产品
编 号：F744051
分子式：C21H16ClN3O5
分子量：425.82
分子式：C21H16ClN3O5
分子量：425.82
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1315311-14-8
产品详情
生物活性：
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.
体内研究：
SAR247799 (1 and 3 mg/kg; p.o.; 1 h before renal occlusion) dose dependently reduces the severity of ischemia/reperfusion (I/R)–induced acute kidney injury.SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction.SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (Cmax and AUC) increases with dose in pigs. Pharmacokinetic parameters :Dose (mg/kg)NCmax (g/mL)Tmax (h)Tlast (h)AUC0-last (g.h/mL)Cl (L/h/kg)Vss (L/kg)T1/2z (h)
142.08 (8)0.5 [0.5][8-48]11.8 (46)0.113 (75)0.516 (11)5.62 (57)
378.10 (12)0.5 [0.5][24-72]42.2 (23)0.0754 (30)0.446 (16)6.21 (28)
10336.7 (5)0.5 [0.5-0.75]72294 (13)0.0343 (13)0.338 (7)7.73 (8)
306112 (27)0.5 [0.5- 1.0][48-72]908 (16)0.0338 (18)0.294 (11)7.35 (11)
Mean values with (CV%) except Tmax, which is expressed as median value with [range] and Tlast as [range]. Cmax, maximum concentration. Tmax, time at which maximum concentration achieved. Tlast, last time point sampled. AUC0-last, area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T1/2z, elimination half-life. N, number of animals.Animal Model:Acute kidney injury rats (12 to 15-week-old Fischer rats)
Dosage:1 and 3 mg/kg
Administration:P.o.; administered 1 hour before renal occlusion.
Result:Inhibited the increase in serum creatinine (89 and 96% at 1 and 3 mg/kg) and urea (61 and 85% at 1 and 3 mg/kg).Protected renal proximal tubules against necrosis and blunted the development of interstitial hemorrhage.
Animal Model:Acute kidney injury rats (8- to 12-week-old Fischer rats)
Dosage:3 mg/kg
Administration:P.o.; twice a day for 7 days and twice a day for 7 day
Result:Showed a dosedependent trend for reducing macrophage.
体外研究：
SAR247799 (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 10 min) induces a concentration-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt) in HUVECs.SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner.SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca2+ flux assay in S1P1-Chinese hamster ovary (CHO) cells.
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.
体内研究：
SAR247799 (1 and 3 mg/kg; p.o.; 1 h before renal occlusion) dose dependently reduces the severity of ischemia/reperfusion (I/R)–induced acute kidney injury.SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction.SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (Cmax and AUC) increases with dose in pigs. Pharmacokinetic parameters :Dose (mg/kg)NCmax (g/mL)Tmax (h)Tlast (h)AUC0-last (g.h/mL)Cl (L/h/kg)Vss (L/kg)T1/2z (h)
142.08 (8)0.5 [0.5][8-48]11.8 (46)0.113 (75)0.516 (11)5.62 (57)
378.10 (12)0.5 [0.5][24-72]42.2 (23)0.0754 (30)0.446 (16)6.21 (28)
10336.7 (5)0.5 [0.5-0.75]72294 (13)0.0343 (13)0.338 (7)7.73 (8)
306112 (27)0.5 [0.5- 1.0][48-72]908 (16)0.0338 (18)0.294 (11)7.35 (11)
Mean values with (CV%) except Tmax, which is expressed as median value with [range] and Tlast as [range]. Cmax, maximum concentration. Tmax, time at which maximum concentration achieved. Tlast, last time point sampled. AUC0-last, area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T1/2z, elimination half-life. N, number of animals.Animal Model:Acute kidney injury rats (12 to 15-week-old Fischer rats)
Dosage:1 and 3 mg/kg
Administration:P.o.; administered 1 hour before renal occlusion.
Result:Inhibited the increase in serum creatinine (89 and 96% at 1 and 3 mg/kg) and urea (61 and 85% at 1 and 3 mg/kg).Protected renal proximal tubules against necrosis and blunted the development of interstitial hemorrhage.
Animal Model:Acute kidney injury rats (8- to 12-week-old Fischer rats)
Dosage:3 mg/kg
Administration:P.o.; twice a day for 7 days and twice a day for 7 day
Result:Showed a dosedependent trend for reducing macrophage.
体外研究：
SAR247799 (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 10 min) induces a concentration-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt) in HUVECs.SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner.SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca2+ flux assay in S1P1-Chinese hamster ovary (CHO) cells.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备