Биологическая активность
Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and селективный антагонист of the IL-23 рецептор. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
Оригинал на английском
Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
Химические свойства
- CAS №
- 2763602-16-8
- Брутто-формула
- C₉₀H₁₂₀N₂₀O₂₂S₂
- Мол. масса
- 1898.17 г/моль
- SMILES
- N(C1(CCOCC1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@H](C(=O)N(C)CC(=O)N)CC1=CN=CC=C1)C(=O)[C@@H](NC(=O)[C@@H](NC(C1C(SSC([C@@H](C(N[C@H](C(=O)NC([C@H](O)C)C(=O)N[C@@H](CC2=CNC3=C(C=CC=C23)C)C(=O)N[C@@H](CCCCNC(=O)C)C(=O)N1)CC(=O)N)=O)NC(=O)C)(C)C)(C)C)=O)CC1C=CC(OCCN)=CC=1)CC1C=CC2C=CC=CC=2C=1
- Синонимы
- 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
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.