Shopping Cart

Your shopping cart is currently empty

SB-657510

Name: SB-657510
Brand: TargetMol
SKU: T12848
Price: 45 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T12848Cas No. 474960-44-6

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

SB-657510

Copy Product Info

🥰Excellent

Purity: 98.06%

Catalog No. T12848Cas No. 474960-44-6

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$45	In Stock	In Stock
5 mg	$123	In Stock	In Stock
10 mg	$197	In Stock	In Stock
25 mg	$328	In Stock	In Stock
50 mg	$443	In Stock	In Stock
100 mg	$592	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$137	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:98.06%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Bioactivity

Description	SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.
Targets&IC50	UTII receptor (rat):65 nM, UTII receptor (cat):30 nM, UTII receptor (mouse):56 nM, UTII receptor (human):61 nM, UTII receptor (monkey):17 nM
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.[1] SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10 nM hU-II(IC50 of 180 nM).[2]
In vivo	The progression of high-fat diet-induced atherosclerosis and diabetes-associated atherosclerosis inhibited by SB-657510.[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]

Chemical Properties

Molecular Weight	505.81
Formula	C₁₉H₂₂BrClN₂O₅S
Cas No.	474960-44-6
Smiles	COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(Cl)c(O[C@@H]2CCN(C)C2)c1
Relative Density.	1.512 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 27 mg/mL (53.38 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9770 mL	9.8851 mL	19.7703 mL	98.8513 mL
5 mM	0.3954 mL	1.9770 mL	3.9541 mL	19.7703 mL
10 mM	0.1977 mL	0.9885 mL	1.9770 mL	9.8851 mL
20 mM	0.0989 mL	0.4943 mL	0.9885 mL	4.9426 mL
50 mM	0.0395 mL	0.1977 mL	0.3954 mL	1.9770 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc