产品
编 号：F271602
分子式：C18H24N6O7S2
分子量：500.55
分子式：C18H24N6O7S2
分子量：500.55
产品类型
规格
价格
是否有货
结构图
CAS No: 2122196-16-9
产品详情
生物活性：
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
体内研究：
PSB 0777 ammonium (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture. PSB 0777 ammonium (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice.PSB 0777 ammonium cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min. Animal Model:Albino male Sprague-Dawley rats of 200 g with Oxazolone-induced colitis
Dosage:0.4 mg/kg
Administration:Oral gavage; daily; from the day 5 to 10
Result:Caused a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture alone or in combination with Dexamethasone (1 mg/kg/day). Counteracted significantly the increment of colonic myeloperoxidase (MPO) levels associated with colitis.
体外研究：
PSB 0777 ammonium (compound 7) shows high selectivity for the A2AAR (>225-fold) versus the other AR subtypes (Ki values of >10000 nM and ?10000 for human A2B receptor and A3 receptor, respectively). PSB 0777 ammonium acts as an full agonist at A2AAR with an EC50 value of 117 nM in CHO-K1 cells. PSB-0777 ammonium binds human β1 (Ki=4.4 μM) and β3 (Ki=3.3 μM) adrenergic receptors. PSB 0777 ammonium (0.1 μM, 1 μM, 10 μM) increases concentration-dependently Acetylcholine (Ach, 1 mM) contractions in untreated and inflamed rat ileum/jejunum preparations in ex vivo experiments.
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
体内研究：
PSB 0777 ammonium (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture. PSB 0777 ammonium (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice.PSB 0777 ammonium cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min. Animal Model:Albino male Sprague-Dawley rats of 200 g with Oxazolone-induced colitis
Dosage:0.4 mg/kg
Administration:Oral gavage; daily; from the day 5 to 10
Result:Caused a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture alone or in combination with Dexamethasone (1 mg/kg/day). Counteracted significantly the increment of colonic myeloperoxidase (MPO) levels associated with colitis.
体外研究：
PSB 0777 ammonium (compound 7) shows high selectivity for the A2AAR (>225-fold) versus the other AR subtypes (Ki values of >10000 nM and ?10000 for human A2B receptor and A3 receptor, respectively). PSB 0777 ammonium acts as an full agonist at A2AAR with an EC50 value of 117 nM in CHO-K1 cells. PSB-0777 ammonium binds human β1 (Ki=4.4 μM) and β3 (Ki=3.3 μM) adrenergic receptors. PSB 0777 ammonium (0.1 μM, 1 μM, 10 μM) increases concentration-dependently Acetylcholine (Ach, 1 mM) contractions in untreated and inflamed rat ileum/jejunum preparations in ex vivo experiments.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备