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Lanraplenib succinate

CAS No. : 1800047-00-0

MCE 站：Lanraplenib succinate

产品活性：Lanraplenib succinate (GS-9876 succinate) 是一种高度选择性的口服 SYK 抑制剂 (IC₅₀=9.5 nM) ，用于治疗炎症性疾病。Lanraplenib succinate (GS-9876 succinate) 通过糖蛋白 VI (GPVI) 受体抑制血小板中的 SYK 活性，而不会延长猴子或人类的出血时间 (BT)。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk

In Vitro: Lanraplenib succinate (GS-9876 succinate) inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells with EC₅₀ values of 24-51 nM. Lanraplenib monosuccinate inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC₅₀=112±10 nM and 164±15 nM, respectively) and anti-IgM /anti-CD40 co-stimulated B cell proliferation (EC₅₀=108±55 nM). In human macrophages, Lanraplenib succinate inhibits IC-stimulated TNFα and IL-1β release (EC₅₀=121±77 nM and 9±17 nM, respectively).
Lanraplenib succinate (GS-9876 succinate) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linker for activation of T cells and phospholipase Cγ2, platelet activation and aggregation in human whole blood, and platelet binding to collagen under arterial flow.

相关产品：Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Kinase Inhibitor Library  |  Clinical Compound Library  |  Clinical Compound Library Plus  |  Protein Tyrosine Kinase Compound Library  |  Drug Repurposing Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Entospletinib  |  R406  |  Cerdulatinib  |  Fostamatinib Disodium  |  TAK-659 hydrochloride  |  Piceatannol  |  BAY 61-3606 dihydrochloride  |  PRT062607 Hydrochloride  |  Lanraplenib  |  Gusacitinib  |  MNS  |  PRT-060318  |  RO9021  |  R112  |  GSK143  |  Syk-IN-3  |  TAS05567

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