| Identification | Back Directory | [Name]
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-methylcyclopropyl]-, calcium salt, hydrate (2:1:2) | [CAS]
3008544-96-2 | [Synonyms]
Orforglipronhemicalciumhydrate
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-methylcyclopropyl]-, calcium salt, hydrate (2:1:2) |
| Hazard Information | Back Directory | [Uses]
Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete[1]. | [in vivo]
Orforglipron hemicalcium hydrate (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 blood glucose reduction in cynomolgus monkey model[1].
Orforglipron hemicalcium hydrate (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 hemicalcium hydrate 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; or 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. |
| [References]
[1] Pyrazolopyridine derivative having glp-1 receptor agonist effect. WO2018056453A1 |
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