Orforglipron
Orforglipron Basic information
- Product Name:
- Orforglipron
- Synonyms:
-
- 1,2,4-Oxadiazol-5(2H)-one, 3-[(1S,2S)-1-[2-[[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2,3-dihydro-2-oxo-1H-imidazol-1-yl]-2,4,6,7-tetrahydro-4-methyl-5H-pyrazolo[4,3-c]pyridin-5-yl]carbonyl]-5-[(4S)-tetrahydro-2,2-dimethyl-2H-pyran-4-yl]-1H-indol-1-yl]-2-methylcy...
- LY3502970
- GLP-1 receptor agonist 1 USP/EP/BP
- Orforglipron
- Orforglipron（LY3502970）
- LY3502970 (Orforglipron)
- 3-((1S,2S)-1-(5-((S)-2,2-dimethyltetrahydro-2H-pyran-4-yl)-2-((S)-3-(3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl)-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-5-carbonyl)-1H-indol-1-yl)-2-methylcyclopropyl)-1,2,4-oxadiazol-5(4H)-one
- OWL 833
- CAS:
- 2212020-52-3
- MF:
- C48H48F2N10O5
- MW:
- 882.97
- EINECS:
- 278-636-5
- Product Categories:
-
- 1
- ADVANCED INT.
- API
- Mol File:
- 2212020-52-3.mol
Orforglipron Chemical Properties
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 125 mg/mL (141.57 mM)
- form
- Solid
- pka
- 7.33±0.20(Predicted)
- color
- Off-white to light yellow
- InChIKey
- USUWIEBBBWHKNI-BBGRWQLENA-N
Orforglipron Usage And Synthesis
Description
Orforglipron (LY3502970) (GLP-1 receptor agonist 1) is GLP-1 receptor agonist extracted from patent WO2018056453A1, Compound 67.
History
Orforglipron is an oral, non-peptide, small-molecule glucagon-like peptide-1 receptor agonist developed by Eli Lilly and Company as a weight-loss drug. Currently, the drug is still in Phase III clinical trials and has not yet received approval from the U.S. Food and Drug Administration (FDA). Eli Lilly's CEO expects the FDA to approve its investigational oral weight-loss drug, orforglipron, by March 2026, and to submit an application for the treatment of type 2 diabetes by the end of 2026.
Uses
Orforglipron is a non-peptide oral glucagon-like peptide-1 receptor agonist (GLP-1RA) widely used in the management of type 2 diabetes mellitus (T2DM) and obesity. In T2DM patients, the drug reduces glycated haemoglobin (HbA1c) by up to 2.10%, facilitates weight loss of up to 10.1 kilograms, and reduces waist circumference by up to 8.7 centimetres. Studies in overweight or obese populations indicate weight loss of up to 13.0 kilograms. Adverse reactions include mild to moderate vomiting and nausea, particularly common following high-dose therapy or rapid dose escalation. Consequently, it should be used cautiously under medical supervision.
Uses
Glucagon-like peptide-1 (GLP-1) agonists (also known as GLP-1 receptor agonists, incretin mimetics, or GLP-1 analogs) represent a class of medications used to treat type 2 diabetes mellitus and, in some cases, obesity.
in vivo
Orforglipron (0.94-4.8 nM in plasma concentration, i.v., or 0.05-0.1 mg/mL, i.g. for 5 days) suppresses food intake in a dose-dependent manner, promotes insulin secretion and decreases blood glucose in cynomolgus monkey model[1].
Orforglipron (0.05-1.35 mg/kg, i.g.) reaches Cmax 2 hours after administration at all doses, exhibits proportional ratio of increase in plasma drug exposure to dose increase, indicates a dose-dependent absorption in the gastrointestinal tract[1].
Pharmacokinetic Analysis of Orforglipron in cynomolgus monkey [1]
| route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | AUC0-24h (ng·h/mL) |
| i.g. | 0.05 | 2.0 | 4.78 | 23.7 |
| i.g. | 0.15 | 2.0 | 20.7 | 135 |
| i.g. | 0.45 | 2.0 | 32.0 | 208 |
| i.g. | 1.35 | 2.0 | 148 | 1040 |
| Animal Model: | cynomolgus monkey model[1] |
| Dosage: | 0.9-4.8 nM; 0.05-0.1 mg/mL |
| Administration: | continuous i.v. administration for 30 minutes until a plasma concentration of 0.9-4.8 nM at steady state; i.g. for 5 days with dose of 0.05-0.1 mg/mL |
| Result: | Increased insulin secretion and decreased plasma-glucose. Suppressed food intake in a dose-dependent manner. |
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Orforglipron(2212020-52-3)Related Product Information
- (S,E)-1-(4-fluoro-1-methyl-1H-indazol-5-yl)-3-(2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridin-3-yl)-1-(2-hydroxyvinyl)urea
- \\
- 5-[(S)-2,2-Dimethyltetrahydro-2H-pyran-4-yl]-1-[(1S,2S)-2-methyl-1-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)cyclopropyl]-1H-indole-2-carboxylic Acid
- 1H-Indole-2-carboxamide, N-methyl-N-phenyl-5-[(4S)-tetrahydro-2,2-dimethyl-2H-pyran-4-yl]-
- (R)-1-(4-fluoro-1-methyl-1H-indazol-5-yl)-3-(2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridin-3-yl)-1,3-dihydro-2H-imidazol-2-one
- 3-((1S,2R)-1-(5-((R)-2,2-dimethyltetrahydro-2H-pyran-4-yl)-2-((R)-3- (3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1Himidazol-1-yl)-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7- tetrahydro-2H-pyrazolo[4,3-c]pyridine-5-carbonyl)-1H-indol-1-yl)-2- methylcyclopropyl)-1,2,4-oxadiazol-5(4H)-one
- Ly3502970