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Ivarmacitinib

CAS No. : 1445987-21-2

MCE 站：Ivarmacitinib

产品活性：Ivarmacitinib (SHR0302) 是一种有效的具有口服活性的 JAK 抑制剂，尤其是 JAK1 的抑制剂。Ivarmacitinib 对 JAK1 的选择性是 JAK2 的 10 倍以上，是 JAK3 的 77 倍，是 Tyk2 的 420 倍。Ivarmacitinib 抑制 JAK1-STAT3 磷酸化并诱导肝星状细胞凋亡 (apoptosis)。Ivarmacitinib 具有抗增殖和抗炎作用。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：JAK  |  Apoptosis

In Vitro: Ivarmacitinib (SHR0302; 1 nM-10 M; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner.
Ivarmacitinib (1 nM-10 M) exerts an inhibitory effect on the activation, proliferation ａnd migration of HSCs.
Ivarmacitinib (1 nM-10 M; 48 hours; HSCs) treatment induces the apoptosis of HSCs.
Ivarmacitinib (1 nM-10 M; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 ａnd Bax in HSCs, ａnd decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway.

In Vivo: Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment ａnd paw swelling degree, ａnd alleviated histopathology of spleen ａnd joint of AA rats.
Ivarmacitinib can inhibit the proliferation of T, B ａnd fibroblast-like synoviocytes (FLS), ａnd down-regulates cytokines TNF-α, IL-1β, IL-17 ａnd antibody IgG1, IgG2a levels, ａnd suppresses the proportion of Th17 ａnd total B, ａnd inhibits JAK1-STAT3 phosphorylation.

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