Bioactivity | 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 (血浆浓度 0.94-4.8 nM,静脉注射 30 分钟;或 0.05-0.1 mg/mL,灌胃,5 天) 在食蟹猴动物模型中剂量依赖性地抑制食蟹猴的食物摄入,促进胰岛素分泌并降低血糖[1]。Orforglipron hemicalcium hydrate (0.05-1.35 mg/kg,灌胃) 在给药后 2 小时后达到 Cmax,血浆药物暴露增加与剂量增加大致成正比,表明 Orforglipron hemicalcium hydrate 在胃肠道内呈剂量依赖性的被吸收[1]。Orforglipron hemicalcium hydrate 在食蟹猴体内的药代动力学分析 [1]route |
CAS | 3008544-96-2 |
Formula | C48H48F2N10O5.1/2Ca.H2O |
Molar Mass | 921.02 |
Appearance | 固体 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Pyrazolopyridine derivative having glp-1 receptor agonist effect. WO2018056453A1 |