TAK-071
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MedKoo CAT#: 465875

CAS#: 1820812-16-5

Description: TAK-071 is a novel muscarinic M1 positive allosteric modulator with low cooperativity, improving cognitive function in rodents with few cholinergic side effects.

Chemical Structure

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TAK-071
CAS# 1820812-16-5
Instruction

Theoretical Analysis

MedKoo Cat#: 465875
Name: TAK-071
CAS#: 1820812-16-5
Chemical Formula: C24H24FN3O3
Exact Mass: 421.18
Molecular Weight: 421.472
Elemental Analysis: C, 68.39; H, 5.74; F, 4.51; N, 9.97; O, 11.39

Price and Availability

Size Price Availability Quantity
10mg USD 550 2 Weeks
100mg USD 1750 2 Weeks
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Synonym: TAK-071; TAK071; TAK 071;

IUPAC/Chemical Name: 6-(4-(1H-pyrazol-1-yl)benzyl)-4-fluoro-2-((3S,4S)-4-hydroxytetrahydro-2H-pyran-3-yl)-5-methylisoindolin-1-one

InChi Key: WFSARWQASFQZMG-VXKWHMMOSA-N

InChi Code: InChI=1S/C24H24FN3O3/c1-15-17(11-16-3-5-18(6-4-16)28-9-2-8-26-28)12-19-20(23(15)25)13-27(24(19)30)21-14-31-10-7-22(21)29/h2-6,8-9,12,21-22,29H,7,10-11,13-14H2,1H3/t21-,22-/m0/s1

SMILES Code: O=C1N([C@H]2COCC[C@@H]2O)CC3=C1C=C(CC4=CC=C(N5N=CC=C5)C=C4)C(C)=C3F

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 421.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kurimoto E, Yamada R, Hirakawa T, Kimura H. Therapeutic potential of TAK-071, a muscarinic M1 receptor positive allosteric modulator with low cooperativity, for the treatment of cognitive deficits and negative symptoms associated with schizophrenia. Neurosci Lett. 2021 Nov 1;764:136240. doi: 10.1016/j.neulet.2021.136240. Epub 2021 Sep 10. PMID: 34509568.

2: Yin W, Mamashli F, Buhl DL, Khudyakov P, Volfson D, Martenyi F, Gevorkyan H, Rosen L, Simen AA. Safety, pharmacokinetics and quantitative EEG modulation of TAK-071, a novel muscarinic M1 receptor positive allosteric modulator, in healthy subjects. Br J Clin Pharmacol. 2022 Feb;88(2):600-612. doi: 10.1111/bcp.14975. Epub 2021 Jul 31. PMID: 34240455.

3: Kucinski A, Sarter M. Reduction of falls in a rat model of PD falls by the M1 PAM TAK-071. Psychopharmacology (Berl). 2021 Jul;238(7):1953-1964. doi: 10.1007/s00213-021-05822-x. Epub 2021 Mar 18. PMID: 33735392; PMCID: PMC7969347.

4: Mandai T, Sako Y, Kurimoto E, Shimizu Y, Nakamura M, Fushimi M, Maeda R, Miyamoto M, Kimura H. T-495, a novel low cooperative M1 receptor positive allosteric modulator, improves memory deficits associated with cholinergic dysfunction and is characterized by low gastrointestinal side effect risk. Pharmacol Res Perspect. 2020 Feb;8(1):e00560. doi: 10.1002/prp2.560. PMID: 31990455; PMCID: PMC6986443.

5: Kucinski A, Phillips KB, Koshy Cherian A, Sarter M. Rescuing the attentional performance of rats with cholinergic losses by the M1 positive allosteric modulator TAK-071. Psychopharmacology (Berl). 2020 Jan;237(1):137-153. doi: 10.1007/s00213-019-05354-5. Epub 2019 Oct 16. PMID: 31620809.

6: Mandai T, Kasahara M, Kurimoto E, Tanaka M, Suzuki M, Nakatani A, Kimura H. In Vivo Pharmacological Comparison of TAK-071, a Positive Allosteric Modulator of Muscarinic M1 Receptor, and Xanomeline, an Agonist of Muscarinic M1/M4 Receptor, in Rodents. Neuroscience. 2019 Aug 21;414:60-76. doi: 10.1016/j.neuroscience.2019.07.003. Epub 2019 Jul 9. PMID: 31299348.

7: Kurimoto E, Nakashima M, Kimura H, Suzuki M. TAK-071, a muscarinic M1 receptor positive allosteric modulator, attenuates scopolamine-induced quantitative electroencephalogram power spectral changes in cynomolgus monkeys. PLoS One. 2019 Mar 11;14(3):e0207969. doi: 10.1371/journal.pone.0207969. PMID: 30856192; PMCID: PMC6411103.

8: Sako Y, Kurimoto E, Mandai T, Suzuki A, Tanaka M, Suzuki M, Shimizu Y, Yamada M, Kimura H. TAK-071, a novel M1 positive allosteric modulator with low cooperativity, improves cognitive function in rodents with few cholinergic side effects. Neuropsychopharmacology. 2019 Apr;44(5):950-960. doi: 10.1038/s41386-018-0168-8. Epub 2018 Aug 1. PMID: 30089885; PMCID: PMC6461781.