货号:A1216692
同义名:
GS-9876; GS-SYK
Lanraplenib (GS-9876) 是一种高度选择性的口服 SYK 抑制剂,IC50 为 9.5 nM,用于炎症性疾病的研究。


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| 产品名称 | Syk ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| PRT062607 HCl |
++++
Syk, IC50: 1 nM |
99%+ | |||||||||||||||||
| R406 |
++
Syk, IC50: 41 nM |
98% | |||||||||||||||||
| Fostamatinib Disodium |
++
Syk, IC50: 41 nM |
99%+ | |||||||||||||||||
| Piceatannol | ✔ | PKC | 98% | ||||||||||||||||
| BAY 61-3606 2HCl |
+++
Syk, Ki: 7.5 nM |
99+% | |||||||||||||||||
| Entospletinib |
+++
Syk, IC50: 7.7 nM |
99%+ | |||||||||||||||||
| MNS |
+
Syk, IC50: 2.5 μM |
p97,Src | 98% | ||||||||||||||||
| Fostamatinib |
++
Syk, IC50: 41 nM |
99%+ | |||||||||||||||||
| RO9021 |
+++
Syk, IC50: 5.6 nM |
98% | |||||||||||||||||
| TAK-659 HCl |
++++
Syk, IC50: 3.2 nM |
FLT3 | 99%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| Concentration | Treated Time | Description | References | |
| Human B cells | 245 nM | 7 days | Lanraplenib dose-dependently inhibited B cell maturation with an EC50 value of 245 nM. | BMC Rheumatol. 2021 Mar 30;5(1):15 |
| Human B cells | 298 nM (HD), 340 nM (SLE) | 16 hours | Lanraplenib dose-dependently inhibited CD69 expression with EC50 values of 298 nM (healthy donors) and 340 nM (SLE patients). | BMC Rheumatol. 2021 Mar 30;5(1):15 |
| Human B cells | 130 nM | 48 hours | Lanraplenib dose-dependently reduced B cell survival with an EC50 value of 130 nM. | BMC Rheumatol. 2021 Mar 30;5(1):15 |
| J774 macrophages | 2 μM | 30 min | Inhibition of Syk kinase activity, reducing intracellular Ca2+ flashing | Mol Biol Cell. 2024 Jan 1;35(1):ar5 |
| Human B cells | 216 nM | 7 days | Lanraplenib dose-dependently inhibited IgM secretion with an EC50 value of 216 nM. | BMC Rheumatol. 2021 Mar 30;5(1):15 |
| Administration | Dosage | Frequency | Description | References | ||
| NZB/W mice | Systemic lupus erythematosus and lupus nephritis model | Oral | 0.25% in chow | Continuous administration until study end | Lanraplenib treatment significantly improved overall survival, prevented the development of proteinuria, and reduced blood urea nitrogen concentrations in NZB/W mice. | BMC Rheumatol. 2021 Mar 30;5(1):15 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.25mL 0.45mL 0.23mL |
11.27mL 2.25mL 1.13mL |
22.55mL 4.51mL 2.25mL |
|
| CAS号 | 1800046-95-0 |
| 分子式 | C23H25N9O |
| 分子量 | 443.5 |
| SMILES Code | NC1=CN=CC(C2=CN3C(C(NC4=CC=C(N5CCN(C6COC6)CC5)C=C4)=N2)=NC=C3)=N1 |
| 别名 | GS-9876; GS-SYK |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 18 mg/mL(40.59 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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