Lanraplenib-succinate-GS-9876-succinate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELanraplenib succinateCat. No.: HY-109091BCAS No.: 1800047-00-0Synonyms: GS-9876 succinate分式: CHNO./CHO分量: 620.64作靶點: Syk作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實驗 DMSO : 83.33 mg/mL (134.26 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6112 mL 8.0562 mL 16.1124 mL5 mM 0.3222 mL 1.6112 mL 3.2225 mL10 mM 0.1611 mL 0.8056 mL 1.6112 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄的儲備液，再依次添加助溶?為保證實驗結(jié)

3、果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.35 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.35 mM); Clear solution1/2 Master of Small Molecules

4、 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Lanraplenib succinate (GS-9876 succinate)種度選擇性的服 SYK 抑制劑 (IC50=9.5 nM) ，于治療炎癥性疾病。Lanraplenib succinate (GS-9876 succinate) 通過糖蛋 VI (GPVI) 受體抑制板中的 SYK 活性，不會延長猴或類的出時間 (BT) 1 2 3。IC50 & Target IC50: 9.5 nM (SYK) 1體外研究 Lanraplenib succinate (GS-9876 succinate)

5、inhibits anti-IgM stimulated phosphorylation of AKT, BLNK, BTK,ERK, MEK, and PKC in human B cells with EC50 values of 24-51 nM. Lanraplenib monosuccinate inhibitsanti-IgM mediated CD69 and CD86 expression on B-cells (EC50=11210 nM and 16415 nM, respectively)and anti-IgM /anti-CD40 co-stimulated B ce

6、ll proliferation (EC50=10855 nM). In human macrophages,Lanraplenib succinate inhibits IC-stimulated TNF and IL-1 release (EC50=12177 nM and 917 nM,respectively) 1.Lanraplenib succinate (GS-9876 succinate) inhibits glycoprotein VI (GPVI)-induced phosphorylation of linkerfor activation of T cells and

7、phospholipase C2, platelet activation and aggregation in human whole blood,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 in MultipleEstablished Rat Models of Coll

8、agen-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 appl