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MLi-2,LRRK2抑制剂, 富亮氨酸重复激酶 2 抑制剂

有力和选择性的LRRK2抑制剂
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货号 (SKU) 包装规格 是否现货 价格 数量
M276039-1mg
 1mg 现货 Stock Image
M276039-5mg
 5mg 现货 Stock Image
M276039-10mg
 10mg 现货 Stock Image
M276039-50mg
 50mg 期货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
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Autophagy (555) leucine rich repeat kinase 2 Inhibitor (24) LRRK2 (31)
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基本描述

别名 (2R,6S)-2,6-二甲基-4-[6-[5-(1-(甲基环丙基)氧基]-1H-吲唑-3-基]嘧啶-4-基]吗啉
英文别名 (2R,6S)-2,6-Dimethyl-4-[6-[5-(1-methylcyclopropyl)oxy-1H-indazol-3-yl]pyrimidin-4-yl]morpholine | cis-2,6-Dimethyl-4-(6-(5-(1-methylcyclopropoxy)-1H-indazol-3-yl)pyrimidin-4-yl)morpholine | rel-3-[6-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-pyrimidinyl]-5-[(
规格或纯度 Moligand™, ≥98%
英文名称 MLi-2
生化机理 高效和选择性的LRRK2抑制剂。在无细胞（IC 50 = 0.76 nM），基于去磷酸化的细胞（IC 50 = 1.4 nM）和放射性配体结合（IC 50 = 3.4 nM）分析中抑制LRRK2。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 富亮氨酸重复激酶 2 抑制剂
备注 有关更多信息，请参考SDS。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

MLi-2 是一种结构新颖、高效、选择性的 LRRK2 激酶抑制剂，具有中枢神经系统活性，IC50为 0.76 nM，有潜力用于帕金森氏病。

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).

AI解读

关联靶点（人）

LRRK2 Tchem 富含亮氨酸重复丝氨酸/苏氨酸蛋白激酶 2(Leucine-rich repeat serine/threonine-protein kinase 2) (4 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TH Tclin Tyrosine 3-hydroxylase (13 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD4 Tchem Dopamine D4 receptor (7907 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA1D Tclin Alpha-1d adrenergic receptor (4171 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR1D Tclin Serotonin 1d (5-HT1d) receptor (2897 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CRHR1 Tclin Corticotropin releasing factor receptor 1 (2996 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA1B Tclin Alpha-1b adrenergic receptor (2912 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PPARG Tclin Peroxisome proliferator-activated receptor gamma (15191 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OPRL1 Tchem Nociceptin receptor (3823 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGFR Tclin Prostanoid FP receptor (687 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTGIR Tclin Prostanoid IP receptor (1280 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PPARA Tclin Peroxisome proliferator-activated receptor alpha (9197 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYSLTR1 Tclin Cysteinyl leukotriene receptor 1 (2118 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM4 Tclin Muscarinic acetylcholine receptor M4 (6041 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM5 Tclin Muscarinic acetylcholine receptor M5 (4677 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DRD5 Tchem Dopamine D5 receptor (1597 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ADRB3 Tclin Beta-3 adrenergic receptor (5850 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Cdk4 Cyclin-dependent kinase 4 (3 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Htr7 Serotonin 7 (5-HT7) receptor (19 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mc4r Melanocortin receptor 4 (1205 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Sigmar1 Sigma opioid receptor (160 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Npy1r Neuropeptide Y receptor type 1 (8 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hrh4 Histamine H4 receptor (388 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Ntsr1 Neurotensin receptor 1 (48 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CA PI3-kinase p110-alpha subunit (51 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Gabrp GABA-A receptor; anion channel (5731 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
pknB Serine/threonine-protein kinase pknB (356 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDPK1 Calcium-dependent protein kinase 1 (793 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CRK2 Cell division control protein 2 homolog (194 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tmem97 Sigma intracellular receptor 2 (922 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
P2ry4 Purinergic P2Y (14 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504772425
分子类型 小分子
IUPAC Name (2R,6S)-2,6-dimethyl-4-[6-[5-(1-methylcyclopropyl)oxy-1H-indazol-3-yl]pyrimidin-4-yl]morpholine
INCHI InChI=1S/C21H25N5O2/c1-13-10-26(11-14(2)27-13)19-9-18(22-12-23-19)20-16-8-15(28-21(3)6-7-21)4-5-17(16)24-25-20/h4-5,8-9,12-14H,6-7,10-11H2,1-3H3,(H,24,25)/t13-,14+
InChi Key ATUUNJCZCOMUKD-OKILXGFUSA-N
Canonical SMILES CC1CN(CC(O1)C)C2=NC=NC(=C2)C3=NNC4=C3C=C(C=C4)OC5(CC5)C
Isomeric SMILES C[C@@H]1CN(C[C@@H](O1)C)C2=NC=NC(=C2)C3=NNC4=C3C=C(C=C4)OC5(CC5)C
PubChem CID 78319901
分子量 379.46

化学和物理性质

溶解性 Soluble in DMSO to 100 mM
分子量 379.500 g/mol
XLogP3 3.200
氢键供体数Hydrogen Bond Donor Count 1
氢键受体数Hydrogen Bond Acceptor Count 6
可旋转键计数Rotatable Bond Count 4
精确质量Exact Mass 379.201 Da
单同位素质量Monoisotopic Mass 379.201 Da
拓扑极表面积Topological Polar Surface Area 76.200 Ų
重原子数Heavy Atom Count 28
形式电荷Formal Charge 0
复杂度Complexity 549.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 2
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

 SDS英文版

技术规格说明书

Purity(HPLC)
Proton NMR spectrum Conforms to Structure
LC-MS for identification Conforms

 技术规格说明书

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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找到9个结果

批号(Lot Number) 证书类型 日期 货号
G2412495 分析证书 25-04-08 M276039
I2419595 分析证书 24-09-11 M276039
I2419596 分析证书 24-09-11 M276039
I2419597 分析证书 24-09-11 M276039
I2419598 分析证书 24-09-11 M276039
G2412496 分析证书 24-07-02 M276039
B2215423 分析证书 23-08-10 M276039
B2215424 分析证书 23-08-10 M276039
B2215430 分析证书 23-08-10 M276039

可替换产品

  1. MLi-2
    MLi-2

    ¥939.90

参考文献

1. Fell MJ, Mirescu C, Basu K, Cheewatrakoolpong B, DeMong DE, Ellis JM, Hyde LA, Lin Y, Markgraf CG, Mei H et al..  (2015)  MLi-2, a Potent, Selective, and Centrally Active Compound for Exploring the Therapeutic Potential and Safety of LRRK2 Kinase Inhibition..  J Pharmacol Exp Ther,  355  (3): (397-409).  [PMID:26407721] [10.1021/op500134e]
2. Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H et al..  (2017)  Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity..  J Med Chem,  60  (7): (2983-2992).  [PMID:28245354] [10.1021/op500134e]
3. Fdez E et al..  (2022)  Pathogenic LRRK2 regulates centrosome cohesion via Rab10/RILPL1-mediated CDK5RAP2 displacement..  iScience,  25  (6): (104476).  [PMID:35721463]

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