GPR61 Inverse agonist 1

Cat. No.: HY-156354: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC₅₀: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia.

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

GPR61 Inverse agonist 1 Chemical Structure

Size	Price	Stock
5 mg	USD 800	Ask For Quote & Lead Time
10 mg	USD 1280	Ask For Quote & Lead Time
25 mg	USD 2560	Ask For Quote & Lead Time
50 mg	USD 4050	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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Biological Activity
Purity & Documentation
References
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Description

Molecular Weight

524.54

Formula

C₂₂H₂₆F₂N₆O₅S

Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C(F)=CN=C1)CNC2=NC(OC)=C(C=C2)S(N(C3=NC(OCC)=CC(C)=N3)CCOC)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (190.64 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	1.9064 mL	9.5322 mL	19.0643 mL
5 mM	0.3813 mL	1.9064 mL	3.8129 mL
10 mM	0.1906 mL	0.9532 mL	1.9064 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.77 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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: ≥98.0%

Select Batch:

Data Sheet (273 KB) SDS (0 KB)

COA (252 KB) HNMR (272 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

References

[1]. Lees JA, et al. An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive allosteric mechanism. Nat Commun. 2023 Sep 23;14(1):5938. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9064 mL	9.5322 mL	19.0643 mL	47.6608 mL
	5 mM	0.3813 mL	1.9064 mL	3.8129 mL	9.5322 mL
	10 mM	0.1906 mL	0.9532 mL	1.9064 mL	4.7661 mL
	15 mM	0.1271 mL	0.6355 mL	1.2710 mL	3.1774 mL
	20 mM	0.0953 mL	0.4766 mL	0.9532 mL	2.3830 mL
	25 mM	0.0763 mL	0.3813 mL	0.7626 mL	1.9064 mL
	30 mM	0.0635 mL	0.3177 mL	0.6355 mL	1.5887 mL
	40 mM	0.0477 mL	0.2383 mL	0.4766 mL	1.1915 mL
	50 mM	0.0381 mL	0.1906 mL	0.3813 mL	0.9532 mL
	60 mM	0.0318 mL	0.1589 mL	0.3177 mL	0.7943 mL
	80 mM	0.0238 mL	0.1192 mL	0.2383 mL	0.5958 mL
	100 mM	0.0191 mL	0.0953 mL	0.1906 mL	0.4766 mL