Medetomidine HCl (MPV-785)

Alias: MPV-785; Medetomidine HCl; Medetomidine hydrochloride; MPV 785; MPV785; Precedex; Domitor. Selektope
Cat No.:V1141 Purity: ≥98%
Medetomidine HCl (MPV-785; MPV 785; MPV785; Precedex. Domitor; Selektope) is a selective and synthetic α2-adrenoceptor agonist with analgesic and anesthetic effects.
Medetomidine HCl (MPV-785) Chemical Structure CAS No.: 86347-15-1
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Medetomidine HCl (MPV-785):

  • Dexmedetomidine
  • Medetomidine (MPV-785)
  • Dexmedetomidine HCl [(S)-Medetomidine]
  • Medetomidine-d3 hydrochloride (MPV785-d3)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Medetomidine HCl (MPV-785; MPV 785; MPV785; Precedex. Domitor; Selektope) is a selective and synthetic α2-adrenoceptor agonist with analgesic and anesthetic effects. It demonstrates 1620-fold selectivity over α1-adrenoceptor and activates α2-adrenoceptor with a Ki of 1.08 nM. The use of medetomidine as an analgesic and surgical anesthetic has been approved. It is an intravenous drug solution containing sterile water that can be used as an alpha-2 adrenergic agonist. A racemic mixture of two stereoisomers, medetomidine is now sold under the brand name Dexdomitor; the more beneficial isomer is dexmedetomidine.

Biological Activity I Assay Protocols (From Reference)
Targets
α2-adrenergic receptor ( Ki = 1.08 nM ); α1-adrenergic receptor ( Ki = 1750 nM )
ln Vitro

In vitro activity: Medetomidine hydrochloride (0–1 µM, 1 h) inhibits the release of aldosterone from the suspension of adrenocortical cells[7].
Medetomidine (10 nM) hydrochloride causes Cyprids to kick in response[8].
Medetomidine hydrochloride (1 µM) stimulates β-like receptors in CHO cells, which in turn increases cellular cAMP production[8].

ln Vivo
Medetomidine (200 μg/kg, p.o. or i.m.) hydrochloride causes sedation in cats[4].
Medetomidine (20 µg/kg, i.v.) hydrochloride demonstrates analgesic and sedative effects in dogs[5].
Medetomidine (0.05-0.3 mg/kg, s.c.) hydrochloride guards against the toxicosis that diazinon causes in mice[6].
Animal Protocol
Diazinon (75 mg/kg, orally)-induced toxicosis in mice
0.05, 0.1 and 0.3 mg/kg
Subcutaneous injection (s.c.), 15 min before Diazinon.
References

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5.

[3]. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist.

[4]. Comparing oral and intramuscular administration of medetomidine in cats.

[5]. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7.

[6]. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8.

[7]. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6.

[8]. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H17CLN2
Molecular Weight
236.74
Exact Mass
236.11
Elemental Analysis
C, 65.95; H, 7.24; Cl, 14.97; N, 11.83
CAS #
86347-15-1
Related CAS #
Dexmedetomidine; 113775-47-6; Medetomidine; 86347-14-0; Dexmedetomidine hydrochloride; 145108-58-3; Medetomidine-d3 hydrochloride; 1246820-20-1
Appearance
Solid powder
SMILES
CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C.Cl
InChi Key
VPNGEIHDPSLNMU-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H16N2.ClH/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13;/h4-8,11H,1-3H3,(H,14,15);1H
Chemical Name
5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole;hydrochloride
Synonyms
MPV-785; Medetomidine HCl; Medetomidine hydrochloride; MPV 785; MPV785; Precedex; Domitor. Selektope
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 12~100 mg/mL (50.7~422.4 mM)
Water: ~47 mg/mL (~198.5 mM)
Ethanol: 47~100 mg/mL (198.5~422.4 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 5: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 6: Saline: 30 mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.2240 mL 21.1202 mL 42.2404 mL
5 mM 0.8448 mL 4.2240 mL 8.4481 mL
10 mM 0.4224 mL 2.1120 mL 4.2240 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Medetomidine HCl

    Effect of medetomidine on electrically evoked tritium overflow from MPLM segments preincubated with [3H]-choline.Br J Pharmacol. 2002 Feb; 135(3): 697–704.
  • Medetomidine HCl

    Effect of medetomidine on electrically evoked tritium overflow from MPLM segments preincubated with [3H]-noradrenaline.Br J Pharmacol. 2002 Feb; 135(3): 697–704.
  • Medetomidine HCl

    Effect of medetomidine on gastrointestinal transit in conscious wild type and α2A-knockout mice.Br J Pharmacol. 2002 Feb;
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