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SB 452533

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Catalog No. T23322Cas No. 459429-39-1

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

SB 452533

SB 452533

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Purity: 99.87%
Catalog No. T23322Cas No. 459429-39-1
SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$35In StockIn Stock
5 mg$58In StockIn Stock
10 mg$98In StockIn Stock
25 mg$193In StockIn Stock
50 mg$298In StockIn Stock
100 mg$433In StockIn Stock
200 mg$616In StockIn Stock
1 mL x 10 mM (in DMSO)$71In StockIn Stock
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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.
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Purity:99.87%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).
Targets&IC50
TRPV1:7.8(pKb)
In vitro
SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2[1].
In vivo
Small dose Cap significantly reduced bleomycin-induced pulmonary fibrosis in mice and obviously reversed alveolar epithelial cells epithelial-mesenchymal transition (EMT) (the expression of E-cadherin and ZO-1 were increased(P<0.05 or P<0.01)and the expression of α-SMA and Vimentin were decreased (P<0.05 or P<0.01) after drugs treatment for 21 day, concomitantly with the increase the expressions of TRPV1 and CGRP (P<0.05 or P<0.01), and inhibiting ERK1/2 phosphorylation and eIF3a expression (P<0.05 or P<0.01). These effects of small dose Cap were abolished in the presence of TRPV1 receptor antagonist SB 452533[2].
Chemical Properties
Molecular Weight376.29
FormulaC18H22BrN3O
Cas No.459429-39-1
SmilesCCN(CCNC(=O)Nc1ccccc1Br)c1cccc(C)c1
Relative Density.1.347 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (159.45 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.32 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6575 mL13.2876 mL26.5752 mL132.8762 mL
5 mM0.5315 mL2.6575 mL5.3150 mL26.5752 mL
10 mM0.2658 mL1.3288 mL2.6575 mL13.2876 mL
20 mM0.1329 mL0.6644 mL1.3288 mL6.6438 mL
50 mM0.0532 mL0.2658 mL0.5315 mL2.6575 mL
100 mM0.0266 mL0.1329 mL0.2658 mL1.3288 mL

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

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