PSN632408
Based on 1 Customer Validation
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.30%
- CAS No.: 857652-30-3
- 화학식: C18H24N4O4
- 분자량:360.41
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보관:Powder -20°C, 3 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]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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GPCR/G Protein Compound Library
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Orally Active Compound Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Activators Library
HY-L159
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Lactylation Compound Library
HY-L249
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
0.63 mM
Compound: 2
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Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
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[PMID: 24751443] |
| HEK293 | EC50 |
1900 nM
Compound: 24; PSN632408
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Agonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assay
Agonist activity at human GPR119 receptor expressed in HEK293 cells after 30 mins by cAMP assay
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[PMID: 26512410] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obese (DIO) rats[1]
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Dosage:100 mg/kg
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Administration:P.o.; daily for 14 days
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Result:The mean daily food intake was decreased by 10% during the first week of dosing and 15% during the second week. Body weight gain was significantly attenuated from day 6 onward with some evidence of weight loss.
Chemical Information
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CAS No. 857652-30-3
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Appearance Solid
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분자량 360.41
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화학식 C18H24N4O4
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Color White to off-white
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SMILES
O=C(OC(C)(C)C)N1CCC(CC1)OCC2=NC(C3=CC=NC=C3)=NO2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (138.73 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: ≥ 2.5 mg/mL (6.94 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.94 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.
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.
순도&문서
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Data Sheet (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Overton HA, et al. Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents. Cell Metab. 2006;3(3):167-175. [Content Brief]
[2]. Gao J, et al. Stimulating beta cell replication and improving islet graft function by GPR119 agonists. Transpl Int. 2011;24(11):1124-1134. [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 |
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| DMSO | 1 mM | 2.7746 mL | 13.8731 mL | 27.7462 mL | 69.3654 mL |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | 13.8731 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL | 6.9365 mL | |
| 15 mM | 0.1850 mL | 0.9249 mL | 1.8497 mL | 4.6244 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7746 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL | 2.3122 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7341 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6937 mL |
PSN632408 Related Classifications
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