| Identification | Back Directory | [Name]
GLP-1 receptor agonist 1 | [CAS]
2212020-52-3 | [Synonyms]
LY3502970
Orforglipron
GLP-1 receptor agonist 1 USP/EP/BP
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... | [EINECS(EC#)]
278-636-5 | [Molecular Formula]
C48H48F2N10O5 | [MOL File]
2212020-52-3.mol | [Molecular Weight]
882.97 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
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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