HCAR2 agonist 1
Based on 1 Customer Validation
HCAR2 agonist 1 (Compound 9n) is a Gi protein-biased allosteric modulator of HCAR2. HCAR2 agonist 1 activates the Gi protein signaling pathway. HCAR2 agonist 1 shows anti-inflammatory effect, and reduces mRNA level of pro-inflammatory cytokine (TNF-α, IL-1β, IL-6, and MCP-1). HCAR2 agonist 1 enhances anti-inflammatory effects of orthosteric agonists in the mouse model of colitis.
For research use only. We do not sell to patients.
- Purity: 99.11%
- CAS No.: 1066676-21-8
- Formula: C26H28N4O2
- Molecular Weight:428.53
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
GPCR/G Protein Compound Library
HY-L006
-
Immunology/Inflammation Compound Library
HY-L007
-
Antidepressant Compound Library
HY-L108
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Chemokine Compound Library
HY-L132
-
Cancer Stem Cells Compound Library
HY-L135
-
Pain-Related Compound Library
HY-L139
-
Allosteric Modulators (AMs) Compound Library
HY-L170
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Lactylation Compound Library
HY-L249
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.12 μM
Compound: 9n
|
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human GPR109A receptor expressed in CHO cells by [35S]GTPgammaS binding assay
|
[PMID: 18752940] |
| CHO | IC50 |
0.17 μM
Compound: 9n
|
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
Displacement of [3H]nicotinic acid from human GPR109A receptor expressed in CHO cells
|
[PMID: 18752940] |
Chemical Information
-
CAS No. 1066676-21-8
-
Appearance Solid
-
Molecular Weight 428.53
-
Formula C26H28N4O2
-
Color Light yellow to green yellow
-
SMILES
CC1=C(C(N[C@H](C)COC2=CC=CC=C2)=O)C=NC3=C(C4=CC=C(C=C4)C(C)C)C=NN13
-
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
DMSO : 100 mg/mL (233.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.67 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (272 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)
-
Handling Instructions (2659 KB)
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 | 2.3336 mL | 11.6678 mL | 23.3356 mL | 58.3390 mL |
| 5 mM | 0.4667 mL | 2.3336 mL | 4.6671 mL | 11.6678 mL | |
| 10 mM | 0.2334 mL | 1.1668 mL | 2.3336 mL | 5.8339 mL | |
| 15 mM | 0.1556 mL | 0.7779 mL | 1.5557 mL | 3.8893 mL | |
| 20 mM | 0.1167 mL | 0.5834 mL | 1.1668 mL | 2.9169 mL | |
| 25 mM | 0.0933 mL | 0.4667 mL | 0.9334 mL | 2.3336 mL | |
| 30 mM | 0.0778 mL | 0.3889 mL | 0.7779 mL | 1.9446 mL | |
| 40 mM | 0.0583 mL | 0.2917 mL | 0.5834 mL | 1.4585 mL | |
| 50 mM | 0.0467 mL | 0.2334 mL | 0.4667 mL | 1.1668 mL | |
| 60 mM | 0.0389 mL | 0.1945 mL | 0.3889 mL | 0.9723 mL | |
| 80 mM | 0.0292 mL | 0.1458 mL | 0.2917 mL | 0.7292 mL | |
| 100 mM | 0.0233 mL | 0.1167 mL | 0.2334 mL | 0.5834 mL |
HCAR2 agonist 1 Related Classifications
HY-156025 Related Classifications
Powered by Bioz