| 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... | [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. | [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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