1. GPCR/G Protein
  2. GPR109A
  3. GPR109 receptor agonist-1

GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptor GPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases.

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

GPR109 receptor agonist-1 Chemical Structure

GPR109 receptor agonist-1 Chemical Structure

CAS No. : 306935-41-1

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5 mg USD 35 In-stock
10 mg USD 55 In-stock
25 mg USD 95 In-stock
50 mg USD 145 In-stock
100 mg USD 195 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptor GPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases[1].

IC50 & Target

pEC50: 6.40 ± 0.36 (GPR109b)[1]

Molecular Weight

205.21

Formula

C10H11N3O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC=C(N(C(C)C)N=N2)C2=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (487.31 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 4.8731 mL 24.3653 mL 48.7306 mL
5 mM 0.9746 mL 4.8731 mL 9.7461 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.

  • 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 (12.18 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 (12.18 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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8731 mL 24.3653 mL 48.7306 mL 121.8264 mL
5 mM 0.9746 mL 4.8731 mL 9.7461 mL 24.3653 mL
10 mM 0.4873 mL 2.4365 mL 4.8731 mL 12.1826 mL
15 mM 0.3249 mL 1.6244 mL 3.2487 mL 8.1218 mL
20 mM 0.2437 mL 1.2183 mL 2.4365 mL 6.0913 mL
25 mM 0.1949 mL 0.9746 mL 1.9492 mL 4.8731 mL
30 mM 0.1624 mL 0.8122 mL 1.6244 mL 4.0609 mL
40 mM 0.1218 mL 0.6091 mL 1.2183 mL 3.0457 mL
50 mM 0.0975 mL 0.4873 mL 0.9746 mL 2.4365 mL
60 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0304 mL
80 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
100 mM 0.0487 mL 0.2437 mL 0.4873 mL 1.2183 mL
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GPR109 receptor agonist-1 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.

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GPR109 receptor agonist-1
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HY-107580
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