Art. -Nr.: HY-B2169

Melperone

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Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.

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Reinheit: 99.84%
CAS. Nr.: 3575-80-2
Formel: C₁₆H₂₂FNO
Molecular Weight:263.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Melperone Chemical Structure

CAS. Nr.: 3575-80-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]^[4]

Human D₂ Receptor

180 nM (Kd)

5-HT_1A Receptor

5-HT_1D Receptor

5-HT_2A Receptor

5-HT_2C Receptor

α1-adrenergic receptor

180 nM (Kd)

α2-adrenergic receptor

150 nM (Kd)

CYP2D6

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

In Vivo

Melperone (2 mg/kg/day; drinking water; changed in lightproof drinking bottles twice a week; for 21 days) increases basal, but not D-Amphetamine-induced, extracellular dopamine levels in the rat nucleus accumbens^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Sprague-Dawley albino rats (180-200 g) was administered subcutaneously with D-Amphetamine sulfate (1.0 mg/kg)^[1]
Dosage:

2 mg/kg/day
Administration:

Drinking water; changed in lightproof drinking bottles twice a week; for 21 days
Result:

Increased basal extracellular DA and enhanced D-Amphetamine-induced DA release in the striatum.

Chemical Information

CAS. Nr. 3575-80-2
Appearance Solid
Molecular Weight 263.35
Formel C₁₆H₂₂FNO
Color White to off-white
SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CCC(C)CC2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 41.67 mg/mL (158.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7972 mL

18.9861 mL

37.9723 mL

5 mM

0.7594 mL

3.7972 mL

7.5945 mL

10 mM

0.3797 mL

1.8986 mL

3.7972 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ichikawa J, et al. The effect of chronic atypical antipsychotic drugs and haloperidol on amphetamine-induced dopamine release in vivo. Brain Res. 1992 Mar 6;574(1-2):98-104. [Content Brief]

[2]. Richelson E, et al. Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds. Life Sci. 2000 Nov 24;68(1):29-39. [Content Brief]

[3]. Hefner G, et al. Melperone but not bisoprolol or metoprolol is a clinically relevant inhibitor of CYP2D6: evidence from a therapeutic drug monitoring survey. J Neural Transm (Vienna). 2015 Nov;122(11):1609-17. [Content Brief]

[4]. Bobo WV, et al. Melperone, an aytpical antipsychotic drug with clozapine-like effect on plasma prolactin: contrast with typical neuroleptics. Hum Psychopharmacol. 2009 Jul;24(5):415-22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.7972 mL	18.9861 mL	37.9723 mL	94.9307 mL
	5 mM	0.7594 mL	3.7972 mL	7.5945 mL	18.9861 mL
	10 mM	0.3797 mL	1.8986 mL	3.7972 mL	9.4931 mL
	15 mM	0.2531 mL	1.2657 mL	2.5315 mL	6.3287 mL
	20 mM	0.1899 mL	0.9493 mL	1.8986 mL	4.7465 mL
	25 mM	0.1519 mL	0.7594 mL	1.5189 mL	3.7972 mL
	30 mM	0.1266 mL	0.6329 mL	1.2657 mL	3.1644 mL
	40 mM	0.0949 mL	0.4747 mL	0.9493 mL	2.3733 mL
	50 mM	0.0759 mL	0.3797 mL	0.7594 mL	1.8986 mL
	60 mM	0.0633 mL	0.3164 mL	0.6329 mL	1.5822 mL
	80 mM	0.0475 mL	0.2373 mL	0.4747 mL	1.1866 mL
	100 mM	0.0380 mL	0.1899 mL	0.3797 mL	0.9493 mL

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Melperone

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Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Melperone Related Classifications

HY-B2169 Related Classifications