TAK-071

Research use only, not for human use.

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.

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.Alzheimer Disease Phase 1 Clinical(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.TAK-071 also induce diarrhea at 10 mg/kg in rats.Combining sub-effective doses of TAK-071 (3 mg/kg) with an acetylcholinesterase inhibitor significantly ameliorates DB00747-induced cognitive deficits in rats.

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TAK071 | TAK 071

GPCR/G Protein

mAChR

mAChR

Neurological Disease

Alzheimer Disease

1820812-16-5

421.472

C24H24FN3O3

>98% (HPLC)

DMSO : 135 mg/mL 320.32 mM

CC1=C(C2=C(C=C1CC3=CC=C(C=C3)N4C=CC=N4)C(=O)N(C2)C5COCCC5O)F

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

(-20℃)

With Ice Pack

≥ 2 years