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Lanraplenib succinate (Synonyms: GS-9876 succinate)

Name: Lanraplenib succinate
Brand: TargetMol
SKU: T11824
Rating: 4.5 (1 reviews)

Catalog No. T11824 Copy Product Info

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

Lanraplenib succinate

Copy Product Info

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Catalog No. T11824

Synonyms GS-9876 succinate

Cas No. 1800047-00-0

Pack Size	Price	USA Stock	Global Stock	Quantity
2 mg	$59	5 days	5 days

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	1241.294
Formula	C₅₈H₆₈N₁₈O₁₄
Cas No.	1800047-00-0
Smiles	OC(=O)CCC(O)=O.OC(=O)CCC(O)=O.OC(=O)CCC(O)=O.Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1.Nc1cncc(n1)-c1cn2ccnc2c(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1
Relative Density.	no data available

Storage & Solubility Information

Storage

Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 83.33 mg/mL (67.13 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (2.66 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

	1mg	5mg	10mg	50mg
1 mM	0.8056 mL	4.0281 mL	8.0561 mL	40.2805 mL
5 mM	0.1611 mL	0.8056 mL	1.6112 mL	8.0561 mL
10 mM	0.0806 mL	0.4028 mL	0.8056 mL	4.0281 mL
20 mM	0.0403 mL	0.2014 mL	0.4028 mL	2.0140 mL
50 mM	0.0161 mL	0.0806 mL	0.1611 mL	0.8056 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc