ChemicalBook > CAS DataBase List > Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-

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

Product Name
Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
CAS No.
540769-28-6
Chemical Name
Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
Synonyms
Palosuran;ACT 058362;PALOSURAN,, >98%;ACT058362;ACT-058362;Palosuran (ACT058362);ACT 058362; PALOSURAN,;Palosuran, 10 mM in DMSO;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
CBNumber
CB42628509
Molecular Formula
C25H30N4O2
Formula Weight
418.53
MOL File
540769-28-6.mol
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Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)- Property

Boiling point:
612.9±55.0 °C(Predicted)
Density 
1.235±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 0.5 mg/ml
form 
A crystalline solid
pka
12.95±0.43(Predicted)
color 
White to pink
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H320Causes eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23460
Product name
Palosuran
Packaging
1mg
Price
$110
Updated
2024/03/01
Cayman Chemical
Product number
23460
Product name
Palosuran
Packaging
10mg
Price
$864
Updated
2024/03/01
Cayman Chemical
Product number
23460
Product name
Palosuran
Packaging
5mg
Price
$459
Updated
2024/03/01
ApexBio Technology
Product number
B1304
Product name
Palosuran
Packaging
25mg
Price
$523
Updated
2021/12/16
ApexBio Technology
Product number
B1304
Product name
Palosuran
Packaging
50mg
Price
$855
Updated
2021/12/16
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Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)- Chemical Properties,Usage,Production

Description

Palosuran is an antagonist of the urotensin II receptor (UTR; IC50s = 3.6 and 1,475 nM for CHO cell membranes expressing human and rat recombinant receptors, respectively). It inhibits contraction of isolated rat aortic rings induced by urotensin II (Item Nos. 24711 | 24753) in a concentration-dependent manner. Palosuran (300 mg/kg twice per day) reduces plasma endothelin-1 , urotensin II, and TGF-β1 levels, as well as the main pulmonary arterial pressure and right ventricular hypertrophy index in a rat model of pulmonary arterial hypertension (PAH) induced by monocrotaline . Palosuran (300 mg/kg per day) reduces serum glucose, cholesterol, and triglyceride levels and increases survival in a rat model of diabetes induced by streptozotocin (STZ; ). It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.

Uses

Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats[1][2].

in vivo

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure[1].
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[2].

Animal Model:Male Wistar rats with renal ischemia and reperfusion[1]
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).

References

[1] Clozel M, et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System. J Pharmacol Exp Ther. 2004 Oct;311(1):204-12. DOI:10.1124/jpet.104.068320
[2] Clozel M, et al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21. DOI:10.1124/jpet.105.094821

Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)- Preparation Products And Raw materials

Raw materials

Preparation Products

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

China 61 India 1 United States 11 Global 73
Shanghai Boyle Chemical Co., Ltd.
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Haoyuan Chemexpress Co., Ltd.
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(86) 21-58955996
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View Lastest Price from Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)- manufacturers

Zhuozhou Wenxi import and Export Co., Ltd
Product
Palosuran 540769-28-6
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Palosuran 540769-28-6
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

540769-28-6, Urea, N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-Related Search:


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  • Palosuran
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  • ACT 058362; PALOSURAN,
  • 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
  • ACT058362;ACT-058362
  • ACT 058362; PALOSURAN,, >98%
  • PALOSURAN,, >98%
  • Palosuran (ACT058362)
  • ACT058362,urotensin,Palosuran,Inhibitor,ischemia,diabetic,UT receptor,reperfusion,Urotensin Receptor,ACT 058362,renal,inhibit,pancreatic
  • Urea,N-[2-[4-hydroxy-4-(phenylMethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
  • Palosuran, 10 mM in DMSO
  • 540769-28-6
  • Inhibitors