SB 657510

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Cat.No. 3571 - SB 657510 | C19H22BrClN2O5S | CAS No. 474960-44-6
Description: Selective urotensin-II (UT) receptor antagonist
Chemical Name: 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxybenzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile action of U-II in isolated mammalian arteries and aortae (EC50 = 50 - 189 nM).

Licensing Information

Sold with the permission of GlaxoSmithKline

Compound Libraries

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Technical Data

M. Wt 505.81
Formula C19H22BrClN2O5S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 474960-44-6
PubChem ID 11272107
InChI Key KQCZCINJGIRLCD-CYBMUJFWSA-N
Smiles BrC1=CC(OC)=C(OC)C=C1S(NC2=CC=C(Cl)C(O[C@H]3CN(C)CC3)=C2)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.58 100

Preparing Stock Solutions

The following data is based on the product molecular weight 505.81. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.98 mL 9.89 mL 19.77 mL
5 mM 0.4 mL 1.98 mL 3.95 mL
10 mM 0.2 mL 0.99 mL 1.98 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Douglas et al (2005) Nonpeptide urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375. Br.J.Pharmacol. 145 620 PMID: 15852036

Behm et al (2008) Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br.J.Pharmacol. 155 374 PMID: 18587423


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Keywords: SB657510 UT-II urotensin-II receptors antagonists GlaxoSmithKline Urotensin-II Receptors

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Literature in this Area

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