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Medetomidine HCl Adrenergic Receptor agonist

Cat.No.S3060

Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.
Medetomidine HCl Adrenergic Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 236.74

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Quality Control

Batch: S306001 Water]47 mg/mL]false]Ethanol]47 mg/mL]false]DMSO]12 mg/mL]false Purity: 99.92%
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99.92

Solubility

In vitro
Batch:

Water : 47 mg/mL

Ethanol : 47 mg/mL

DMSO : 12 mg/mL (50.68 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 236.74 Formula

C13H16N2.HCl

Storage (From the date of receipt)
CAS No. 86347-15-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C.Cl

Mechanism of Action

Targets/IC50/Ki
α2-adrenoceptor
1.08 nM(Ki)
In vitro
Medetomidine is a selectiveα2-adrenoceptor agonist, with Ki of 1.08 nM, exhibits 1620-fold selectivity over α1-adrenoceptor, has very weak or no binding to other neurotransmitter receptors.
In vivo
In anesthetized rats, medetomidine (1-100 μg/kg, i.v.) induces a dose-dependent, relatively short-lived reduction in blood pressure and heart rate. In the pithed rat, medetomidine shows very potent vasopressor (PD50 1.7 μg/kg) and sympatho-inhibitory (ID50 1.6 μg/kg) effects without affecting basal heart rate. Medetomidine induces dose-dependent sedation, which at high doses (>100μg/kg) includes loss of the righting reflex and hypothermia. Medetomidine induces a decreases in the turnover rate of biogenic amines in the brain, dose-dependently inhibits norepinephrine (NE) turnover, inhibits brain dopamine turnover at high doses, decreases serotonin turnover.
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