Lanraplenib-monosuccinate-GS-9876-monosuccinate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELanraplenib monosuccinateCat. No.: HY-109091ACAS No.: 1800046-97-2Synonyms: GS-9876 monosuccinate分式: CHNO分量: 561.59作靶点: Syk作通路: Protein Tyrosine Kinase/RTK储存式: Please store the product under the recommended conditions inthe COA.

2、溶解性数据体外实验 DMSO : 125 mg/mL (222.58 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7807 mL 8.9033 mL 17.8066 mL5 mM 0.3561 mL 1.7807 mL 3.5613 mL10 mM 0.1781 mL 0.8903 mL 1.7807 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保

3、证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.70 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.70 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Ma

4、ster of Small Molecules 您边的抑制剂师www.MedChemE物活性 Lanraplenib monosuccinate (GS-9876 monosuccinate)种度选择性的服 SYK 抑制剂 (IC50=9.5 nM) ，于治疗炎症性疾病。Lanraplenib monosuccinate (GS-9876 monosuccinate) 通过糖蛋 VI (GPVI) 受体抑制板中的 SYK 活性，不会延长猴或类的出时间 (BT) 1 2 3。IC50 & Target IC50: 9.5 nM (SYK) 1体外研究 Lanraplenib monosuccin

5、ate (GS-9876 monosuccinate) inhibits anti-IgM stimulated phosphorylation of AKT,BLNK, BTK, ERK, MEK, and PKC in human B cells with EC50 values of 24-51 nM. Lanraplenibmonosuccinate inhibits anti-IgM mediated CD69 and CD86 expression on B-cells (EC50=11210 nM and16415 nM, respectively) and anti-IgM /

6、anti-CD40 co-stimulated B cell proliferation (EC50=10855 nM). Inhuman macrophages, Lanraplenib monosuccinate inhibits IC-stimulated TNF and IL-1 release(EC50=12177 nM and 917 nM, respectively) 1.Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits glycoprotein VI (GPVI)-induced phosphorylation

7、of linker for activation of T cells and phospholipase C2, platelet activation and aggregation in human wholeblood, and platelet binding to collagen under arterial flow 2.REFERENCES1. Di Paolo J, et al. FRI0049 Preclinical Characterization of GS-9876, A Novel, Oral SYK Inhibitor That Shows Efficacy i

8、n MultipleEstablished Rat Models of Collagen-Induced Arthritis.Annals of the Rheumatic Diseases 2016;75:443-444.2. Clarke AS, et al. Effects of GS-9876, a novel spleen tyrosine kinase inhibitor, on platelet function and systemic hemostasis. ThrombRes. 2018 Oct;170:109-118.3. Kivitz AJ, et al. GS-9876, a Novel, Highly Selective, SYK Inhibitor in Patients with Active Rheumatoid Arthritis: Safety, Tolerability andEfficacy Results of a Phase 2 Study abstract. Arthritis Rheumatol.2018; 70 (suppl 10).McePdfHeightCaution: Product has not been fully validated for medical ap