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Icotrokinra

Chemical Structure : Icotrokinra

CAS No.: 2763602-16-8

Icotrokinra (JNJ-77242113, PN-21235, JNJ-2113)

Catalog No.: PC-24977Not For Human Use, Lab Use Only.

Icotrokinra (JNJ-77242113, PN-21235) is a highly potent, selective peptide antagonist targeting the IL-23 receptor with KD of 7.1 pM, potently and selectively inhibits proximal IL-23 signaling (IC50=5.6 pM) without impacting IL-12 signaling.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Icotrokinra (JNJ-77242113, PN-21235) is a highly potent, selective peptide antagonist targeting the IL-23 receptor with KD of 7.1 pM, potently and selectively inhibits proximal IL-23 signaling (IC50=5.6 pM) without impacting IL-12 signaling.
JNJ-77242113 inhibited IL-23–induced interferon (IFN)γ production in NK cells, and in blood from healthy donors and psoriasis patients with IC50 of 18.4, 11 and 9 pM, respectively).
JNJ-77242113 attenuated disease parameters at doses ≥ 0.3 mg/kg/day in rat trinitrobenzene sulfonic acid-induced colitis model. JNJ-77242113 exhibits dose-dependent inhibition of ex vivo IL-23–stimulated IL-17A production in blood from rats.
JNJ-77242113 inhibited IL-23–induced skin thickening and IL-17A, -17F and -22 gene induction in IL-23–induced rat skin inflammation model.

Physicochemical Properties

M.Wt 1898.17
Formula C90H120N20O22S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Glycinamide, N-acetyl-3-mercapto-L-valyl-L-asparaginyl-L-threonyl-7-methyl-L-tryptophyl-N6-acetyl-L-lysyl-3-mercapto-L-valyl-O-(2-aminoethyl)-L-tyrosyl-3-(2-naphthalenyl)-L-alanyl-4-aminotetrahydro-2H-pyran-4-carbonyl-L-α-glutamyl-L-asparaginyl-3-(3-pyridinyl)-L-alanyl-N2-methyl-, cyclic (1→6)-disulfide

References

1. Bissonnette R, et al. N Engl J Med. 2024 Feb 8;390(6):510-521.

2. Fourie AM, et al. Sci Rep. 2024 Jul 30;14(1):17515.

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