2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU0152100

VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia.

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VU0152100 Chemical Structure

VU0152100 Chemical Structure

CAS No. : 409351-28-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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 USD 174 In-stock
Solution
10 mM * 1 mL in DMSO USD 174 In-stock
Solid
5 mg USD 101 In-stock
10 mg USD 158 In-stock
25 mg USD 347 In-stock
50 mg USD 520 In-stock
100 mg USD 780 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

VU0152100 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

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Description

VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia[1][2].

IC50 & Target

mAChR4

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 EC50
620 nM
Compound: ML108
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
[PMID: 23177787]
In Vivo

VU0152100 (10, 30, 56.6 mg/kg; i.p.; single) reverses amphetamine-induced hyperlocomotion in rats[1].
VU0152100 (10, 30, 56.6 mg/kg; i.p.; single) blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning and prepulse inhibition of the acoustic startle reflex in rats[1].
VU0152100 reverses amphetamine-induced increases in extracellular dopamine levels in nucleus accumbens and caudate-putamen[1].

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

Animal Model: Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced hyperlocomotion model)[1].
Dosage: 10, 30, 56.6 mg/kg
Administration: Intraperitoneal injection; single (pre-treatment)
Result: Produced a robust dose-dependent reversal of amphetamine-induced hyperlocomotion.
Animal Model: Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced)[1].
Dosage: 10, 30, 56.6 mg/kg
Administration: Intraperitoneal injection; single (pre-treatment)
Result: Blocked amphetamine-induced disruption of prepulse inhibition.
Dose-dependently reversed the disruptive effects of amphetamine on the acquisition of a context-dependent fear.
Molecular Weight

341.43

Formula

C18H19N3O2S
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

CC1=C2C(SC(C(NCC3=CC=C(OC)C=C3)=O)=C2N)=NC(C)=C1
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 : ≥ 50 mg/mL (146.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9289 mL 14.6443 mL 29.2886 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 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: ≥ 2.5 mg/mL (7.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2.9289 mL 14.6443 mL 29.2886 mL 73.2215 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 mL 14.6443 mL
10 mM 0.2929 mL 1.4644 mL 2.9289 mL 7.3221 mL
15 mM 0.1953 mL 0.9763 mL 1.9526 mL 4.8814 mL
20 mM 0.1464 mL 0.7322 mL 1.4644 mL 3.6611 mL
25 mM 0.1172 mL 0.5858 mL 1.1715 mL 2.9289 mL
30 mM 0.0976 mL 0.4881 mL 0.9763 mL 2.4407 mL
40 mM 0.0732 mL 0.3661 mL 0.7322 mL 1.8305 mL
50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4644 mL
60 mM 0.0488 mL 0.2441 mL 0.4881 mL 1.2204 mL
80 mM 0.0366 mL 0.1831 mL 0.3661 mL 0.9153 mL
100 mM 0.0293 mL 0.1464 mL 0.2929 mL 0.7322 mL
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VU0152100 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:

VU0152100409351-28-6VU152100VU 0152100VU-0152100VU 152100VU-152100mAChRMuscarinic acetylcholine receptorpsychosisschizophreniamental disordersdopamineNASCPInhibitorinhibitorinhibit

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