1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVatinoxan hydrochlorideCat. No.: HY-19057ACAS No.: 130466-38-5Synonyms: MK-467 hydrochloride; L-659066 hydrochloride分式: CHClNOS分量: 454.97作靶點: Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: 4C, stored under nitrog

2、en* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數據體外實驗 H2O : 133 mg/mL (292.33 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.1979 mL 10.9897 mL 21.9795 mL5 mM 0.4396 mL 2.1979 mL 4.3959 mL10 mM 0.2198 mL 1.0990 mL 2.1979 mL請根據

3、產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Vatinoxan hydrochloride (MK-467hydrochloride;L-659066 hydrochloride)種外周 2 腎上腺素能受體 (2 adrenergic receptor) 拮抗劑。IC50 & Target 2 adrenergic receptor 1體內研究Vatinoxan alone increases cardiac index and tissue oxygen delivery and has no deleter

4、ious adverse effects.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEVatinoxan attenuates or prevents dexmedetomidines systemic hemodynamic effects in a dose-dependentmanner when given simultaneously i.v. but has no effect on the pulmonary outcome in conscious dogs. A50:1 dose ratio (Vatinoxan:dexm

5、edetomidine) induces the least alterations in cardiovascular function 1.Vatinoxan dose-dependently attenuates the bradycardia associated with dexmedetomidine, and shortens thesedative effect without altering its quality. Vatinoxan may be useful in attenuating reductions in heart rate inconscious cat

6、sadministered dexmedetomidine 2.PROTOCOLAnimal Dogs 1Administration 12 Eight dogs receive either dexmedetomidine (10 g/kg), Vatinoxan (250 g/kg or dexmedetomidine (10 g/kg)with increasing doses of Vatinoxan (250 g/kg, 500 g/kg and 750 g/kg). Treatments are givenintravenously (i.v.) in a randomized,

7、crossover design with a 14-day ishout period. Systemic hemodynamicsand arterial blood gas analyses are recorded at baseline and at intervals up to 90 min after drugsadministration 1.Cats 2Cats are administered seven IV treatments are administered at least 2 weeks apart, consisting ofdexmedetomidine

8、12.5 g/kg (D12.5) and 25 g/kg (D25), Vatinoxan 300 g/kg (M300), and D25 combinedwith 75, 150, 300 and 600 g/kg of Vatinoxan (D25M 75, D25M150, D25M300 and D25M600, respectively).Heart rates (HR) are recorded via telemetry and sedation assessed with a simple descriptive score and avisual analogue sca

9、le prior to treatments and at intervals until 8 hours thereafter 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Honkavaara JM, et al. The effects of increasing doses of MK-467, a peripheral alpha(2)-adrenergic receptor antagonist, on the

10、cardiopulmonary effects of intravenous dexmedetomidine in conscious dogs. J Vet Pharmacol Ther. 2011 Aug;34(4):332-7.2. Honkavaara J, et al. The effect of MK-467, a peripheral 2-adrenoceptor antagonist, on dexmedetomidine-inducedsedation andbradycardia after intravenous administration in conscious cats. Vet Anaesth Analg. 2017 Feb 22. pii: S1467-2987(16)31387-3.McePdfHeightCaution: Product has not been fully v