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| 5mg |
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| 10mg |
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| Targets |
GLP-1 receptor (GLP-1R). GLP-1R modulator L7-028 is an allosteric modulator of the GLP-1R that enhances the binding of GLP-1 to its receptor via a transmembrane site. By potentiating GLP-1 signaling, it enhances cAMP accumulation and downstream metabolic effects.
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| ln Vitro |
GLP-1R modulator L7-028 enhances GLP-1 binding to GLP-1R with an EC50 of 11.01 ± 2.73 μM. It enhances affinity for GLP-1 and increases cAMP signaling. Its activity is characterized by its ability to potentiate GLP-1-mediated responses in GLP-1R-expressing cells.
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| ln Vivo |
In vivo, GLP-1R modulator L7-028 would be expected to exert metabolic effects through GLP-1R potentiation. By enhancing GLP-1 signaling, it could improve glycemic control and influence energy homeostasis. Its effects in vivo would be assessed in animal models of type 2 diabetes and metabolic disorders.
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| Enzyme Assay |
In vitro binding and functional assays are used to characterize GLP-1R modulator L7-028 as a GLP-1R modulator. Radioligand binding assays or functional assays measuring cAMP accumulation are performed using GLP-1R-expressing cells in the presence of GLP-1 to determine its EC50 of 11.01 μM and confirm its modulatory activity.
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| Cell Assay |
Cellular assays for GLP-1R modulator L7-028 involve treating GLP-1R-expressing cells with the compound in the presence of GLP-1 and measuring cAMP accumulation. The compound enhances GLP-1-mediated cAMP signaling with an EC50 of 11.01 μM, confirming its activity as a GLP-1R modulator.
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| Animal Protocol |
In vivo efficacy of GLP-1R modulator L7-028 would be evaluated in animal models of type 2 diabetes and metabolic disorders. The compound could be administered, and its effects on glucose tolerance, insulin secretion, and metabolic parameters would be assessed. Its potential for treating metabolic diseases is an area of investigation.
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| ADME/Pharmacokinetics |
GLP-1R modulator L7-028 has a molecular formula of C24H28N2O3 and a molecular weight of 392.49. As a small-molecule GLP-1R modulator, its pharmacokinetic properties would be characteristic of this class. The compound should be stored under recommended conditions. It is for research use only.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for GLP-1R modulator L7-028. As a GLP-1R modulator, its safety profile would be an important consideration. Potential toxicities could be related to its effects on GLP-1 signaling. Standard preclinical safety studies would be required to evaluate its safety for potential therapeutic applications.
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| References |
[1]. Wang J, et al. Allosteric Modulators Enhancing GLP-1 Binding to GLP-1R via a Transmembrane Site. ACS Chem Biol. 2021 Nov 19;16(11):2444-2452.
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| Additional Infomation |
GLP-1R modulator L7-028 (CAS#: 2648317-95-5) is an allosteric modulator that enhances GLP-1 binding to GLP-1R via a transmembrane site with an EC50 of 11.01 μM. It enhances affinity for GLP-1 and cAMP signaling. It has a molecular formula of C24H28N2O3 and a molecular weight of 392.49. It is a research tool for studying GLP-1R function.
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| Molecular Formula |
C24H28N2O3
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|---|---|
| Molecular Weight |
392.490726470947
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| Exact Mass |
392.209
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| CAS # |
2648317-95-5
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| PubChem CID |
162641034
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| Appearance |
White to off-white solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)C(=O)C2=CC(=CC=C2)NC(=O)C3=CC(=CC=C3)OC4CCCC4
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| InChi Key |
QASJOTNVPCHDTC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28N2O3/c27-23(18-8-7-13-22(17-18)29-21-11-2-3-12-21)25-20-10-6-9-19(16-20)24(28)26-14-4-1-5-15-26/h6-10,13,16-17,21H,1-5,11-12,14-15H2,(H,25,27)
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| Chemical Name |
3-cyclopentyloxy-N-[3-(piperidine-1-carbonyl)phenyl]benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~254.8 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.37 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.37 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (6.37 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5478 mL | 12.7392 mL | 25.4784 mL | |
| 5 mM | 0.5096 mL | 2.5478 mL | 5.0957 mL | |
| 10 mM | 0.2548 mL | 1.2739 mL | 2.5478 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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