg; p.o.; once daily for 7 days) acetate 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) acetate 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.

1898.17 (free base)

C₉₀H₁₂₀N₂₀O₂₂S₂·xC₂H₄O₂

Solid

White to off-white

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

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Fourie AM, et al., JNJ-77242113, a highly potent, selective peptide targeting the IL-23 receptor, provides robust IL-23 pathway inhibition upon oral dosing in rats and humans. Sci Rep. 2024 Jul 30;14(1):17515.  [Content Brief]