BMS-986165 是一种高选择性、口服生物可利用的变构 TYK2 抑制剂，用于治疗自身免疫性疾病。它通过稳定调节 JH2 结构域来阻断受体介导的 Tyk2 激活，可抑制IL-12/23和 I 型IFN 途径。 Information Deucravacitinib (BMS-986165) Deucravacitinib (BMS-986165) is a highly potent and selective allosteric inhibitor of Tyk2 with a Ki value of 0.02 nM for binding to the Tyk2 pseudokinase domain. It is highly selective against a panel of 265 kinases and pseudokinases. Targets Tyk2 (Cell-free assay) 0.02 nM In vitro BMS-986165 is highly differentiated from all other reported JAK/TYK2 inhibitors due to its ability to achieve an unprecedented level of selectivity for TYK2, especially over JAK1, JAK2, and JAK3. In vivo BMS-986165 has been identified as a highly potent and selective allosteric TYK2 inhibitor having excellent PK properties across species with minimal profiling liabilities and is orally efficacious with dose-dependent activity in a murine disease model of psoriasis. Significant activity has also been observed with 11 in other murine autoimmune disease models of colitis and lupus. Cell Research(from reference) Cell lines：CD3+ T-cells, CD161+ CD3+ T-cells, TF-1 cells, mononuclear cells, platelets Concentrations：0 - 10 μM
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Deucravacitinib (BMS-986165)
CAS number：1609392-27-9 molecular formula：C20H19D3N8O3
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| Chinese alias | - | ||
| English alias | Deucravacitinib | NSC825520 | compound 11 [PMID: 31318208} | EN300-22276121 | Deucravacitinib [USAN] | (BMS-986165) | SCHEMBL20520348 | Sotyktu | AT18623 | DEUCRAVACITINIB [JAN] | 6-[(Cyclopropylcarbonyl)amino]-4-[[2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3 | ||
| CAS number | 1609392-27-9 | molecular formula | C20H19D3N8O3 |
| molecular weight | 425.46 g/mol | Exact mass | - |
| PSA | 136.000 Ų | logp | 1.2 |
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