| Identification | Back 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 Properties | Back 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 Information | Back 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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YantaiBio
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