TAK-071
产品编号: DC11208
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应用领域
TAK-071是一种新型, 高效，选择性的毒蕈碱乙酰胆碱受体1 (M1R)正变构调节剂。 TAK-071激活M1R的EC50为520nM。
| Cas No.: |
1820812-16-5 |
| 名称: |
4-fluoro-2-[(3S,4S)-4-hydroxytetrahydro-2H-pyran-3-yl]-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2,3-dihydro-1H-isoindol-1-one |
| 别名: |
TAK071;TAK 071 |
| SMILES: |
C(=O)1C2=C(C(F)=C(C)C(CC3=CC=C(N4C=CC=N4)C=C3)=C2)CN1[C@H]1[C@H](O)CCOC1 |
| 分子式: |
C24H24FN3O3 |
| 分子量: |
421.472 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| References: |
TAK-071 (TAK071) is a novel potent, selective, low cooperativity (α-value) positive allosteric modulator of muscarinic M1 receptor with inflection point of 2.7 nM in Ca2+ flux assays in CHO-K1 cells; displays >370-fold M1R selectivity over other muscarinic receptors; selectively induces afterdepolarization in prefrontal cortical pyramidal neurons significantly ameliorates scopolamine-induced cognitive deficits in rats combined with acetylcholinesterase inhibitor donepezil, with minimizing peripheral cholinergic side effects. |
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MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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