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Art. -Nr.: HY-10656

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SB-657510

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Based on 1 Customer Validation

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The K_i 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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Reinheit: 99.84%
CAS. Nr.: 474960-44-6
Formel: C₁₉H₂₂BrClN₂O₅S
Molecular Weight:505.81

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SB-657510 Chemical Structure

CAS. Nr.: 474960-44-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	43 nM Compound: 4	Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay	[PMID: 23453841]

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.

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.

Chemical Information

CAS. Nr. 474960-44-6
Appearance Solid
Molecular Weight 505.81
Formel C₁₉H₂₂BrClN₂O₅S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9770 mL

9.8851 mL

19.7703 mL

5 mM

0.3954 mL

1.9770 mL

3.9541 mL

10 mM

0.1977 mL

0.9885 mL

1.9770 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Park SL, et al. Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Inducedby Urotensin II in Human Vascular Endothelial Cells. Biomol Ther (Seoul). 2013 Jul 30;21(4):277-83. [Content Brief]

[2]. Behm DJ, et al. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008 Oct;155(3):374-86. [Content Brief]

[3]. Watson AM, et al. Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia. 2013 May;56(5):1155-65. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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SB-657510

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-diabetic Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-657510

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-diabetic Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SB-657510 Related Classifications

HY-10656 Related Classifications