Detomidine HCl (MPV 253; MPV253)

Alias: MPV 253; MPV253; Detomidine hydrochloride; MPV-253; Detomidine HCl
Cat No.:V1108 Purity: ≥98%
Detomidine HCl (MPV 253; MPV-253), the hydrochloride salt of detomidine, is an alpha2/α2-Adrenoreceptor agonist with sedative properties.
Detomidine HCl (MPV 253; MPV253) Chemical Structure CAS No.: 90038-01-0
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
5mg
10mg
25mg
50mg
100mg
500mg
1g
Other Sizes

Other Forms of Detomidine HCl (MPV 253; MPV253):

  • Detomidine
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Detomidine HCl (MPV 253; MPV-253), the hydrochloride salt of detomidine, is an alpha2/α2-Adrenoreceptor agonist with sedative properties. It creates analgesic and sedative effects that are dose-dependent and mediated by α2 catecholamine receptor activation. Detomidine is an imidazole derivative and α2-adrenergic agonist that is mainly used in horses as a large animal sedative. Typically, it can be found as the salt detomidine hydrochloride. Veterinarians can obtain it as a prescription drug under the brand name Dormosedan.

Biological Activity I Assay Protocols (From Reference)
Targets
Adrenergic Receptor
ln Vitro
Currently detomidine is only authorized for use on equines. A negative feedback response is induced by α2-adrenergic agonists, which reduce the production of excitatory neurotransmitters and produce dose-dependent analgesic effects through the activation of α2 catecholamine receptors. In addition to its effects on the heart and lungs, detomidine also has an antidiuretic effect and inhibits the sympathetic nervous system.
References

[1]. Pharmacological evidence for the involvement of alpha-2 adrenoceptors in the sedative effect of detomidine, a novel sedative-analgesic. J Vet Pharmacol Ther. 1985 Mar;8(1):30-7.

[2]. Cardiovascular and respiratory effects of detomidine in isoflurane-anaesthetised horses. J S Afr Vet Assoc. 1996 Dec;67(4):199-203. . 2019 Jan-Mar;35(1):36-40.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C12H15CLN2
Molecular Weight
222.71
Exact Mass
222.09
Elemental Analysis
C, 64.72; H, 6.79; Cl, 15.92; N, 12.58
CAS #
90038-01-0
Related CAS #
Detomidine; 76631-46-4
Appearance
Solid powder
SMILES
CC1=C(C(=CC=C1)CC2=CN=CN2)C.Cl
InChi Key
OIWRDXKNDCJZSM-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H14N2.ClH/c1-9-4-3-5-11(10(9)2)6-12-7-13-8-14-12;/h3-5,7-8H,6H2,1-2H3,(H,13,14);1H
Chemical Name
5-[(2,3-dimethylphenyl)methyl]-1H-imidazole;hydrochloride
Synonyms
MPV 253; MPV253; Detomidine hydrochloride; MPV-253; Detomidine HCl
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: ~45 mg/mL (~202.1 mM)
Water: ~45 mg/mL (~202.1 mM)
Ethanol: 45 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.23 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 (11.23 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 (11.23 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: 140 mg/mL (628.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.4901 mL 22.4507 mL 44.9014 mL
5 mM 0.8980 mL 4.4901 mL 8.9803 mL
10 mM 0.4490 mL 2.2451 mL 4.4901 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

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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?
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  • 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:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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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
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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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
  • Detomidine HCl
    Mean (± SE) PCV (A) and TS (B) of healthy horses over time following administration of xylazine IV (clear circle with solid line), romifidine IV (shaded triangle with dotted line), detomidine IV (shaded square with long dashed line), and detomidine.Can Vet J. 2014 Apr; 55(4): 334–340.
  • Detomidine HCl
    Figure 4 Mean (± SE) splenic thickness measured in ICS 9 of healthy horses over time following administration of xylazine IV (clear circle with solid line), romifidine IV (shaded triangle with dotted line), detomidine IV.Can Vet J. 2014 Apr; 55(4): 334–340.
  • Detomidine HCl
    Mean (± SE) RBC count (A), COP (B), plasma osmolality (C), and blood glucose concentration (D) of healthy horses over time following administration of xylazine IV (clear circle with solid line), romifidine IV (shaded triangle with dotted line),Can Vet J. 2014 Apr; 55(4): 334–340.
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