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Lanraplenib monosuccinate

Catalog No. T11824LCas No. 1800046-97-2

Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.

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Pack Size	Price	Availability
25 mg	$1,520	1-2 weeks
50 mg	$1,980	1-2 weeks
100 mg	$2,500	1-2 weeks

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Product Introduction

Bioactivity

Description	Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.
In vitro	In human macrophages, Lanraplenib monosuccinate inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively). Lanraplenib monosuccinate 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.Lanraplenib monosuccinate ?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).
Alias	GS-9876 monosuccinate

Chemical Properties

Molecular Weight	561.59
Formula	C27H31N9O5
Cas No.	1800046-97-2

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (222.58 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7807 mL	8.9033 mL	17.8066 mL	89.0329 mL
5 mM	0.3561 mL	1.7807 mL	3.5613 mL	17.8066 mL
10 mM	0.1781 mL	0.8903 mL	1.7807 mL	8.9033 mL
20 mM	0.0890 mL	0.4452 mL	0.8903 mL	4.4516 mL
50 mM	0.0356 mL	0.1781 mL	0.3561 mL	1.7807 mL
100 mM	0.0178 mL	0.0890 mL	0.1781 mL	0.8903 mL

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