2775417-67-7

2775417-67-7 structure
2775417-67-7 structure
  • Name: Tyk2-IN-13
  • Chemical Name: Tyk2-IN-13
  • CAS Number: 2775417-67-7
  • Molecular Formula: C29H30D3N7O6
  • Molecular Weight: 578.63
  • Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
  • Create Date: 2022-11-14 23:12:18
  • Modify Date: 2024-04-03 17:42:36
  • Tyk2-IN-13 (compound 30) is an orally active TYK2 inhibitor. Tyk2-IN-13 inhibits IFNα stimulated STAT3 phosphorylation with an IC50 value of 1.90 nM. Tyk2-IN-13 can be used for the research of autoimmune diseases[1].

Name Tyk2-IN-13
Description Tyk2-IN-13 (compound 30) is an orally active TYK2 inhibitor. Tyk2-IN-13 inhibits IFNα stimulated STAT3 phosphorylation with an IC50 value of 1.90 nM. Tyk2-IN-13 can be used for the research of autoimmune diseases[1].
Related Catalog
Target

IL-6:33 nM (IC50)

IL-2:41 nM (IC50)

In Vitro Tyk2-IN-13 (0-10 μM; 1.5 h) shows inhibitory effect to IFNα stimulated STAT3 phosphorylation with an IC50 value of 1.90 nM[1]. Tyk2-IN-13 (0.244-1000 nM; 30 min) exhibits binding affinities with IC50s of 3496, 41 and 33 nM for EPO, 1L-2 and 1L-6, respectively[1].
In Vivo Tyk2-IN-13 (30 mg/kg; p.o. BID for 6 days) decreases the colonic weight of colitis mice[1]. Tyk2-IN-13 (20 mg/kg; p.o. BID for 5 days) weakens IL-23-induced acanthosis in vivo[1]. Animal Model: Male CB17-SCID mice with IL-23-dependent colitis[1] Dosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg; twice daily for 6 days Result: Showed a decreasing effect in colonic weight, and no significant difference was observed relative to deucravacitinib. Animal Model: Female C57BL/6 mice with psoriasis-like skin inflammation[1] Dosage: 20 mg/kg Administration: Oral gavage; 20 mg/kg; twice daily for 5 days Result: Significantly protected mice from IL-23-induced acanthosis with no significant weight losses, and showed comparable results with deucravacitinib.
References

[1]. Liu Fei, et al. Novel TYK2 Inhibitors with an N-(Methyl-d3)pyridazine-3-carboxamide Skeleton for the Treatment of Autoimmune Diseases. ACS Medicinal Chemistry Letters. 2022.

Molecular Formula C29H30D3N7O6
Molecular Weight 578.63