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编 号：F755863
分子式：C21H23ClN4O5
分子量：446.88
分子式：C21H23ClN4O5
分子量：446.88
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CAS No: 2768219-28-7
产品详情
生物活性：
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research.
体内研究：
PHD2-IN-1 (Compound 22) (10,20,50 mg/kg 口服，每日一次持续三天) 在 C57BL/6 小鼠中刺激红细胞生成并以剂量依赖性方式增加网织红细胞。PHD2-IN-1 (50,100,200 mg/kg，腹腔注射, 每日一次持续三天) 对 ICR 小鼠无明显毒性反应。PHD2-IN-1 (静脉注射1 mg/kg，口服10 mg/kg) 显示在大鼠中 T1/2 为 2.29 小时 (口服) 或 3.72 小时 (静脉注射)，在小鼠中 T1/2 为 1.17 小时 (口服) 或 0.33 小时 (静脉注射)。在大鼠和小鼠中的口服生物利用度 (F%) 分别为 33.9% 和 35.3%。 Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice SpeciesRouteDose (mg/kg)Tmax (h) Cmax (ng/mL)AUC0-t (h?ng/mL)AUC0-? (h?ng/mL)T1/2 (h) CL (mL?min-1/kg-1)VZ (mL/kg)MRT0-? (h)F (%)
ratp.o.100.0826140711871352.29141746290.5633.9
rati.v.1//206921063.7248326441.54/
micep.o.100.53036447544891.17224645321.6735.3
micei.v.1//138413870.337213450.53/
Animal Model:C57BL/6 mice
Dosage:10,20, and 50 mg/kg
Administration:Oral gavage (p.o.), once daily for three days
Result:Increased reticulocytes in a dose-dependent manner. The reticulocyte count/red blood cell count (RBC%) increased significantly in a dose-dependent manner.
Animal Model:SD rats and C57BL/6 mice (Pharmacokinetic assay)
Dosage:1, 10 mg/kg
Administration:Intravenous injection (i.v.)，Oral gavage (p.o.)
Result:Showed T1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice.
Animal Model:Subacute toxicity assessment in ICR mice
Dosage:50,100,200 mg/kg
Administration:Intraperitoneal injection (i.p.) once daily for 14 days
Result:Had no significant hepatotoxicity or nephrotoxicity reactions after administration of a high dose of 200 mg/kg, at 10 imes the efficacious dose (20mg/kg). Observed no death or behavioral abnormalities when the mice were treatedin the dose of 800 mg/kg by p.o. administration.
体外研究：
PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 小时) 稳定 HIF-α 并增加促红细胞生成素 (EPO) 基因的表达。
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research.
体内研究：
PHD2-IN-1 (Compound 22) (10,20,50 mg/kg 口服，每日一次持续三天) 在 C57BL/6 小鼠中刺激红细胞生成并以剂量依赖性方式增加网织红细胞。PHD2-IN-1 (50,100,200 mg/kg，腹腔注射, 每日一次持续三天) 对 ICR 小鼠无明显毒性反应。PHD2-IN-1 (静脉注射1 mg/kg，口服10 mg/kg) 显示在大鼠中 T1/2 为 2.29 小时 (口服) 或 3.72 小时 (静脉注射)，在小鼠中 T1/2 为 1.17 小时 (口服) 或 0.33 小时 (静脉注射)。在大鼠和小鼠中的口服生物利用度 (F%) 分别为 33.9% 和 35.3%。 Pharmacokinetic parameters for PHD2-IN-1 (Compound 22) in SD rats and C57BL/6 mice SpeciesRouteDose (mg/kg)Tmax (h) Cmax (ng/mL)AUC0-t (h?ng/mL)AUC0-? (h?ng/mL)T1/2 (h) CL (mL?min-1/kg-1)VZ (mL/kg)MRT0-? (h)F (%)
ratp.o.100.0826140711871352.29141746290.5633.9
rati.v.1//206921063.7248326441.54/
micep.o.100.53036447544891.17224645321.6735.3
micei.v.1//138413870.337213450.53/
Animal Model:C57BL/6 mice
Dosage:10,20, and 50 mg/kg
Administration:Oral gavage (p.o.), once daily for three days
Result:Increased reticulocytes in a dose-dependent manner. The reticulocyte count/red blood cell count (RBC%) increased significantly in a dose-dependent manner.
Animal Model:SD rats and C57BL/6 mice (Pharmacokinetic assay)
Dosage:1, 10 mg/kg
Administration:Intravenous injection (i.v.)，Oral gavage (p.o.)
Result:Showed T1/2s of 2.29 h (p.o.) or 3.72 h (i.v.) in rats and 1.17 h (p.o.) or 0.33 h (i.v.) in mice. And oral bioavailability (F%) of 33.9% in rats and 35.3% in mice.
Animal Model:Subacute toxicity assessment in ICR mice
Dosage:50,100,200 mg/kg
Administration:Intraperitoneal injection (i.p.) once daily for 14 days
Result:Had no significant hepatotoxicity or nephrotoxicity reactions after administration of a high dose of 200 mg/kg, at 10 imes the efficacious dose (20mg/kg). Observed no death or behavioral abnormalities when the mice were treatedin the dose of 800 mg/kg by p.o. administration.
体外研究：
PHD2-IN-1 (Compound 22) ( 0-50 μM; 12 小时) 稳定 HIF-α 并增加促红细胞生成素 (EPO) 基因的表达。
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