
HG-10-102-01
CAS No. 1351758-81-0
HG-10-102-01 ( —— )
产品货号. M20640 CAS No. 1351758-81-0
HG-10-102-01 是富含亮氨酸重复激酶 2(LRRK2,IC50 为 20.3 nM)的抑制剂。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥721 | 有现货 |
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10MG | ¥1158 | 有现货 |
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25MG | ¥2341 | 有现货 |
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50MG | ¥3750 | 有现货 |
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100MG | ¥5411 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称HG-10-102-01
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述HG-10-102-01 是富含亮氨酸重复激酶 2(LRRK2,IC50 为 20.3 nM)的抑制剂。
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产品描述HG-10-102-01 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2 IC50 of 20.3 nM).
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体外实验HG-10-102-01 (0-3 μM, 90 min) substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant.Western Blot AnalysisCell Line:HEK293 cells, Mouse Swiss 3T3 cells and Mouse embryonic fibroblast cells Concentration:0, 0.01, 0.03, 0.1, 0.3, 1, and 3 μM Incubation Time:90 min Result:Induced a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. Induced similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells and mouse embryonic fibroblast cells.
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体内实验HG-10-102-01 (0-100 mg/kg, IP, once) shows inhibition of LRRK2 Ser910/Ser935 phosphorylation in kidney, spleen, and brain of mice.HG-10-102-01 (1 mg/kg, IV; 10 mg/kg, PO; once) shows good oral bioavailability (%F = 67), a short half-life of 0.13 h, and low plasma exposure. Animal Model:Wild type male C57BL/6 mice Dosage:0, 3, 10, 30, 50, and 100 mg/kg Administration:IP, once Result:Showed near complete dephosphorylation of Ser910 and Ser935 of LRRK2 in all tissues including brain at 100 mg/kg and 50 mg/kg, but only partial inhibition in brain at the 30 and 10 mg/kg doses.Animal Model:Wild type male C57BL/6 mice Dosage:1 mg/kg (IV); 10 mg/kg (PO) Administration:IV, PO; once (Pharmacokinetic Analysis)Result:Pharmacokinetic Parameters of HG-10-102-01 in male C57BL/6 mice.
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同义词——
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通路Autophagy
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靶点LRRK2
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受体LRRK2
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研究领域——
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适应症——
化学信息
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CAS Number1351758-81-0
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分子量377.83
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分子式C17H20ClN5O3
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纯度>98% (HPLC)
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溶解度DMSO:50 mg/mL (132.33 mM)
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SMILESCNc1nc(Nc2ccc(cc2OC)C(=O)N2CCOCC2)ncc1Cl
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化学全称[4-[[5-chloro-4-(methylamino)-2-pyrimidinyl]amino]-3-methoxyphenyl]-4-morpholinyl-methanone
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Choi H G Zhang J Deng X et al. Brain Penetrant LRRK2 Inhibitor[J]. ACS Medicinal Chemistry Letters 2012 3(8):658-662.
产品手册




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