[CAS NO. 1820812-16-5] TAK-071

Name: TAK-071
Brand: Arctom Scientific
SKU: AS945189

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PRODUCTS SPECIFICATIONS [1820812-16-5]

Distributor

Catalog

AS945189

Brand

Arctom Scientific

CAS

1820812-16-5

DESCRIPTION [1820812-16-5]

Overview

MDL	-
Molecular Weight	421.46
Molecular Formula	C24H24FN3O3
SMILES	O=C1C2=CC(CC3=CC=C(N4C=CC=N4)C=C3)=C(C)C(F)=C2CN1[C@@H]5[C@H](CCOC5)O

For research use only. We do not sell to patients.

Summary

TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC ₅₀ of TAK-071 M1R agonist activities is 520 nM ^[1] .

IC50 & Target

EC50: 520 nM (M1R) ^[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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02769065	Takeda	Alzheimer Disease\|Healthy Volunteers	May 5, 2016	Phase 1
NCT04334317	Takeda\|Michael J. Fox Foundation for Parkinson´s Research	Parkinson Disease\|Healthy Participants	October 21, 2020	Phase 2
NCT02918266	Takeda	Healthy Volunteers	November 21, 2016	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 135 mg/mL ( 320.32 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3727 mL	11.8635 mL	23.7270 mL
5 mM	0.4745 mL	2.3727 mL	4.7454 mL
10 mM	0.2373 mL	1.1864 mL	2.3727 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.25 mg/mL (5.34 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.25 mg/mL (5.34 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.25 mg/mL (5.34 mM); Clear solution

* All of the co-solvents are available by MCE.

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.