Art. -Nr.: HY-156772

GPR88 agonist 2

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GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC₅₀ value of 14 µM in GPR88 cAMP functional assay.

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Reinheit: 99.57%
CAS. Nr.: 2821859-71-4
Formel: C₂₆H₃₃N₅O₃
Molecular Weight:463.57

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GPR88 agonist 2 Chemical Structure

CAS. Nr.: 2821859-71-4

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC₅₀ value of 14 µM in GPR88 cAMP functional assay^[1].

In Vitro

GPR88 agonist 2 significantly enhance ^[35S]GTPγS binding activity (EC₅₀: 8.9 μM) in WT mouse striatal membranes, but GPR88 agonist 2 is inactive in striatal membranes prepared from GPR88 KO mice.^[1].

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

In Vivo

GPR88 agonist 2 (20mg/ml, ip) has a good plasma exposure (C_max:1670 ng/mL) and acceptable metabolic stability (T_1/2:4.66h, CL:21mL/mg/kg)^[1].
GPR88 agonist 2 (20mg/ml, ip) has sufficient brain penetration (C_max:576 ng/mL)^[1].
Pharmacokinetic analysis in mice^[1]

20 mg/kg, ip	C_max (ng/mL)	T_1/2 (h)	CL(mL/min/kg)	B/P_ratio
plasma	1670	5.6	21	0.34
brain	576	/	/

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

Chemical Information

CAS. Nr. 2821859-71-4
Appearance Solid
Molecular Weight 463.57
Formel C₂₆H₃₃N₅O₃
Color Off-white to light yellow
SMILES

CNC(C(N=N1)=CN1C[C@@H](C2=CC=C(C=C2)OC[C@@H](C)CC)NC([C@H](C3=CC=CC=C3)C)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (215.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1572 mL

10.7859 mL

21.5717 mL

5 mM

0.4314 mL

2.1572 mL

4.3143 mL

10 mM

0.2157 mL

1.0786 mL

2.1572 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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% Corn Oil

Solubility: 2.5 mg/mL (5.39 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Rahman MT, et al. Evaluation of Amide Bioisosteres Leading to 1,2,3-Triazole Containing Compounds as GPR88 Agonists: Design, Synthesis, and Structure-Activity Relationship Studies. J Med Chem. 2021 Aug 26;64(16):12397-12413. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.1572 mL	10.7859 mL	21.5717 mL	53.9293 mL
	5 mM	0.4314 mL	2.1572 mL	4.3143 mL	10.7859 mL
	10 mM	0.2157 mL	1.0786 mL	2.1572 mL	5.3929 mL
	15 mM	0.1438 mL	0.7191 mL	1.4381 mL	3.5953 mL
	20 mM	0.1079 mL	0.5393 mL	1.0786 mL	2.6965 mL
	25 mM	0.0863 mL	0.4314 mL	0.8629 mL	2.1572 mL
	30 mM	0.0719 mL	0.3595 mL	0.7191 mL	1.7976 mL
	40 mM	0.0539 mL	0.2696 mL	0.5393 mL	1.3482 mL
	50 mM	0.0431 mL	0.2157 mL	0.4314 mL	1.0786 mL
	60 mM	0.0360 mL	0.1798 mL	0.3595 mL	0.8988 mL
	80 mM	0.0270 mL	0.1348 mL	0.2696 mL	0.6741 mL
	100 mM	0.0216 mL	0.1079 mL	0.2157 mL	0.5393 mL

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GPR88 agonist 2

GPCR/G Protein Compound Library

CNS-Penetrant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GPR88 agonist 2

GPCR/G Protein Compound Library

CNS-Penetrant Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GPR88 agonist 2 Related Classifications

HY-156772 Related Classifications