A urotensin II receptor antagonist
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SB-657510

Item No. 42321

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxy-benzenesulfonamide
CAS Number
474960-44-6
Molecular Formula
C19H22BrClN2O5S
Formula Weight
505.8
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
BrC1=CC(OC)=C(C=C1S(=O)(NC2=CC(O[C@@H]3CCN(C)C3)=C(Cl)C=C2)=O)OC
InChi Code
InChI=1S/C19H22BrClN2O5S/c1-23-7-6-13(11-23)28-16-8-12(4-5-15(16)21)22-29(24,25)19-10-18(27-3)17(26-2)9-14(19)20/h4-5,8-10,13,22H,6-7,11H2,1-3H3/t13-/m1/s1
InChi Key
KQCZCINJGIRLCD-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Cayman Chemical
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    Product Description

    SB-657510 is an antagonist of the urotensin II receptor (UTR; Kis = 61, 17, 30, 65, and 56 nM for the human, monkey, cat, rat, and mouse receptors, respectively).1 It reduces urotensin II-induced increases in the expression of IL1B, IL6, and VCAM1 in EA.hy926 human endothelial cells and urotensin II-induced adhesion of U937 human monocytes to EA.hy926 cells when used at a concentration of 1 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Behm, D.J., McAtee, J.J., Dodson, J.W., et al. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Brit. J. Pharmacol. 155(3), 374-386 (2008).

    2. Park, S.L., Lee, B.K., Kim, Y.-A., et al. Inhibitory effect of an urotensin II receptor antagonist on proinflammatory activation induced by urotensin II in human vascular endothelial cells. Biomol. Ther. (Seoul) 21(4), 277-283 (2013).