| Identification | Back Directory | [Name]
TAK-071 | [CAS]
1820812-16-5 | [Synonyms]
TAK-071
CPD2800
TAK071;TAK 071
mAChR,inhibit,TAK071,TAK-071,Muscarinic acetylcholine receptor,TAK 071,Inhibitor
6-(4-(1H-pyrazol-1-yl)benzyl)-4-fluoro-2-((3S,4S)-4-hydroxytetrahydro-2H-pyran-3-yl)-5-methylisoindolin-1-one
L-threo-Pentitol, 1,5-anhydro-2,4-dideoxy-2-[4-fluoro-1,3-dihydro-5-methyl-1-oxo-6-[[4-(1H-pyrazol-1-yl)phenyl]methyl]-2H-isoindol-2-yl]- | [Molecular Formula]
C24H24FN3O3 | [MDL Number]
MFCD31813734 | [MOL File]
1820812-16-5.mol | [Molecular Weight]
421.46 |
| Chemical Properties | Back Directory | [Boiling point ]
658.7±55.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 135 mg/mL (320.32 mM) | [form ]
Solid | [pka]
13.94±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC50 of TAK-071 M1R agonist activities is 520 nM[1]. | [in vivo]
TAK-071 increase hippocampal inositol monophosphate production through M1R activation and improved DB00747
-induced cognitive deficits in rats at 0.3 mg/kg[1].
TAK-071 also induce diarrhea at 10 mg/kg in rats[1]. Combining sub-effective doses of TAK-071 (3 mg/kg) with an acetylcholinesterase inhibitor significantly ameliorates DB00747-induced cognitive deficits in rats[1]. | [storage]
Store at -20°C | [References]
[1] Sako Y, et al. TAK-071, a novel M1 positive allosteric modulator with low cooperativity, improves cognitive function in rodents with few cholinergic side effects. Neuropsychopharmacology. 2018 Aug 1. doi: 10.1038/s41386-018-0168-8. DOI:10.1038/s41386-018-0168-8 |
|
|