254740-64-2

中文名称 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

英文名称 Sparsentan (RE-021)

CAS 254740-64-2

分子式 C32H40N4O5S

分子量 592.75

MOL 文件 254740-64-2.mol

更新日期 2025/05/17 14:37:10

254740-64-2 结构式

基本信息物理化学性质安全数据司帕生坦价格(试剂级) 常见问题列表

基本信息

中文别名

化合物SPARSENTAN
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

英文别名

RE 201
RE-021
PS433540
Sparsentan
BMS-346567
Sparsentan (RE-021)
Sparsentan(PS433540)
formerly known as DARA
Sparsentan-d5 (RE-021-d5)
PS433540
RE-021
FORMERLY KNOWN AS DARA

所属类别

生物：小分子化合物

物理化学性质

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-20°C储存

溶解度可溶于DMSO

酸度系数(pKa)7.06±0.50(Predicted)

形态结晶固体

颜色White to off-white

InChIKeyWRFHGDPIDHPWIQ-UHFFFAOYSA-N

SMILESC1(C2=CC=C(CN3C(=O)C4(CCCC4)N=C3CCCC)C=C2COCC)=CC=CC=C1S(NC1C(C)=C(C)ON=1)(=O)=O

安全数据

危险性符号(GHS) GHS hazard pictograms

GHS07

警示词警告

危险性描述H315-H319

防范说明P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

司帕生坦价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2025/02/08	HY-17621	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	254740-64-2	5mg	642元
2025/02/08	HY-17621	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	254740-64-2	10mM * 1mLin DMSO	837元
2025/02/08	HY-17621	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	254740-64-2	10mg	1044元

常见问题列表

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.