| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P421809-1ml |
1ml |
现货  |
|
| 英文别名 | 3FE | PF 06447475 | BDBM50059277 | 3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile | CCG-267523 | 3-(4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile | PF06447475 | PF-06447475 | SB17260 | Q5276428 | SCHEMBL15401353 | 1527473-33- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PF-06447475 |
| 生化机理 | PF-06447475 是一种强效、选择性和脑穿透性 LRRK2 激酶抑制剂，IC50 为 3 nM。 |
| 储存温度 | -80℃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 |
| 产品介绍 |
Information PF-06447475 PF-06447475 is a potent, selective, and brain penetrant LRRK2 kinase inhibitor with IC50 of 3 nM. Targets LRRK2 (Cell-free assay); G2019S LRRK2 (Cell-free assay) 3nM; 11nM In vitro In the macrophage cell line Raw264.7, PF-06447475 inhibits endogenous LRRK2 kinase activity with IC50 of <10 nM. In astrocytes, PF-06447475 rescues LRRK2 mutation-induced defects in lysosomal morphology and function. In vivo In G2019S BAC-transgenic mice, PF-06447475 (100 mg/kg, p.o.) inhibits pS935 and pS1292 phosphorylation of LRRK2 with IC50 of 103 nM and 21 nM, respectively. In G2019S-LRRK2 rats, PF-06447475 (30 mg/kg, p.o.) blocks α-synuclein-induced dopaminergic neurodegeneration and attenuates neuroinflammation associated with G2019S-LRRK2 expression. |
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| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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| EC号 | 808-609-0 |
|---|---|
| 分子类型 | 小分子 |
| IUPAC Name | 3-(4-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)benzonitrile |
| INCHI | InChI=1S/C17H15N5O/c18-9-12-2-1-3-13(8-12)14-10-19-16-15(14)17(21-11-20-16)22-4-6-23-7-5-22/h1-3,8,10-11H,4-7H2,(H,19,20,21) |
| InChi Key | BHTWDJBVZQBRKP-UHFFFAOYSA-N |
| Canonical SMILES | C1COCCN1C2=NC=NC3=C2C(=CN3)C4=CC=CC(=C4)C#N |
| Isomeric SMILES | C1COCCN1C2=NC=NC3=C2C(=CN3)C4=CC=CC(=C4)C#N |
| 关联CAS | 1527473-33-1 |
| PubChem CID | 72706840 |
| MeSH Entry Terms | 3-(4-(morpholin-4-yl)-7H-pyrrolo(2,3-d)pyrimidin-5-yl)benzonitrile;PF-06447475 |
| 分子量 | 305.33 |
| 分子量 | 305.330 g/mol |
|---|---|
| XLogP3 | 2.100 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 2 |
| 精确质量Exact Mass | 305.128 Da |
| 单同位素质量Monoisotopic Mass | 305.128 Da |
| 拓扑极表面积Topological Polar Surface Area | 77.800 Ų |
| 重原子数Heavy Atom Count | 23 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 457.000 |
| 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 | 0 |
| 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 |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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