Lanraplenib succinate
Modify Date: 2024-01-17 15:09:07
Lanraplenib succinate structure
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Common Name | Lanraplenib succinate | ||
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| CAS Number | 1800047-00-0 | Molecular Weight | 620.64 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C23H25N9O.3/2C4H6O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Lanraplenib succinateLanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3]. |
| Name | Lanraplenib succinate |
|---|
| Description | Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans[1][2][3]. |
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| Related Catalog | |
| Target |
IC50: 9.5 nM (SYK)[1] |
| 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)[1]. 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[2]. |
| References |
| Molecular Formula | C23H25N9O.3/2C4H6O4 |
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| Molecular Weight | 620.64 |