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Lanraplenib

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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

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Purity: 98.35%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$47In StockIn Stock
2 mg$68In StockIn Stock
5 mg$101In StockIn Stock
10 mg$170In StockIn Stock
25 mg$306In StockIn Stock
50 mg$453In StockIn Stock
100 mg$667-In Stock
1 mL x 10 mM (in DMSO)$117In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.35%
Appearance:Solid
Color:White
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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].
SynonymsGS-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
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 24.2 mg/mL (54.57 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.51 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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