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DY268

Name: DY268
Brand: TargetMol
SKU: T31587
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T31587Cas No. 1609564-75-1

Alias DY-268, DY 268

DY268 is a compound based on trisubstituted pyrazolamide without any FXR agonist activity and cytotoxicity and can be used as an effective FXR antagonist (IC50 = 7.5 nM).

DY268

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Purity: 99.75%

Catalog No. T31587Alias DY-268, DY 268Cas No. 1609564-75-1

DY268 is a compound based on trisubstituted pyrazolamide without any FXR agonist activity and cytotoxicity and can be used as an effective FXR antagonist (IC50 = 7.5 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
5 mg	$80	In Stock	In Stock
10 mg	$128	In Stock	In Stock
25 mg	$258	In Stock	In Stock
50 mg	$478	In Stock	In Stock
100 mg	$689	In Stock	In Stock
500 mg	$1,480	-	In Stock
1 mL x 10 mM (in DMSO)	$89	In Stock	In 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:99.75%

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

DY268 AI Summary

DY268 exhibits significant antagonist activity at human FXR (Farnesoid X receptor) with an IC50 value of 7.5 nM in a TR-FRET assay, showing a 130.1% inhibition relative to control. It also inhibits GW4064-induced transactivation of FXR in HEK293T cells, with an IC50 value of 468.5 nM in a beta-lactamase reporter gene assay, resulting in 98.9% inhibition. Tested in CHO-K1 FXR cells coexpressed with beta-galactosidase at 10 µM, the compound showed 96.0% activity compared to control after a 60-min preincubation followed by GW4064 addition measured over 3 to 16 hours using a PathHunter chemiluminescence assay. Regarding cytotoxicity, DY268 demonstrates minimal effects on HEK293T cells expressing FXR and beta-lactamase genes, with less than 5.0% inhibition at 40 µM after 16 hours. The growth rate of U2OS and HEK293T cells ranged from 0.76 to 0.99, while human fibroblast cells showed more variable growth rates from 0.43 to 0.89, suggesting a generally positive impact on cell viability with variability depending on cell type. Lastly, the compound has diverse bioactivities affecting the thermal stability of various protein regions, either increasing or decreasing the melting temperature (TM) in a thermal shift assay. This indicates potential influences on protein folding and stability across multiple domains..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	DY268 is a compound based on trisubstituted pyrazolamide without any FXR agonist activity and cytotoxicity and can be used as an effective FXR antagonist (IC50 = 7.5 nM).
Targets&IC50	FXR:7.5 nM
Synonyms	DY-268, DY 268

Chemical Properties

Molecular Weight	560.66
Formula	C₃₀H₃₂N₄O₅S
Cas No.	1609564-75-1
Smiles	C(NC1=CC(S(=O)(=O)N2CCOCC2)=C(C)C=C1)(=O)C=3C(=NN(CC4=CC(OC)=CC=C4)C3)C5=CC=C(C)C=C5
Relative Density.	1.30 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: 50 mg/mL (89.18 mM), Sonication is recommended.

H2O: Insoluble

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (8.92 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

	1mg	5mg	10mg	50mg
1 mM	1.7836 mL	8.9181 mL	17.8361 mL	89.1806 mL
5 mM	0.3567 mL	1.7836 mL	3.5672 mL	17.8361 mL
10 mM	0.1784 mL	0.8918 mL	1.7836 mL	8.9181 mL
20 mM	0.0892 mL	0.4459 mL	0.8918 mL	4.4590 mL
50 mM	0.0357 mL	0.1784 mL	0.3567 mL	1.7836 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