GPR52 agonist-1

Name: GPR52 agonist-1
Brand: MedChemExpress
SKU: HY-147395
Rating: 4.5 (1 reviews)

Cat. No.: HY-147395 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

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GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC₅₀ value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity.

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

GPR52 agonist-1 Chemical Structure

CAS No. : 1207965-40-9

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

pEC₅₀: 7.53 (GPR52)^[1]

In Vivo

GPR52 agonist-1 (compound 7m) (3, 10, and 30 mg/kg; PO; single dosage) attenuates Methamphetamine-induced hyperlocomotion in mice^[1].
GPR52 agonist-1 (0.1 mg/kg, IV and 1 mg/kg, PO; single dosage) exhibits good oral pharmacokinetic profile with an C_max of 108.1 ng/mL, an AUC_0-8h of 613.7 ng·h/mL, and an F (bioavailability) of 73% in mouse^[1].

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

Animal Model:	Male ICR mice (7-8 weeks; subcutaneously injected with 2 mg/kg Methamphetamine after 60 min administration)^[1]
Dosage:	3, 10, and 30 mg/kg
Administration:	PO; single dosage
Result:	Attenuated Methamphetamine-induced hyperlocomotion dose-dependently. Did not show significant cataleptogenic effects even at a dose of 100 mg/kg and had a low risk of extrapyramidal side effects.

Molecular Weight

453.96

Formula

C₂₅H₂₁ClFNO₂S

CAS No.

1207965-40-9

Appearance

Solid

Color

White to off-white

SMILES

COCCNC(C1=CC(C2=C3SC(CC4=CC(Cl)=CC(F)=C4)=CC3=CC=C2)=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (220.28 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	2.2028 mL	11.0142 mL	22.0284 mL
5 mM	0.4406 mL	2.2028 mL	4.4057 mL
10 mM	0.2203 mL	1.1014 mL	2.2028 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.51 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.76%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (246 KB) HNMR (258 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Setoh M, et al. Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52. J Med Chem. 2014 Jun 26;57(12):5226-37. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2028 mL	11.0142 mL	22.0284 mL	55.0709 mL
	5 mM	0.4406 mL	2.2028 mL	4.4057 mL	11.0142 mL
	10 mM	0.2203 mL	1.1014 mL	2.2028 mL	5.5071 mL
	15 mM	0.1469 mL	0.7343 mL	1.4686 mL	3.6714 mL
	20 mM	0.1101 mL	0.5507 mL	1.1014 mL	2.7535 mL
	25 mM	0.0881 mL	0.4406 mL	0.8811 mL	2.2028 mL
	30 mM	0.0734 mL	0.3671 mL	0.7343 mL	1.8357 mL
	40 mM	0.0551 mL	0.2754 mL	0.5507 mL	1.3768 mL
	50 mM	0.0441 mL	0.2203 mL	0.4406 mL	1.1014 mL
	60 mM	0.0367 mL	0.1836 mL	0.3671 mL	0.9178 mL
	80 mM	0.0275 mL	0.1377 mL	0.2754 mL	0.6884 mL
	100 mM	0.0220 mL	0.1101 mL	0.2203 mL	0.5507 mL

GPR52 agonist-1 Related Classifications

Neurological Disease

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:

GPR52 agonist-11207965-40-9GPR52G Protein-Coupled Receptor 52orally activeblood-brain barrierBBBcAMP accumulationhyperactivityantipsychoticICR miceInhibitorinhibitorinhibit

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GPR52 agonist-1

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Complete Stock Solution Preparation Table

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