GSK1820795A
Based on 1 Customer Validation
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides. GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38).
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- Pureté : 99.80%
- CAS No.: 2650253-86-2
- Formule: C35H34N8
- Masse moléculaire:566.70
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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AT1 Receptor 0.006 μM (IC50) |
hPPARγ 0.25 μM (EC50) |
mouse PPARγ 0.27 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.006 μM
Compound: 38
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Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay
Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay
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[PMID: 24462665] |
| CV-1 | EC50 |
>10 μM
Compound: 38
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Agonist activity at mouse PPARalpha expressed in CV-1 cells by reporter gene assay
Agonist activity at mouse PPARalpha expressed in CV-1 cells by reporter gene assay
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[PMID: 24462665] |
| CV-1 | EC50 |
>10 μM
Compound: 38
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Agonist activity at mouse PPARdelta expressed in CV-1 cells by reporter gene assay
Agonist activity at mouse PPARdelta expressed in CV-1 cells by reporter gene assay
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[PMID: 24462665] |
| CV-1 | EC50 |
0.25 μM
Compound: 38
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Partial agonist activity at human PPARgamma expressed in CV-1 cells by reporter gene assay
Partial agonist activity at human PPARgamma expressed in CV-1 cells by reporter gene assay
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[PMID: 24462665] |
| CV-1 | EC50 |
0.27 μM
Compound: 38
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Partial agonist activity at mouse PPARgamma expressed in CV-1 cells by reporter gene assay
Partial agonist activity at mouse PPARgamma expressed in CV-1 cells by reporter gene assay
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[PMID: 24462665] |
In Vitro
GSK1820795A blocks responses of yeast expressing hGPR132a to agonists NPGly, NLGly, linoleamide, and SB-583831[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Chemical Information
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CAS No. 2650253-86-2
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Appearance Solid
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Masse moléculaire 566.70
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Formule C35H34N8
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Color Off-white to light yellow
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SMILES
CCCN1C(CC2=CC=C(C3=C(C4=NNN=N4)C=CC=C3)C=C2)=C5C(C=CC(C6=NC(C=CC=C7)=C7N6CCCC)=C5)=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (176.46 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)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.41 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Pureté et documentation
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Fiche technique (277 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Foster JR, et al. N-Palmitoylglycine and other N-acylamides activate the lipid receptor G2A/GPR132. Pharmacol Res Perspect. 2019;7(6):e00542. [Content Brief]
[2]. Lamotte Y, Faucher N, Sançon J, et al. Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists. Bioorg Med Chem Lett. 2014;24(4):1098-1103. [Content Brief]
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 | 1.7646 mL | 8.8230 mL | 17.6460 mL | 44.1151 mL |
| 5 mM | 0.3529 mL | 1.7646 mL | 3.5292 mL | 8.8230 mL | |
| 10 mM | 0.1765 mL | 0.8823 mL | 1.7646 mL | 4.4115 mL | |
| 15 mM | 0.1176 mL | 0.5882 mL | 1.1764 mL | 2.9410 mL | |
| 20 mM | 0.0882 mL | 0.4412 mL | 0.8823 mL | 2.2058 mL | |
| 25 mM | 0.0706 mL | 0.3529 mL | 0.7058 mL | 1.7646 mL | |
| 30 mM | 0.0588 mL | 0.2941 mL | 0.5882 mL | 1.4705 mL | |
| 40 mM | 0.0441 mL | 0.2206 mL | 0.4412 mL | 1.1029 mL | |
| 50 mM | 0.0353 mL | 0.1765 mL | 0.3529 mL | 0.8823 mL | |
| 60 mM | 0.0294 mL | 0.1471 mL | 0.2941 mL | 0.7353 mL | |
| 80 mM | 0.0221 mL | 0.1103 mL | 0.2206 mL | 0.5514 mL | |
| 100 mM | 0.0176 mL | 0.0882 mL | 0.1765 mL | 0.4412 mL |
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