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Palosuran

Name: Palosuran
Brand: TargetMol
SKU: T2058
Price: 33 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2058Cas No. 540769-28-6

Alias ACT-058362

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

Palosuran

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Purity: 99.65%

Catalog No. T2058Alias ACT-058362Cas No. 540769-28-6

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$33	In Stock	In Stock
5 mg	$52	In Stock	In Stock
10 mg	$84	-	In Stock
25 mg	$163	-	In Stock
50 mg	$265	-	In Stock
100 mg	$413	-	In Stock
1 mL x 10 mM (in DMSO)	$57	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:99.65%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Palosuran AI Summary

Palosuran exhibits a range of pharmacological activities. It acts as an antagonist at the urotensin 2 receptor in both rat urotensin 2 receptor-expressing CHOK1 cells and human RMS13 cells, inhibiting urotensin 2-induced intracellular calcium mobilization with IC50 values greater than 75000.0 nM and 320.0 nM, respectively. Additionally, it displaces [125I]urotensin 2 from the receptor with a Ki value of 41.0 nM. When evaluated at the recombinant human urotensin 2 receptor, Palosuran inhibits urotensin 2-stimulated Ca2+ mobilization with an IC50 of 39.0 nM and displays high affinity by displacing [125I]-U2 with an IC50 of less than 5.0 nM. The compound also undergoes significant drug metabolism in human liver microsomes, with a metabolism rate of 53.0% relative to total liver blood flow. Palosuran shows antiviral activity by inhibiting SARS-CoV-2-induced cytotoxicity in various cells, including Caco-2 and VERO-6 cells at 10 µM concentration. However, the inhibitory activity is modest, with an IC50 value greater than 20000.0 nM in VERO-6 cells and showing various percentages of inhibition. In terms of enzymatic activity, Palosuran shows weak inhibitory activity against human HDAC6 with inhibition percentages of -13.48% and -3.32% using different peptide substrates. The compound influences cell viability differently across cell types, promoting growth in HEK293T cells while reducing it in U2OS cells and human fibroblasts. Additionally, it has variable effects on the thermal stability of different protein domains, either increasing or decreasing their melting temperatures. Lastly, Palosuran exhibits dual bioactivity in GPCR beta-arrestin recruitment assays. It serves as a positive modulator and inhibitor across various receptors, including ADGRF1, S1PR1, FFAR4, GPR35, ADRA2A, FPR2, AGTR1, APLNR, C5AR1, GPR119, ADRB2, CX3CR1, and GLP1R, demonstrating complex interactions with different GPCR targets..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.
Targets&IC50	UT receptor (human):3.6±0.2 nM
Synonyms	ACT-058362

Chemical Properties

Molecular Weight	418.53
Formula	C₂₅H₃₀N₄O₂
Cas No.	540769-28-6
Smiles	Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2ccccc2n1
Relative Density.	1.235 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: 55 mg/mL (131.41 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.39 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	2.3893 mL	11.9466 mL	23.8931 mL	119.4657 mL
5 mM	0.4779 mL	2.3893 mL	4.7786 mL	23.8931 mL
10 mM	0.2389 mL	1.1947 mL	2.3893 mL	11.9466 mL
20 mM	0.1195 mL	0.5973 mL	1.1947 mL	5.9733 mL
50 mM	0.0478 mL	0.2389 mL	0.4779 mL	2.3893 mL
100 mM	0.0239 mL	0.1195 mL	0.2389 mL	1.1947 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