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Specific PXR antagonist 70

Name: Specific PXR antagonist 70
Brand: TargetMol
SKU: T41255
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T41255Cas No. 931314-31-7

Specific PXR antagonist 70 is a selective pregnane X receptor (PXR) antagonist with an IC50 of 540 nM and Ki of 390 nM for human PCR and enhances the chemosensitivity of cancer cells.

Specific PXR antagonist 70

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Purity: 98.41%

Catalog No. T41255Cas No. 931314-31-7

Specific PXR antagonist 70 is a selective pregnane X receptor (PXR) antagonist with an IC50 of 540 nM and Ki of 390 nM for human PCR and enhances the chemosensitivity of cancer cells.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$106	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$239	In Stock	In Stock
50 mg	$372	In Stock	In Stock
100 mg	$538	In Stock	In Stock
500 mg	$1,150	-	In Stock

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

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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:98.41%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Specific PXR antagonist 70 AI Summary

Specific PXR antagonist 70 demonstrates various bioactivities related to human Pregnane X Receptor (PXR) and CRBN/DDB1 complex interactions. For PXR, it shows significant displacement of BODIPY FL vindoline from GST-tagged PXR LBD, with an IC50 of 190.0 nM and 95.0% inhibition at 10 µM. It also acts as an inverse agonist in HepG2 cells with an IC50 of 24.0 nM, and inhibits PXR activity in the presence of rifampicin, with an IC50 of 250.0 nM and 100% inhibition at 10 µM. In contrast, for the CRBN/DDB1 complex, it displays relatively low potency with an EC50 greater than 3000.0 nM in displacement of BODIPY FL thalidomide. Overall, Specific PXR antagonist 70 shows strong modulation potential for PXR-regulated pathways but relatively low activity in the context of CRBN/DDB1 complex interaction..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Specific PXR antagonist 70 is a selective pregnane X receptor (PXR) antagonist with an IC50 of 540 nM and Ki of 390 nM for human PCR and enhances the chemosensitivity of cancer cells.

Chemical Properties

Molecular Weight	415.51
Formula	C₂₁H₂₅N₃O₄S
Cas No.	931314-31-7
Smiles	COC1=CC=C(OC)C(=C1)N1N=NC(=C1C)S(=O)(=O)C1=CC=C(C=C1)C(C)(C)C
Relative Density.	1.22 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

H2O: 76.92 mg/mL (185.12 mM), Sonication is recommended.

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	2.4067 mL	12.0334 mL	24.0668 mL	120.3340 mL
5 mM	0.4813 mL	2.4067 mL	4.8134 mL	24.0668 mL
10 mM	0.2407 mL	1.2033 mL	2.4067 mL	12.0334 mL
20 mM	0.1203 mL	0.6017 mL	1.2033 mL	6.0167 mL
50 mM	0.0481 mL	0.2407 mL	0.4813 mL	2.4067 mL
100 mM	0.0241 mL	0.1203 mL	0.2407 mL	1.2033 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:

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