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CAS No. : 1800046-95-0
MCE 国际站:Lanraplenib
产品活性:Lanraplenib (GS-9876) 是一种高度选择性的口服 SYK 抑制剂 (IC50=9.5 nM) ,用于研究炎症性疾病。Lanraplenib (GS-9876) 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 (GS-9876) 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 (GS-9876) 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 (GS-9876) inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively).
Lanraplenib (GS-9876) 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 Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Pyroptosis Compound Library | Orally Active Compound Library | Rare Diseases Drug Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Sovleplenib | Syk Kinase Peptide Substrate | Cevidoplenib dimesylate | Syk-IN-4 | Syk Inhibitor II dihydrochloride dihydrate | GSK143 dihydrochloride | Syk-IN-6 | PRT062607 Hydrochloride | MNS | TAK-659 hydrochloride | Gusacitinib hydrochloride | Dehydroabietinol | R406 free base | Fostamatinib Disodium | Syk Kinase Peptide Substrate, Biotin labeled | BAY 61-3606 dihydrochloride | SYK/JAK-IN-1 | Cerdulatinib hydrochloride | TAS05567 | SRX3207 | Entospletinib | GSK2646264 | Syk-IN-3 | R112
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