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Lanraplenib succinate

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

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Catalog No. T11824Cas No. 1800047-00-0

Alias GS-9876 succinate

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

😃Good

Catalog No. T11824Alias GS-9876 succinateCas No. 1800047-00-0

Pack Size	Price	Availability	Quantity
2 mg	56 €	5 days

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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).
Alias	GS-9876 succinate

Chemical Properties

Molecular Weight	1241.294
Formula	C₅₈H₆₈N₁₈O₁₄
Cas No.	1800047-00-0
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 83.33 mg/mL (134.26 mM), Sonication is recommended.

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
100 mM	0.0081 mL	0.0403 mL	0.0806 mL	0.4028 mL

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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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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