Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
説明 | Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. |
ターゲット&IC50 | Syk:9.5 nM |
In vitro | 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 [2]. Lanraplenib inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK, ERK, MEK, and PKCδ in human B cells (EC50s: 24-51 nM). Lanraplenib 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 inhibits IC-stimulated TNFα and IL-1β release (EC50: 121±77 nM and 9±17 nM, respectively) [1]. |
別名 | GS-9876 |
分子量 | 443.5 |
分子式 | C23H25N9O |
CAS No. | 1800046-95-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 41.67 mg/mL (93.96 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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Lanraplenib 1800046-95-0 Angiogenesis Tyrosine Kinase/Adaptors Syk Spleen tyrosine kinase Inhibitor GS9876 GS-9876 GS 9876 inhibit inhibitor