Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4].
产品描述 | SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4]. |
靶点活性 | S1PR1:12.6-493 nM (EC50) |
体外活性 | 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[1]. SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner[1]. SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca 2+ flux assay in S1P1-Chinese hamster ovary (CHO) cells[1]. |
体内活性 | 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[1]. SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction[1]. SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (C max and AUC) increases with dose in pigs. Pharmacokinetic parameters[1]: Dose (mg/kg) N C max (g/mL) T max (h) T last (h) AUC 0-last (g.h/mL) Cl (L/h/kg) Vss (L/kg) T 1/2z (h) 1 4 2.08 (8) 0.5 [0.5] [8-48] 11.8 (46) 0.113 (75) 0.516 (11) 5.62 (57) 3 7 8.10 (12) 0.5 [0.5] [24-72] 42.2 (23) 0.0754 (30) 0.446 (16) 6.21 (28) 10 3 36.7 (5) 0.5 [0.5-0.75] 72 294 (13) 0.0343 (13) 0.338 (7) 7.73 (8) 30 6 112 (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 T max , which is expressed as median value with [range] and Tlast as [range]. C max , maximum concentration. T max , time at which maximum concentration achieved. T last , last time point sampled. AUC 0-last , area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T 1/2z , elimination half-life. N, number of animals. Animal Model: Acute kidney injury rats (12 to 15-week-old Fischer rats)[1]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)[1]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. |
别名 | SAR247799, S1P1 agonist 3 |
分子量 | 425.83 |
分子式 | C21H16ClN3O5 |
CAS No. | 1315311-14-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SAR247799 1315311-14-8 SAR 247799 S1P1 agonist 3 SAR-247799 Inhibitor inhibitor inhibit