Cas No.: | 1609392-27-9 |
Chemical Name: | 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2, 4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide |
Synonyms: | Tyk2-IN-4,BMS986165,BMS-986165,BMS 986165 |
SMILES: | O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H] |
Formula: | C20H19D3N8O3 |
M.Wt: | 425.46 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2). |
In Vivo: | Lupus-like disease is strongly inhibited in NZB/W mice treated with Tyk2-IN-4. Tyk2-IN-4 is safe and overall well-tolerated. There are no serious adverse events and the frequency of non-serious adverse events are similar in the active (75%) and placebo (76%) groups. After oral administration, Tyk2-IN-4 is rapidly absorbed and exhibits an apparent elimination half-life of 8-15 hours[1]. |
In Vitro: | Tyk2-IN-4 blocks receptor-mediated Tyk2 activation by stabilizing the regulatory pseudokinase domain of the protein[1]. |