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| Targets |
GLP-1 receptor (GLP-1R). GLP-1R modulator C16 is a positive allosteric modulator (PAM) of the GLP-1R. It enhances the binding of GLP-1 to its receptor via a transmembrane site. By potentiating GLP-1 signaling, it promotes glucose-dependent insulin release and inhibits glucagon secretion.
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| ln Vitro |
GLP-1R modulator C16 is an allosteric modulator that enhances GLP-1 binding to GLP-1R with an EC50 of 8.43 ± 3.82 μM. By potentiating GLP-1 signaling, it promotes glucose-dependent insulin release and inhibits excessive glucagon secretion. Its activity is characterized by its ability to enhance GLP-1-mediated cAMP accumulation in GLP-1R-expressing cells.
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| ln Vivo |
In vivo, GLP-1R modulator C16 would be expected to exert beneficial metabolic effects through GLP-1R potentiation. By enhancing GLP-1 signaling, it could improve glycemic control, reduce body weight, and slow gastric emptying. Its effects in vivo would be assessed in animal models of type 2 diabetes and obesity.
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| Enzyme Assay |
In vitro binding and functional assays are used to characterize GLP-1R modulator C16 as a GLP-1R PAM. 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 8.43 μM and confirm its PAM activity.
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| Cell Assay |
Cellular assays for GLP-1R modulator C16 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 8.43 μM, confirming its PAM activity.
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| Animal Protocol |
In vivo efficacy of GLP-1R modulator C16 would be evaluated in animal models of type 2 diabetes and obesity. The compound could be administered orally, and its effects on glucose tolerance, insulin secretion, body weight, and food intake would be assessed. Its potential for treating metabolic disorders is an area of investigation.
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| ADME/Pharmacokinetics |
GLP-1R modulator C16 has a molecular formula of C21H26ClFN2O3 and a molecular weight of 408.89. As a small-molecule GLP-1R PAM, its pharmacokinetic properties would support oral dosing. 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 C16. As a GLP-1R PAM, its safety profile would be an important consideration. Potential toxicities could be related to its effects on GLP-1 signaling in various tissues. 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 C16 (CAS#: 875005-43-9) is a small-molecule positive allosteric modulator of the GLP-1 receptor. It enhances GLP-1 binding via a transmembrane site with an EC50 of 8.43 μM. It promotes glucose-dependent insulin release and inhibits glucagon secretion. It has a molecular formula of C21H26ClFN2O3 and a molecular weight of 408.89.
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| Molecular Formula |
C21H26CLFN2O3
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| Molecular Weight |
408.894148349762
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| Exact Mass |
408.161
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| CAS # |
875005-43-9
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| PubChem CID |
3162206
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
28
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=CC=C(C=1COC1C=CC(=CC=1OC)CNCCN1CCOCC1)F
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| InChi Key |
PQAPAXXUERVALT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H26ClFN2O3/c1-26-21-13-16(14-24-7-8-25-9-11-27-12-10-25)5-6-20(21)28-15-17-18(22)3-2-4-19(17)23/h2-6,13,24H,7-12,14-15H2,1H3
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| Chemical Name |
N-[[4-[(2-chloro-6-fluorophenyl)methoxy]-3-methoxyphenyl]methyl]-2-morpholin-4-ylethanamine
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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: 50 mg/mL (122.28 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4456 mL | 12.2282 mL | 24.4565 mL | |
| 5 mM | 0.4891 mL | 2.4456 mL | 4.8913 mL | |
| 10 mM | 0.2446 mL | 1.2228 mL | 2.4456 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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