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Melperone

Name: Melperone
Brand: TargetMol
SKU: T7421
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7421Cas No. 3575-80-2

Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.

Melperone

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Purity: 98.84%

Catalog No. T7421Cas No. 3575-80-2

Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.

Pack Size	Price	USA Warehouse	Global Warehouse
25 mg	$40	In Stock	In Stock
50 mg	$58	In Stock	In Stock
100 mg	$113	In Stock	In Stock
200 mg	$167	-	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]

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:98.84%

Appearance:Solid

Color:Yellow

Resource Download

COA LCMS HNMR

Product Introduction

Melperone AI Summary

Melperone exhibits a wide range of bioactivities with varying potencies across different assays. It shows significant potency in inhibiting the Menin-MLL interaction in MLL-related leukemias (44668.4 nM) and acts as a delayed death inhibitor of the malarial parasite plastid after a 96-hour incubation (95.3 nM). It demonstrates potencies in promoting Schwann cell viability (40533.4 nM), involvement in a Schwann cell luciferase assay (16136.6 nM), and blocking the entry of Ebola virus with AC50 values of 6309.6 nM and 6.31 µM in different assays. Pharmacokinetically, Melperone shows moderate clearance (46.0 mL·min⁻¹·kg⁻¹), a short half-life (3.9 hours), a moderate mean residence time (5.0 hours), and a moderate volume of distribution at steady state (14.0 L·kg⁻¹) in humans after intravenous administration. The compound exhibits moderate hepatotoxicity, characterized by cytolytic, choleostatic, and mixed liver toxicity, though severe hepatitis and chronic liver conditions have not been linked to it. In antiviral activity assays, Melperone showed mixed results against SARS-CoV-2. It inhibited cytotoxicity in Caco-2 cells by -27.17% at a 10 µM concentration over 48 hours and displayed 16.3% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM. However, its IC50 value against SARS-CoV-2 induced cytotoxicity in VERO-6 cells was greater than 20000.0 nM, indicating a relatively weak inhibitory effect. It also demonstrated no significant inhibition of various human transporters (BSEP, MRP2, MRP3, and MRP4) with IC50 values exceeding 133000.0 nM. Additionally, the compound shows minor inhibition rates for human HDAC6, with 18.11% inhibition in one enzymatic assay and -9.44% in another using different peptide substrates. It has bioactivity involving a primary screen assay using NF54 nanoGlo with a Z score of 0.66 and -6.0% inhibition at 2µM over 72 hours. Melperone also interacts with several receptors, including DRD1, DRD3, ADRA2A, HTR1A, and others, with AC50 values from 305.0 nM to 12567.5 nM, showing agonistic activity at HTR2B and ADRA1A receptors (AC50 > 30000.0 nM), and antagonist activity at the TBXA2R receptor (AC50 > 30000.0 nM). These interactions suggest potential effects on neurotransmitter systems and hormone receptors..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

Melperone, a butyrophenone tranquillizer, caused bradycardia in vivo and in vitro.

Chemical Properties

Molecular Weight	263.35
Formula	C₁₆H₂₂FNO
Cas No.	3575-80-2
Smiles	CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1
Relative Density.	1.046 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: 41.67 mg/mL (158.23 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.59 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	3.7972 mL	18.9861 mL	37.9723 mL	189.8614 mL
5 mM	0.7594 mL	3.7972 mL	7.5945 mL	37.9723 mL
10 mM	0.3797 mL	1.8986 mL	3.7972 mL	18.9861 mL
20 mM	0.1899 mL	0.9493 mL	1.8986 mL	9.4931 mL
50 mM	0.0759 mL	0.3797 mL	0.7594 mL	3.7972 mL
100 mM	0.0380 mL	0.1899 mL	0.3797 mL	1.8986 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