169545-27-1
中文名称
N-3-[1,1'-BIPHENYL]-4-YL-N-(3,5-DIMETHYLBENZOYL)-N-METHYL-D-ALANYL-L-TRYPTOPHAN
英文名称
IRL-2500
CAS
169545-27-1
分子式
C36H35N3O4
分子量
573.68
MOL 文件
169545-27-1.mol
更新日期
2024/07/12 22:21:22
169545-27-1 结构式
基本信息
中文别名
T15596化合物 T15596
化合物IRL 2500
(S)-2-((R)-3-([1,1'-联苯]-4-基)-2-(N,3,5-三甲基苯甲酰胺基)丙酰胺基)-3-(1H-吲哚-3-基)丙酸
英文别名
IRL-2500L-Tryptophan, 3-[1,1'-biphenyl]-4-yl-N-(3,5-dimethylbenzoyl)-N-methyl-D-alanyl-
N-3-[1,1'-BIPHENYL]-4-YL-N-(3,5-DIMETHYLBENZOYL)-N-METHYL-D-ALANYL-L-TRYPTOPHAN
物理化学性质
沸点893.7±65.0 °C(Predicted)
密度1.246±0.06 g/cm3(Predicted)
储存条件Keep in dark place,Sealed in dry,Store in freezer, under -20°C
溶解度Soluble to 100 mM in 1eq. NaOH
酸度系数(pKa)3.34±0.10(Predicted)
形态粉末
颜色White to light yellow
常见问题列表
生物活性
IRL 2500 是一种有效的内皮素受体 (Endothelin receptor) 拮抗剂，其 ETB 和 ETA 受体的 IC50 值分别为 1.3 和 94 nM。 IRL 2500 在体内抑制 ETB 受体介导的血压升高和肾血管阻力。靶点
|
ET B 1.3 nM (IC 50 ) |
ET A 94 nM (IC 50 ) |
体内研究
IRL 2500 (intravenous injection;10 mg/kg) inhibits the initial transient decrease in mean arterial pressure (MAP) induced by the ETB-selective agonist IRL 1620 in rats, IRL 2500 also attenuates the IRL 1620-mediated increase in renal vascular resistance (RVR) in the anesthetized rat. IRL 2500 (intravenous injection;10 mg/kg) pre-reatment significantly reduces the initial vasodepressor response to endothelin-1 (ET-1) and IRL 1620, however, it is not alters the secondary and sustained pressor response to these agonists.