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Acetohexamide

Name: Acetohexamide
Brand: TargetMol
SKU: T0816
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0816Cas No. 968-81-0

Alias Gamadiabet, Dymelor, Acetohexamid

Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.

Acetohexamide

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Purity: 99.19%

Catalog No. T0816Alias Gamadiabet, Dymelor, AcetohexamidCas No. 968-81-0

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$29	In Stock	In Stock
100 mg	$48	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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

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Purity:99.19%

Appearance:Solid

Color:White

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Product Introduction

Acetohexamide AI Summary

Acetohexamide exhibits a wide array of bioactivities and interactions across various biological targets. It has shown a binding affinity to beta cyclodextrin with a log Ks value of 2.94 and displays multiple potencies: inhibiting the thyroid hormone receptor interaction (2.5 nM), activating the thyroid stimulating hormone receptor (6.3 nM), inhibiting ALDH1A1 (39810.7 nM), and Bloom's syndrome helicase (2.8 nM). It also demonstrates inhibitory activity against histone lysine methyltransferase G9a (2667.9 nM and 3162.3 nM), functions as an antagonist of farnesoid X receptor signaling (2.2 nM), and inhibits Mammalian Selenoprotein Thioredoxin Reductase 1 (1258.9 nM). Acetohexamide exhibits a plasma protein binding of 75.0%, a log P value of 2.4, and a 1-octanol-water distribution coefficient (log D) of -0.3 at pH 7.4 and 1.3 at pH 5.5. It has a moderate hydrophilic nature with a LogD7.4 value of -0.49. From a toxicity perspective, Acetohexamide displays moderate cytolytic liver toxicity, as indicated by increased ALT or AST levels, and shows potential for inducing drug-induced liver injury in the Drug Induced Liver Injury Prediction System (DILIps). The compound has antiviral activities, including activity against SARS-CoV-2. It inhibits virus-induced cytotoxicity in VERO-6 cells, with limited effectiveness indicated by an inhibition index of 0.1115 in Vero E6 cells and an IC50 greater than 20,000 nM in other assays. It shows variable inhibition percentages of SARS-CoV-2 3CL-Pro protease at 20 µM (15.64% and 9.27%) and inhibition of cytotoxicity in Caco-2 cells and HRCE cells. Additionally, it has shown 100.0% inhibition of CHIKV replication in hamster BHK-21 cells at 20 µM concentration. In terms of receptor interactions, Acetohexamide has binding affinities towards various receptors such as ADRB2, OPRM1, and HRH2, and displays agonist or antagonist activities in receptors like CHRM2 and HTR1A. It also inhibits enzymes such as PTGS2 and MAOA. Overall, Acetohexamide demonstrates diverse bioactivities and interactions, making it a candidate for multiple pharmacological applications, although its potential hepatotoxic effects require careful consideration..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.
Targets&IC50	KIR6.2:14.2 µM(Ki), SUR1:22.9 µM(Ki)
Synonyms	Gamadiabet, Dymelor, Acetohexamid

Chemical Properties

Molecular Weight	324.40
Formula	C₁₅H₂₀N₂O₄S
Cas No.	968-81-0
Smiles	CC(=O)c1ccc(cc1)S(=O)(=O)NC(=O)NC1CCCCC1
Relative Density.	1.3g/cm3

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: 30 mg/mL (92.48 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (6.17 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	3.0826 mL	15.4131 mL	30.8261 mL	154.1307 mL
5 mM	0.6165 mL	3.0826 mL	6.1652 mL	30.8261 mL
10 mM	0.3083 mL	1.5413 mL	3.0826 mL	15.4131 mL
20 mM	0.1541 mL	0.7707 mL	1.5413 mL	7.7065 mL
50 mM	0.0617 mL	0.3083 mL	0.6165 mL	3.0826 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