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Lanraplenib

🥰Excellent
Catalog No. T11824LLCas No. 1800046-95-0
Alias GS-9876

Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

Lanraplenib

Lanraplenib

🥰Excellent
Purity: 99.42%
Catalog No. T11824LLAlias GS-9876Cas No. 1800046-95-0
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
Pack SizePriceAvailabilityQuantity
1 mg$47In Stock
2 mg$68In Stock
5 mg$101In Stock
10 mg$170In Stock
25 mg$306In Stock
50 mg$453In Stock
100 mg$667In Stock
1 mL x 10 mM (in DMSO)$117In Stock
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Purity:99.42%
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Product Introduction

Bioactivity
Description
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) being developed for treating inflammatory diseases. It inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
Targets&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].
AliasGS-9876
Chemical Properties
Molecular Weight443.5
FormulaC23H25N9O
Cas No.1800046-95-0
SmilesNc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Relative Density.1.52 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 41.67 mg/mL (93.96 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2548 mL11.2740 mL22.5479 mL112.7396 mL
5 mM0.4510 mL2.2548 mL4.5096 mL22.5479 mL
10 mM0.2255 mL1.1274 mL2.2548 mL11.2740 mL
20 mM0.1127 mL0.5637 mL1.1274 mL5.6370 mL
50 mM0.0451 mL0.2255 mL0.4510 mL2.2548 mL

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