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Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.
别名 GS-9876 monosuccinate
Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.

| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 25 mg | ¥ 10,600 | 1-2周 | |
| 50 mg | ¥ 13,800 | 1-2周 | |
| 100 mg | ¥ 17,500 | 1-2周 |
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| 产品描述 | Lanraplenib monosuccinate inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. Lanraplenib monosuccinate is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. |
| 靶点活性 | Syk:9.5 nM |
| 体外活性 | In human macrophages, Lanraplenib monosuccinate inhibits IC-stimulated TNFα and IL-1β release (EC50=121±77 nM and 9±17 nM, respectively). Lanraplenib monosuccinate 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 monosuccinate ?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). |
| 别名 | GS-9876 monosuccinate |
| 分子量 | 561.59 |
| 分子式 | C27H31N9O5 |
| CAS No. | 1800046-97-2 |
| Smiles | O=C(O)CCC(=O)O.N1=CC(=NC(=C1)C=2N=C(NC3=CC=C(C=C3)N4CCN(CC4)C5COC5)C6=NC=CN6C2)N |
| 密度 | no data available |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 125 mg/mL (222.58 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (5.88 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | ||||||||||||||||||||||||||||||||||||
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