VU0152100 (Synonyms: VU152100)

Cat. No.: HY-13340 Purity: 98.98%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

VU0152100 Chemical Structure

CAS No. : 409351-28-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 174	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 174	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Purity & Documentation
References
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Description

IC₅₀ & Target

mAChR4

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.

409351-28-6

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
10 mM	0.2929 mL	1.4644 mL	2.9289 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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)

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

Purity: 98.98%

Select Batch:

Data Sheet (275 KB) SDS (419 KB)

COA (250 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Byun NE, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93. [Content Brief]

[2]. Brady AE, et al. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53. [Content Brief]

Complete Stock Solution Preparation Table

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

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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