540769-28-6

中文名稱 ACT 058362; PALOSURAN,

英文名稱 Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-

CAS 540769-28-6

分子式 C25H30N4O2

分子量 418.53

MOL 文件 540769-28-6.mol

更新日期 2026/06/09 18:09:49

540769-28-6 結(jié)構(gòu)式

基本信息物理化學(xué)性質(zhì) 安全數(shù)據(jù) 圖譜信息 ACT 058362; PALOSURAN,價格(試劑級) 常見問題列表

基本信息

中文別名

化合物PALOSURAN

英文別名

Palosuran
ACT 058362
PALOSURAN,, >98%
ACT058362
ACT-058362
ACT 058362
PALOSURAN,
ACT 058362
PALOSURAN,, >98%
1-[2-(4-Benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
N-[2-[4-Hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)urea
Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-

物理化學(xué)性質(zhì)

沸點612.9±55.0 °C(Predicted)

密度1.235±0.06 g/cm3(Predicted)

儲存條件-20°C儲存

溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 0.5 mg/ml

酸度系數(shù)(pKa)12.95±0.43(Predicted)

形態(tài)結(jié)晶固體

顏色White to pink

InChI1S/C25H30N4O2/c1-19-17-23(21-9-5-6-10-22(21)27-19)28-24(30)26-13-16-29-14-11-25(31,12-15-29)18-20-7-3-2-4-8-20/h2-10,17,31H,11-16,18H2,1H3,(H2,26,27,28,30)

InChIKeyWYJCYXOCHXWTHG-UHFFFAOYSA-N

SMILESN3(CCC(CC3)(O)Cc4ccccc4)CCNC(=O)Nc1c2c(nc(c1)C)cccc2

安全數(shù)據(jù)

危險性符號(GHS) 有害 (GHS07)

GHS07

警示詞警告

危險性描述H302-H315-H320-H335

防范說明P261-P280-P301+P312-P302+P352-P305+P351+P338

WGK GermanyWGK 3

存儲類別11 - Combustible Solids

圖譜信息

ACT 058362; PALOSURAN,(540769-28-6)核磁圖(¹HNMR)

ACT 058362; PALOSURAN,價格(試劑級)

報價日期	產(chǎn)品編號	產(chǎn)品名稱	CAS號	包裝	價格
2026/06/05	HY-10655R	ACT 058362; PALOSURAN, Palosuran (Standard)	540769-28-6	1 mg	800元
2026/06/05	HY-10655R	ACT 058362; PALOSURAN, Palosuran (Standard)	540769-28-6	5 mg	2000元
2026/06/05	HY-10655R	ACT 058362; PALOSURAN, Palosuran (Standard)	540769-28-6	10 mg	3250元

常見問題列表

生物活性

Palosuran (ACT-058362) 是一種有效，選擇性和具有口服活性的 urotensin II receptor 受體拮抗劑，對于表達人重組受體的 CHO 細胞膜的 IC50 值為 3.6 nM。Palosuran 可改善糖尿病大鼠的胰腺和腎臟功能。

靶點

IC50: 3.6 nM (human urotensin II receptor)

體外研究

Palosuran (8 h) inhibits ¹²⁵ I-U-II binding to human UT receptor, with IC ₅₀ s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells.
Palosuran inhibits Ca ²⁺ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC ₅₀ s of 17 and >10000 nM, respectively.
Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC ₅₀ of 150 nM.

體內(nèi)研究

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure.
Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats.

Animal Model:	Male Wistar rats with renal ischemia and reperfusion
Dosage:	20 mg/kg/h for 135 min
Administration:	I.v. (continuous infusion) for 135 min
Result:	Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values. Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).