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SB-200646

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Catalog No. T8357Cas No. 143797-63-1

SB-200646 is a selective and potent antagonist of 5-HT2B/5-HT2C receptor

SB-200646

SB-200646

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Purity: 99.61%
Catalog No. T8357Cas No. 143797-63-1
SB-200646 is a selective and potent antagonist of 5-HT2B/5-HT2C receptor
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$59In StockIn Stock
5 mg$131In StockIn Stock
10 mg$197In StockIn Stock
25 mg$332In StockIn Stock
50 mg$478In StockIn Stock
100 mg$653In StockIn Stock
1 mL x 10 mM (in DMSO)$137In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.61%
Appearance:Solid
Color:White
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Product Introduction

SB-200646 AI Summary
SB-200646 shows high binding affinity for the 5-HT2B receptor (Ki value of 21.0 nM) in rat stomach fundus, and moderate affinity for the 5-HT2C receptor, with very low affinity for the 5-HT2A receptor, suggesting a selectivity toward the 5-HT2B receptor. It exhibits multiple bioactivities, including inhibitory effects on various targets such as menin-MLL interactions in MLL-related leukemias, RECQ1 DNA helicase, human JMJD2E, tyrosyl-DNA phosphodiesterase, Tau fibril formation, Cruzain, Cytochrome P450 enzymes, and ROR gamma transcriptional activity. It also modulates lipid storage, blocks interactions between CBF-beta and RUNX1 in acute myeloid leukemia, and prevents cellular entry by Lassa and Marburg viruses. Additionally, SB-200646 shows antiviral activity by inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells, with inhibition rates of -4.21% and 0.09% at 10 μM concentration after 48 hours respectively, and by inhibiting SARS-CoV-2 3CL-Pro protease activity by 18.71% at 20 μM. It also exhibits significant enzymatic inhibitory activity against human HDAC6, with inhibition percentages ranging from 39.59% to 88.14%, indicating its potential as an HDAC6 inhibitor. These bioactivities suggest that SB-200646 has diverse pharmacological effects related to serotonin receptor modulation, antiviral activity, and inhibition of key enzymatic pathways, offering potential therapeutic applications in various diseases and conditions..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
SB-200646 is a selective and potent antagonist of 5-HT2B/5-HT2C receptor
Targets&IC50
5-HT2B receptor:7.5 (pKi) , 5-HT2C receptor:6.9 (pKi) , 5-HT2A receptor:5.2 (pKi)
Chemical Properties
Molecular Weight266.3
FormulaC15H14N4O
Cas No.143797-63-1
SmilesCN1C=2C(=CC(NC(NC=3C=CC=NC3)=O)=CC2)C=C1
Relative Density.1.26g/cm3
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
DMSO: 53 mg/mL (199.02 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.7552 mL18.7758 mL37.5516 mL187.7582 mL
5 mM0.7510 mL3.7552 mL7.5103 mL37.5516 mL
10 mM0.3755 mL1.8776 mL3.7552 mL18.7758 mL
20 mM0.1878 mL0.9388 mL1.8776 mL9.3879 mL
50 mM0.0751 mL0.3755 mL0.7510 mL3.7552 mL
100 mM0.0376 mL0.1878 mL0.3755 mL1.8776 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

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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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