GNE-9605
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GNE-9605是一种有效的LRRK2选择性抑制剂,IC50值为19 nM[1].
富含亮氨酸重复激酶2(LRRK2)是富含亮氨酸重复激酶家族的成员.LRRK2基因变异是帕金森氏病和克罗恩氏病的最常见原因.
GNE-9605是一种脑渗透的\有效的和选择性的LRRK2抑制剂.GNE-9605对LRRK2高度有效,Ki值和IC50值分别为2.0和18.7 nM.在人类肝细胞和肝微粒体中,GNE-9605具有优异的人类代谢稳定性[1].
在大鼠药代动力学(PK)研究中,GNE-9605具有90%的优异的口服生物利用度和26 mL/min/kg的总血浆清除率.在表达人类G2019S LRRK2蛋白帕金森氏病突变的细菌人工染色体(BAC)转基因小鼠中,GNE-9605(10或50 mg/kg)可以浓度依赖的方式抑制LRRK2 Ser1292自磷酸化,IC50值为20 nM.在食蟹猴PK研究中,GNE-9605具有优秀的脑渗透性[1].
参考文献：
[1]. Estrada AA, Chan BK, Baker-Glenn C, et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem, 2014, 57(3): 921-936.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 449.83 |
| Cas No. | 1536200-31-3 |
| Formula | C17H20ClF4N7O |
| Solubility | ≥22.5 mg/mL in DMSO |
| Chemical Name | N2-(5-chloro-1-((3S,4S)-3-fluoro-1-(oxetan-3-yl)piperidin-4-yl)-1H-pyrazol-4-yl)-N4-methyl-5-(trifluoromethyl)pyrimidine-2,4-diamine |
| SDF | Download SDF |
| Canonical SMILES | CNC1=NC(NC2=C(Cl)N([C@@H]3[C@@H](F)CN(C4COC4)CC3)N=C2)=NC=C1C(F)(F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
