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ChemicalBook--->CAS DataBase List--->2763602-16-8

2763602-16-8

2763602-16-8 Structure

2763602-16-8 Structure
IdentificationBack Directory
[Name]

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)-disul…
[CAS]

2763602-16-8
[Synonyms]

JNJ-2113
Icotrokinra
JNJ-77242113
Icotrokinra/JNJ-77242113/JNJ-2113/PN-235
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)-disul…
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
[Molecular Formula]

C90H120N20O22S2
[MOL File]

2763602-16-8.mol
[Molecular Weight]

1898.17
Chemical PropertiesBack Directory
[Boiling point ]

2119.4±65.0 °C(Predicted)
[density ]

1.42±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
[form ]

Solid
[pka]

4.45±0.10(Predicted)
[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)
Hazard InformationBack Directory
[Uses]

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. In addition, 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].
[in vivo]

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].

[IC 50]

IL-23: 7.1 pM (Kd)
[References]

[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. DOI:10.1038/s41598-024-67371-5
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