A urotensin II receptor antagonist
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Palosuran

Item No. 23460

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-methyl-4-quinolinyl)-urea
CAS Number
540769-28-6
Synonyms
  • ACT058362
Molecular Formula
C25H30N4O2
Formula Weight
418.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
216, 234, 338 nm
SMILES
OC1(CCN(CCNC(NC2=CC(C)=NC3=C2C=CC=C3)=O)CC1)CC4=CC=CC=C4
InChi Code
InChI=1S/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)
InChi Key
WYJCYXOCHXWTHG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $121

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    5 mg

    $505

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    10 mg

    $951

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product 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).1 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 (Item No. 24127), 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 (Item No. 16666).2 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; Item No. 13104).3 It also decreases albuminuria and global kidney lesion scores in STZ-induced diabetic rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clozel, M., Binkert, C., Birker-Robaczewska, 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. 311(1), 204-212 (2004).

    2. Onat, A.M., Pehlivan, Y., Turkbeyler, I.H., et al. Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension. Inflammation 36(2), 405-412 (2013).

    3. Clozel, M., Hess, P., Qiu, C., et al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J. Pharmacol. Exp. Ther. 316(3), 1115-1121 (2006).