1. GPCR/G Protein
  2. Urotensin Receptor
  3. SB-657510

SB-657510 

Cat. No.: HY-10656 Purity: 99.76%
Handling Instructions

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.

For research use only. We do not sell to patients.

SB-657510 Chemical Structure

SB-657510 Chemical Structure

CAS No. : 474960-44-6

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10 mM * 1 mL in DMSO USD 512 In-stock
Estimated Time of Arrival: December 31
1 mg USD 155 In-stock
Estimated Time of Arrival: December 31
5 mg USD 460 In-stock
Estimated Time of Arrival: December 31
10 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells[1][2].

In Vitro

SB-657510 dramatically blocks the UII-induced increase in adhesion between U937 and EA.hy926 cell. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells[1].
SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10 nM hU-II with an IC50 of 180 nM[2].

Western Blot Analysis[1]

Cell Line: EA.hy926 cells (UII-induced)
Concentration: 1 μM
Incubation Time: 0.5, 1, 2, 4, 8 hours
Result: Remarkably decreased the UII-induced protein expression of tissue factor.
In Vivo

SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis[1].
Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice)[3].

Molecular Weight

505.81

Formula

C₁₉H₂₂BrClN₂O₅S

CAS No.

474960-44-6

SMILES

ClC(C=C1)=C(O[[email protected]]2CN(C)CC2)C=C1NS(C3=CC(OC)=C(OC)C=C3Br)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

SB-657510SB657510SB 657510Urotensin ReceptorUT receptorselectiveanti-inflammatorymediatorscytokinesCa2+mobilizationInhibitorinhibitorinhibit

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SB-657510
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