SB-657510

SKU: orb1708577

Description

SB-657510 is a potent urotensin-II receptor (UT) antagonist with species-variable binding affinity, exhibiting anti-inflammatory effects by blocking UII-induced mediators in vascular endothelial cells. It has demonstrated therapeutic potential in preclinical models of diabetes-associated atherosclerosis.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 474960-44-6
• MW: 505.81
• Purity: 98.18% (May vary between batches)
• Formula: C₁₉H₂₂BrClN₂O₅S
• SMILES: COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(Cl)c(O[C@@H]2CCN(C)C2)c1
• Target: GPCR,Neurotensin Receptor
• Solubility: DMSO:27 mg/mL (53.38 mM)

Bioactivity

• Target IC50:
  UTII receptor (rat):65 nM|UTII receptor (mouse):56 nM|UTII receptor (cat):30 nM|UTII receptor (human):61 nM|UTII receptor (monkey):17 nM
• In Vivo:
  The progression of high-fat diet-induced atherosclerosis and diabetes-associated atherosclerosis inhibited by SB-657510. Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice).
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• In Vitro:
  The UII-induced increase in adhesion between U937 and EA.hy926 cells was blocked by SB-657510 dramatically. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells. SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10 nM hU-II(IC50 of 180 nM).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB 657510, SB657510, SB-657510, urotensin-II (UT), Neurotensin Receptor, NeurotensinReceptor

Compound Identifiers

PubChem CID

11272107