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编 号:F620450
分子式:C48H48F2N10O5
分子量:882.96
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete.

体内研究:
Orforglipron (血浆浓度达到 0.94-4.8 nM in plasma concentration,静脉注射 30 反正;或 0.05-0.1 mg/mL,灌胃,5天) 在食蟹猴动物模型中以剂量依赖的方式抑制食蟹猴的食物摄取,促进胰岛素分泌并降低血糖。Orforglipron (0.05-1.35 mg/kg,灌胃) 在给药 2 小时后达到最大血浆浓度 Cmax,血浆药物暴露增加与剂量增加大致呈正比,表明 Orforglipron 在胃肠道中呈剂量依赖性的被吸收。Orforglipron 在食蟹猴体内的药代动力学分析routeDose (mg/kg)Tmax (h)Cmax (ng/mL)AUC0-24h (ng·h/mL)
i.g.0.052.04.7823.7
i.g.0.152.020.7135
i.g.0.452.032.0208
i.g.1.352.01481040
Animal Model:cynomolgus monkey model
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.

体外研究:
Orforglipron is an incretin secreted from L cells of the small intestine when nutrients pass through the digestive tract, and glucose is transmitted via the GLP-1 receptor. Orforglipron exhibits various actions such as dependent gastric emptying delay, and feeding suppression.
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