Art. -Nr.: HY-12380A

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Atipamezole

(Synonyms: MPV 1248)

9 Cited Publications

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Based on 9 publication(s) in Google Scholar

Atipamezole (MPV 1248) is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM.

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Reinheit: 99.97%
CAS. Nr.: 104054-27-5
Formel: C₁₄H₁₆N₂
Molecular Weight:212.29

Speicherung:

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

Atipamezole Chemical Structure

CAS. Nr.: 104054-27-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Atipamezole (MPV 1248) is a potent α₂-adrenoceptor antagonist with a K_i of 1.6 nM^[1].

IC₅₀ & Target

α adrenergic receptor

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

The affinity of atipamezole for α₂-adrenoceptors and its α₂/α₁ selectivity ratio are considerably higher than yohimbine. Atipamezole is not selective for subtypes of α₂-adrenoceptors. It has negligible affinity for 5-HT₁, 5-HT2 and I2 bindings sites^[1].

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

In Vivo

Atipamezole is well tolerated in rodents. In anesthetized, normotensive rats, the cardiovascular effects of atipamezole (0.01–1 mg/kg, i.v.) are rather modest. Atipamezole is commonly used by veterinarians to awaken animals from sedation or anesthesia. Atipamezole increases sexual activity in rats and monkeys. In animals with sustained nociception, atipamezole increases pain-related responses by blocking the noradrenergic feedback inhibition of pain. Atipamezole at low doses has beneficial effects on alertness, selective attention, planning, learning, and recall in experimental animals, but not necessarily on short-term working memory^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 104054-27-5
Appearance Solid
Molecular Weight 212.29
Formel C₁₄H₁₆N₂
Color White to off-white
SMILES

CCC1(C2=CN=CN2)CC3=C(C=CC=C3)C1
Synonyms

MPV 1248
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

Publications (9)

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Journal Impact Factor

Protein Cell

Identification of serotonin 2A receptor as a novel HCV entry factor by a chemical biology strategy. [Abstract]

2019 Mar;10(3):178-195. PMID: 29542010
Sci Transl Med

S-217622, a SARS-CoV-2 main protease inhibitor, decreases viral load and ameliorates COVID-19 severity in hamsters. [Abstract]

2023 Jan 18;15(679):eabq4064. PMID: 36327352
Int Immunopharmacol

Repurposing the anesthetic dexmedetomidine: a novel antidote for sulfur mustard analog-induced acute lung injury via multi-mechanism modulation. [Abstract]

2026 Feb 1:170:116069. PMID: 41421231
Front Cell Dev Biol

Protective Effects of Dexmedetomidine on the Vascular Endothelial Barrier Function by Inhibiting Mitochondrial Fission via ER/Mitochondria Contact. [Abstract]

2021 Mar 11:9:636327. PMID: 33777946
Exp Mol Pathol

Up-regulation of miRNA-151-3p enhanced the neuroprotective effect of dexmedetomidine against β-amyloid by targeting DAPK-1 and TP53. [Abstract]

2021 Feb:118:104587. PMID: 33275947
Brain Res

Blockade of adenosine A1 receptor in nucleus tractus solitarius attenuates baroreflex sensitivity response to dexmedetomidine in rats. [Abstract]

2020 Sep 15:1743:146949. PMID: 32522627
Eur J Neurosci

Dexmedetomidine protects SH-SY5Y cells against MPP+ -induced declining of mitochondrial membrane potential and cell cycle deficits. [Abstract]

2021 Apr 27. PMID: 33905578
bioRxiv

2024 November 03.
Research Square Preprint

2022 May.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (471.05 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

4.7105 mL

23.5527 mL

47.1054 mL

5 mM

0.9421 mL

4.7105 mL

9.4211 mL

10 mM

0.4711 mL

2.3553 mL

4.7105 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: ≥ 2.5 mg/mL (11.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (11.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 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]. Pertovaara A, et al.Pharmacological properties, central nervous system effects, and potential therapeutic applicationsof atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88. [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	4.7105 mL	23.5527 mL	47.1054 mL	117.7634 mL
	5 mM	0.9421 mL	4.7105 mL	9.4211 mL	23.5527 mL
	10 mM	0.4711 mL	2.3553 mL	4.7105 mL	11.7763 mL
	15 mM	0.3140 mL	1.5702 mL	3.1404 mL	7.8509 mL
	20 mM	0.2355 mL	1.1776 mL	2.3553 mL	5.8882 mL
	25 mM	0.1884 mL	0.9421 mL	1.8842 mL	4.7105 mL
	30 mM	0.1570 mL	0.7851 mL	1.5702 mL	3.9254 mL
	40 mM	0.1178 mL	0.5888 mL	1.1776 mL	2.9441 mL
	50 mM	0.0942 mL	0.4711 mL	0.9421 mL	2.3553 mL
	60 mM	0.0785 mL	0.3925 mL	0.7851 mL	1.9627 mL
	80 mM	0.0589 mL	0.2944 mL	0.5888 mL	1.4720 mL
	100 mM	0.0471 mL	0.2355 mL	0.4711 mL	1.1776 mL

Keywords

Atipamezole

9 Cited Publications

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Atipamezole

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Publications Citing Use of MedChemExpress (MCE) Atipamezole

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atipamezole

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Endocrinology Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Human Metabolite Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Atipamezole

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Atipamezole Related Classifications

HY-12380A Related Classifications