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SB 258585

Name: SB 258585
Brand: TargetMol
SKU: T23318L
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T23318LCas No. 209480-63-7

SB 258585 is a selective 5-HT6 receptor antagonist.SB 258585 has a high affinity for individual receptor populations in cell lines with human recombinant 5-HT6 receptors.SB 258585 can be used to label both recombinant and natural 5-HT6 receptors, and can be used to assay cognitive enhancement and antipsychotic activity.

SB 258585

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Purity: 99.77%

Catalog No. T23318LCas No. 209480-63-7

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$40	-	In Stock
10 mg	$68	-	In Stock
25 mg	$123	-	In Stock
50 mg	$217	-	In Stock
100 mg	$310	-	In Stock
200 mg	$436	-	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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Batch Information

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Purity:99.77%

Appearance:Solid

Color:Yellow

Resource Download

COA LCMS HNMR

Product Introduction

SB 258585 AI Summary

SB 258585 exhibits a high binding affinity and strong selectivity for the human 5-hydroxytryptamine 6 (5-HT6) receptor, with a Ki value of 2.512 nM and a selectivity value greater than 160.0 compared to other serotonin and dopamine receptors. It acts as an antagonist at the human 5-HT6 receptor, inhibiting serotonin-induced cAMP accumulation in human HeLa cells with an IC50 value of 19.0 nM and a significant 97.7% inhibition at 10 μM concentration. Additionally, it demonstrates antagonist activity at mouse 5HT6 receptors, showing the most potent binding to the W6.48A mutant (Ki = 0.32 nM) and varying potency against other mutants. SB 258585 also exhibits bioactivities against various proteins and interactions, including Menin-MLL, JMJD2E, ALDH1A1, 15-human lipoxygenase, and tyrosyl-DNA phosphodiesterase 1, with potency values ranging from 7943.3 nM to 39810.7 nM. Moreover, it displays antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, as well as inhibiting the SARS-CoV-2 3CL-Pro protease. The compound shows a toxicity effect in mouse astrocytes with a CC50 value higher than 1000.0 nM. Lastly, it inhibits Butyrylcholinesterase (BuChE) in human plasma with less than 50.0% inhibition..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Chemical Properties

Molecular Weight	487.36
Formula	C₁₈H₂₂IN₃O₃S
Cas No.	209480-63-7
Smiles	O=S(NC1=CC=C(C(N2CCN(CC2)C)=C1)OC)(C3=CC=C(C=C3)I)=O
Relative Density.	no data available

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 (102.59 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0519 mL	10.2594 mL	20.5187 mL	102.5936 mL
5 mM	0.4104 mL	2.0519 mL	4.1037 mL	20.5187 mL
10 mM	0.2052 mL	1.0259 mL	2.0519 mL	10.2594 mL
20 mM	0.1026 mL	0.5130 mL	1.0259 mL	5.1297 mL
50 mM	0.0410 mL	0.2052 mL	0.4104 mL	2.0519 mL
100 mM	0.0205 mL	0.1026 mL	0.2052 mL	1.0259 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