2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. TAK-071

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.

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TAK-071 Chemical Structure

TAK-071 Chemical Structure

CAS No. : 1820812-16-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 187 In-stock
Solution
10 mM * 1 mL in DMSO USD 187 In-stock
Solid
5 mg USD 109 In-stock
10 mg USD 170 In-stock
50 mg USD 480 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

TAK-071 Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

421.46

Formula

C24H24FN3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=CC(CC3=CC=C(N4C=CC=N4)C=C3)=C(C)C(F)=C2CN1[C@@H]5[C@H](CCOC5)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 135 mg/mL (320.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3727 mL 11.8635 mL 23.7270 mL 59.3176 mL
5 mM 0.4745 mL 2.3727 mL 4.7454 mL 11.8635 mL
10 mM 0.2373 mL 1.1864 mL 2.3727 mL 5.9318 mL
15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9545 mL
20 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.9659 mL
25 mM 0.0949 mL 0.4745 mL 0.9491 mL 2.3727 mL
30 mM 0.0791 mL 0.3955 mL 0.7909 mL 1.9773 mL
40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4829 mL
50 mM 0.0475 mL 0.2373 mL 0.4745 mL 1.1864 mL
60 mM 0.0395 mL 0.1977 mL 0.3955 mL 0.9886 mL
80 mM 0.0297 mL 0.1483 mL 0.2966 mL 0.7415 mL
100 mM 0.0237 mL 0.1186 mL 0.2373 mL 0.5932 mL
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TAK-071 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAK-0711820812-16-5TAK071TAK 071mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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