ChemicalBook CAS数据库列表 4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺

4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺

CAS号:254740-64-2
英文名:Sparsentan (RE-021)
中文名:4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺
CBNumber:CB12707221
分子式:C32H40N4O5S
分子量:592.75
MOL File:254740-64-2.mol

4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺化学性质

熔点 :148 °C(Solv: isopropanol (67-63-0); water (7732-18-5))
沸点 :744.4±70.0 °C(Predicted)
密度 :1.28±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: soluble
形态 :A crystalline solid
酸度系数(pKa) :7.06±0.50(Predicted)
InChIKey :WRFHGDPIDHPWIQ-UHFFFAOYSA-N
SMILES :C1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2COCC)=CC=CC=C1S(NC1C(C)=C(C)ON=1)(=O)=O

4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺性质、用途与生产工艺

生物活性 Sparsentan (PS-433540, RE-021, DARA) 是endothelin type A receptor(ETA)和angiotensin II type 1 receptor的双重拮抗剂。
靶点
Target Value
endothelin type A receptor
()
angiotensin II type 1 receptor
()
体内研究

Sparsentan dose dependently antagonizes the angiotensin II-induced pressor response with an ED ₅₀ value of 0.8 µmol/kg iv and 3.6 µmol/kg po. Sparsentan also shows efficacious and long acting in the big ET-1-induced pressor model. Sparsentan causes a significant lowering of blood pressure at the lowest dose tested (10 µmol/kg/day) in spontaneously hypertensive rats. Sparsentan shows good oral bioavailability in rats, dogs, and monkeys, averaging 40%, 86%, and 21% F, respectively. At 100 µmol/kg/day, Sparsentan reduces the blood pressure from 170 to less than 100 mmHg during the course of the drug’s pharmacokinetic duration. Sparsentan at 100 µmol/kg/day essentially converts the spontaneously hypertensive rats into normotensive rats during the course of its pharmacokinetic duration.

4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺上下游产品信息

上游原料

下游产品

更新日期：2024/04/30
产品编号：HY-17621
产品名称：4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺 Sparsentan
CAS编号：254740-64-2
包装：5mg
价格：1100元

4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺生产厂家

254740-64-2, 4'-[(2-丁基-4-氧代-1,3-二氮杂螺[4.4]壬-1-烯-3-基)甲基]-N-(4,5-二甲基-3-异恶唑基)-2'-(乙氧基甲基)-[1,1'-联苯]-2-磺酰胺相关搜索:

Target	Value
endothelin type A receptor ()
angiotensin II type 1 receptor ()