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

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.

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SB-657510 Chemical Structure

SB-657510 Chemical Structure

CAS No. : 474960-44-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

SB-657510 Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-657510 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

505.81

Formula

C19H22BrClN2O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C=C1)=C(O[C@H]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
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (197.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9770 mL 9.8851 mL 19.7703 mL
5 mM 0.3954 mL 1.9770 mL 3.9541 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.84%

COA (256 KB) RP-HPLC (244 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9770 mL 9.8851 mL 19.7703 mL 49.4257 mL
5 mM 0.3954 mL 1.9770 mL 3.9541 mL 9.8851 mL
10 mM 0.1977 mL 0.9885 mL 1.9770 mL 4.9426 mL
15 mM 0.1318 mL 0.6590 mL 1.3180 mL 3.2950 mL
20 mM 0.0989 mL 0.4943 mL 0.9885 mL 2.4713 mL
25 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9770 mL
30 mM 0.0659 mL 0.3295 mL 0.6590 mL 1.6475 mL
40 mM 0.0494 mL 0.2471 mL 0.4943 mL 1.2356 mL
50 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9885 mL
60 mM 0.0330 mL 0.1648 mL 0.3295 mL 0.8238 mL
80 mM 0.0247 mL 0.1236 mL 0.2471 mL 0.6178 mL
100 mM 0.0198 mL 0.0989 mL 0.1977 mL 0.4943 mL
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SB-657510 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-657510474960-44-6SB657510SB 657510Urotensin ReceptorUT receptorselectiveanti-inflammatorymediatorscytokinesCa2+mobilizationInhibitorinhibitorinhibit

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