GLP-1R Antagonist 1
Based on 7 publication(s) in Google Scholar
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
For research use only. We do not sell to patients.
- Purity: 99.67%
- CAS No.: 488097-06-9
- Formula: C16H11ClF6N4O2
- Molecular Weight:440.73
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GLP-1R Antagonist 1
More- Nat Commun. 2024 Sep 12;15(1):7991. [Abstract]
- Arch Pharm Res. 2026 Apr;49(4):554-574. [Abstract]
- Antioxid Redox Signal. 2025 Dec;43(16-18):819-832. [Abstract]
- Eur J Pharmacol. 2025 Aug 5:1000:177722. [Abstract]
- Hypertens Res. 2026 Apr 10.
- Sci Rep. 2025 Apr 3;15(1):11486. [Abstract]
- Acta Biochim Biophys Sin (Shanghai). 2023 Nov 15;55(12):1855-1863. [Abstract]
Biological Activity
IC50: 650 nM (GLP-1R)[1].
Pharmacokinetic Analysis in MC38 Syngeneic Model[1]
| Route | Dose (mg/kg) | CLp (mL/min/kg) | t1/2 (min) | Vss (L/kg) | %F |
| i.v., p.o. | 1, 3 | 4.79 | 587 | 3.57 | 50 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 488097-06-9
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Appearance Solid
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Molecular Weight 440.73
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Formula C16H11ClF6N4O2
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Color White to light yellow
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SMILES
O=C1C2=C(NC(C3=CC=C(Cl)C=C3)=NC2(C(F)(F)F)C(F)(F)F)N(C)C(N1C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Adipocyte inflammation is the primary driver of hepatic insulin resistance in a human iPSC-based microphysiological system. [Abstract]2024 Sep 12;15(1):7991. PMID: 39266553 -
Arch Pharm Res
Tirzepatide mitigates atherosclerosis progression and modulates oxLDL-mediated proatherogenic effects in macrophages: evidence for M1/M2 homeostasis restoration. [Abstract]2026 Apr;49(4):554-574. PMID: 41904760 -
Antioxid Redox Signal
D-Allulose Regulates Obesity via Endoplasmic Reticulum Stress-Mediated Glucagon-Like Peptide-1 Receptor Pathway. [Abstract]2025 Dec;43(16-18):819-832. PMID: 41327798 -
Eur J Pharmacol
Involvement of glucagon-like peptide-1 receptor in fisetin tetramethyl ether-enhanced insulin secretion in MIN6 cells. [Abstract]2025 Aug 5:1000:177722. PMID: 40348320 -
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Sci Rep
Glucagon like peptide-1 modulates urinary sodium excretion in diabetic kidney disease via ENaC activation. [Abstract]2025 Apr 3;15(1):11486. PMID: 40181096 -
Acta Biochim Biophys Sin (Shanghai)
Evolution of GCGR family ligand-receptor extensive cross-interaction systems suggests a therapeutic direction for hyperglycemia in mammals. [Abstract]2023 Nov 15;55(12):1855-1863. PMID: 37969012
Solvent & Solubility
DMSO : 100 mg/mL (226.90 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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.
Purity & Documentation
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Data Sheet (277 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]. Kellie D. Nance, et al. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core. J. Med. Chem. 19 Jan 2017. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2690 mL | 11.3448 mL | 22.6896 mL | 56.7241 mL |
| 5 mM | 0.4538 mL | 2.2690 mL | 4.5379 mL | 11.3448 mL | |
| 10 mM | 0.2269 mL | 1.1345 mL | 2.2690 mL | 5.6724 mL | |
| 15 mM | 0.1513 mL | 0.7563 mL | 1.5126 mL | 3.7816 mL | |
| 20 mM | 0.1134 mL | 0.5672 mL | 1.1345 mL | 2.8362 mL | |
| 25 mM | 0.0908 mL | 0.4538 mL | 0.9076 mL | 2.2690 mL | |
| 30 mM | 0.0756 mL | 0.3782 mL | 0.7563 mL | 1.8908 mL | |
| 40 mM | 0.0567 mL | 0.2836 mL | 0.5672 mL | 1.4181 mL | |
| 50 mM | 0.0454 mL | 0.2269 mL | 0.4538 mL | 1.1345 mL | |
| 60 mM | 0.0378 mL | 0.1891 mL | 0.3782 mL | 0.9454 mL | |
| 80 mM | 0.0284 mL | 0.1418 mL | 0.2836 mL | 0.7091 mL | |
| 100 mM | 0.0227 mL | 0.1134 mL | 0.2269 mL | 0.5672 mL |
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