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Droperidol

Name: Droperidol
Brand: TargetMol
SKU: T0990
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0990Cas No. 548-73-2

Alias NSC 169874, Dehydrobenzperidol

Droperidol (Dehydrobenzperidol) is a Dopamine-2 Receptor Antagonist. The mechanism of action of droperidol is as a Dopamine D2 Antagonist.

Droperidol

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Purity: 98%

Catalog No. T0990Alias NSC 169874, DehydrobenzperidolCas No. 548-73-2

Droperidol (Dehydrobenzperidol) is a Dopamine-2 Receptor Antagonist. The mechanism of action of droperidol is as a Dopamine D2 Antagonist.

Pack Size	Price	USA Warehouse	Global Warehouse
100 mg	$39	In Stock	In Stock
200 mg	$55	In Stock	In Stock
500 mg	$91	Inquiry	Inquiry
1 mL x 10 mM (in DMSO)	$43	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:98%

Color:Yellow

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Product Introduction

Droperidol AI Summary

Droperidol exhibits a diverse range of bioactivities. It shows potent inhibition of human ERG (Kv11.1) potassium channels with an IC50 value of 32.36 nM in various cell types, including HEK293 and CHO cells. Additionally, it demonstrates binding affinity for human serum albumin (log binding constant of 0.43) and inhibits batrachotoxinin binding to voltage-dependent sodium channels in guinea pig cerebral cortex with an IC50 value of 740.0 nM. It also blocks the Cav1.2 channel with an IC50 value of 7600.0 nM and shows potent inhibition of sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells. Moreover, Droperidol displays antiviral activity against SARS-CoV-2 with a range of inhibition activities in cell viability assays and a 17.82% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM. It also shows antifungal and antibacterial activities against various pathogens, including a modest effect on Candida albicans and more significant inhibition of Acinetobacter baumannii and Staphylococcus aureus MRSA. In addition, the compound has some inhibitory activity against Mycobacterium tuberculosis H37Ra with a MIC value of 31300.0 nM and demonstrates potential activity against human HDAC6 and BSEP enzymes. Despite its multifaceted bioactivities, Droperidol exhibits no significant hepatic toxicity based on Drug Induced Liver Injury Prediction System assays..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Droperidol (Dehydrobenzperidol) is a Dopamine-2 Receptor Antagonist. The mechanism of action of droperidol is as a Dopamine D2 Antagonist.
In vitro	Droperidol has a dual effect on repolarization, prolonging the development of EADs and the subsequent triggering of activity in rabbit Purkinje fibers at low concentrations. In rabbit Purkinje fibers stimulated with 60 pulses/min, 0.01 mM-0.3 mM Droperidol increased action potential duration (APD) in a dose-dependent manner without altering other parameters.1 mM-3 mM Droperidol resulted in a reversal of the prolongation effect in rabbit Purkinje fibers.10 mM- 30 mM Droperidol produced a shortening of the APD at 50% repolarization, accompanied by significant reductions in Vmax, action potential amplitude, and resting membrane potential in rabbit Purkinje fibers. A single dose of 3 mg/kg Droperidol not only dose-dependently reduced activity and rearing frequency in the open-field experiment, but also reduced the Apomorphine effect in rats.Droperidol (3 mg/kg, long-term administration) induced significant tolerance to all activity parameters recorded in the rat open field.
In vivo	Droperidol has been shown to block potassium efflux from the myocardium of isolated animal ventricular myocytes, resulting in a dose-dependent delay in repolarization.Droperidol also induces early depolarization of Purkinje fibers in isolated animals.Droperidol produces mild alpha-adrenergic blockade and peripheral vasodilation.
Synonyms	NSC 169874, Dehydrobenzperidol

Chemical Properties

Molecular Weight	379.43
Formula	C₂₂H₂₂FN₃O₂
Cas No.	548-73-2
Smiles	O=C1N(C=2C(N1)=CC=CC2)C=3CCN(CCCC(=O)C4=CC=C(F)C=C4)CC3
Relative Density.	1.269g/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: 247.5 mg/mL (652.29 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.27 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	2.6355 mL	13.1777 mL	26.3553 mL	131.7766 mL
5 mM	0.5271 mL	2.6355 mL	5.2711 mL	26.3553 mL
10 mM	0.2636 mL	1.3178 mL	2.6355 mL	13.1777 mL
20 mM	0.1318 mL	0.6589 mL	1.3178 mL	6.5888 mL
50 mM	0.0527 mL	0.2636 mL	0.5271 mL	2.6355 mL
100 mM	0.0264 mL	0.1318 mL	0.2636 mL	1.3178 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