2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Medetomidine

Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels.

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Medetomidine Chemical Structure

Medetomidine Chemical Structure

CAS No. : 86347-14-0

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Other Forms of Medetomidine:

Medetomidine Related Antibodies

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Description

Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels[1][2][3][4].

IC50 & Target[1]

α2-adrenergic receptor

1.08 nM (Ki)

α1-adrenergic receptor

1750 nM (Ki)

In Vitro

Medetomidine (0-1 µM, 1 h) inhibits aldosterone release from the adrenocortical cell suspension[7].
Medetomidine (10 nM) activates a kicking response in Cyprids[8].
Medetomidine (1 µM) increases cellular cAMP production by activating β-like receptors in CHO cells[8].

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

Medetomidine Related Antibodies
In Vivo

Medetomidine (200 μg/kg, p.o. or i.m.) induces a sedation in cats[4].
Medetomidine (20 µg/kg, i.v.) shows sedative and analgesic effects in dogs[5].
Medetomidine (0.05-0.3 mg/kg, s.c.) protects against Diazinon-induced toxicosis in mice[6].

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

Animal Model: Diazinon (75 mg/kg, orally)-induced toxicosis in mice[6]
Dosage: 0.05, 0.1 and 0.3 mg/kg
Administration: Subcutaneous injection (s.c.), 15 min before Diazinon.
Result: Protected the mice from the toxicity induced by Diazinon.
Decreased the occurrence of Straub tail, excessive salivation and tremor.
Increased the latencies to onset of tremor and death when compared with control.
Animal Model: Dogs[5]
Dosage: 20 µg/kg
Administration: Intravenous injection (i.v.)
Result: Showed sedative and analgesic effects. Increased in SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, core body temperature.
Decreased in HR, CO, CI, SV, SI, RR, pH.
Molecular Weight

200.28

Formula

C13H16N2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C1=CN=CN1)C2=CC=CC(C)=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1248.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.9930 mL 24.9650 mL 49.9301 mL
5 mM 0.9986 mL 4.9930 mL 9.9860 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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 (12.48 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (12.48 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.99%

COA (254 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.9930 mL 24.9650 mL 49.9301 mL 124.8252 mL
5 mM 0.9986 mL 4.9930 mL 9.9860 mL 24.9650 mL
10 mM 0.4993 mL 2.4965 mL 4.9930 mL 12.4825 mL
15 mM 0.3329 mL 1.6643 mL 3.3287 mL 8.3217 mL
20 mM 0.2497 mL 1.2483 mL 2.4965 mL 6.2413 mL
25 mM 0.1997 mL 0.9986 mL 1.9972 mL 4.9930 mL
30 mM 0.1664 mL 0.8322 mL 1.6643 mL 4.1608 mL
40 mM 0.1248 mL 0.6241 mL 1.2483 mL 3.1206 mL
50 mM 0.0999 mL 0.4993 mL 0.9986 mL 2.4965 mL
60 mM 0.0832 mL 0.4161 mL 0.8322 mL 2.0804 mL
80 mM 0.0624 mL 0.3121 mL 0.6241 mL 1.5603 mL
100 mM 0.0499 mL 0.2497 mL 0.4993 mL 1.2483 mL
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Medetomidine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Medetomidine86347-14-0Adrenergic ReceptorBeta ReceptorSedativeanalgesicvasoconstrictionaldosteronecAMPCHOtoxicosisInhibitorinhibitorinhibit

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