Semaglutide Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217 For research use only
Semaglutide, sold under the brand names Ozempic, Wegovy and Rybelsus, is an antidiabetic medication used for the treatment of type 2 diabetes and as anti-obesity medication for long-term weight management, developed by Novo Nordisk in 2012. Semaglutide is a GLP-1 receptor agonist, meaning that it mimics the action of the human incretin glucagon-like peptide-1 (GLP-1), thereby increasing insulin secretion and increasing blood sugar disposal and improving glycemic control. Side effects include nausea, vomiting, diarrhea, abdominal pain, and constipation. In December 2017, the injectable version named Ozempic was approved. In September 2019, a version which can be taken by mouth (Rybelsus) was approved, and in June 2021, a higher-dose injection sold under the brand name Wegovy for long-term weight management in adults was approved by the US Food and Drug Administration (FDA). In January of 2023, FDA gave Novo Nordisk permission to revise the label to indicate that oral Rybelsus can be used as a first-line treatment for adults with type 2 diabetes—meaning in people who have not previously taken another diabetes medication. In 2020, semaglutide was the 129th most commonly prescribed medication in the United States, with more than 4 million prescriptions. Synonyms: Rybelsus, Ozempic, NN9535, OG217SC, For research use only.
Biological Activity
| Description | Semaglutide (Rybelsus, Ozempic, NN9535, OG217SC, NNC 0113-0217), a long-acting glucagon-like peptide 1 (GLP-1) analogue, is a GLP-1 receptor agonist with the potential for the treatment of type 2 diabetes mellitus (T2DM). |
| Targets | GLP-1 receptor |
| In vitro | Semaglutide is selected as the optimal once weekly candidate. Semaglutide has two amino acid substitutions compared to human GLP-1 (Aib8, Arg34) and is derivatized at lysine 26. The GLP-1R affinity of semaglutide (0.38 ± 0.06 nM) is three-fold decreased compared to liraglutide, whereas the albumin affinity is increased. |
| In vivo | The plasma half-life is 46.1 h in mini-pigs following i.v. administration, and semaglutide has an MRT of 63.6 h after s.c. dosing to mini-pigs. |
Protocol (from reference)
| Cell Research: | ● Cell lines: BHK cells ● Concentrations: 0.01 pM – 0.1 μM ● Incubation Time: 3 h ● Method: Frozen aliquots of BHK cells that express both the hGLP-1R and CRE firefly luciferase (clone FCW467-12A/KZ10-1) are thawed, washed twice in PBS, and suspended in assay buffer. Cells are plated out into 96-well plates at 5000 cells/well in a volume of 50 μL. Compounds to be tested are diluted in assay buffer and a 50 μL aliquot transferred to the plate containing the cells to reach final assay concentrations of 1 × 10−14 − 1 × 10−7 M. The plate is incubated for 3 h at 5% CO2 at 37 °C. The plate was allowed to stand at room temperature for 15 min prior to adding 100 μL of steadylite plus reagent. The plate is covered to protect it from light and shaken at room temperature for 30 min. The plate is read in a TopCount NXT instrument. |
Solubility (25°C)
| In vitroBatch: | DMSO | 3 mg/mL(0.73 mM) |
| Ethanol | Insoluble | |
| Water | Insoluble |
Chemical Information
| Molecular Weight | 4113.58 | ||
| Formula | C187H291N45O59 | ||
| CAS No. | 910463-68-2 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Shipping | Room temperature shipping(Quality concern free: the product is good at 37℃ for at least 1 week.) | ||
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05537233 | Not yet recruiting | Drug: Semaglutide|Drug: Placebo | Type 1 Diabetes|Obesity | University of Colorado Denver|Juvenile Diabetes Research Foundation | January 1 2023 | Phase 2 |
| NCT04885634 | Not yet recruiting | Drug: Semaglutide Injectable Product|Drug: Placebo | Atrial Fibrillation|Overweight and Obesity | Axel Brandes|Herlev and Gentofte Hospital|Hillerod Hospital Denmark|Svendborg Hospital|Hospital of South West Jutland|Odense University Hospital | October 2022 | Phase 3 |
| NCT05579977 | Recruiting | Drug: PF-07081532|Other: Placebo|Drug: Rybelsus | Diabetes Mellitus|Obesity | Pfizer | October 27 2022 | Phase 2 |
| NCT05254314 | Recruiting | Drug: Semaglutide Pen Injector 2.4mg weekly|Other: Placebo | Asthma | Vanderbilt University Medical Center|National Institute of Allergy and Infectious Diseases (NIAID) | September 7 2022 | Phase 2 |
| NCT05478252 | Recruiting | Drug: Semaglutide J|Drug: Semaglutide B | Diabetes Mellitus Type 2 | Novo Nordisk A/S | August 3 2022 | Phase 3 |
(data from https://clinicaltrials.gov, updated on 2022-11-29)
