Atipamezole-MPV-1248-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAtipamezoleCat. No.: HY-12380ACAS No.: 104054-27-5Synonyms: MPV 1248分式: CHN分量: 212.29作靶点: Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、DMSO : 30 mg/mL (141.32 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.7105 mL 23.5527 mL 47.1054 mL5 mM 0.9421 mL 4.7105 mL 9.4211 mL10 mM 0.4711 mL 2.3553 mL 4.7105 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备

3、液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.78 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (11.78 mM); Clear solution1/2 Master

4、 of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.78 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Atipamezole是合成的2-肾上腺素受体拮抗剂，Ki值为1.6 nM。IC50 & Target Ki: 1.6 nM 1体外研究 The affinity of atipamezole for 2-adrenoceptors and its 2/1 selectivity ratio are cons

5、iderably higher thanyohimbine. Atipamezole is not selective for subtypes of 2-adrenoceptors. It has negligible affinity for 5-HT1,5-HT2 and I2 bindings sites 1.体内研究 Atipamezole is well tolerated in rodents. In anesthetized, normotensive rats, the cardiovascular effects ofatipamezole (0.011 mg/kg, i.

6、v.) are rather modest. Atipamezole is commonly used by veterinarians toawaken animals from sedation or anesthesia. Atipamezole increases sexual activity in rats and monkeys. Inanimals with sustained nociception, atipamezole increases pain-related responses by blocking thenoradrenergic feedback inhib

7、ition of pain. Atipamezole at low doses has beneficial effects on alertness,selective attention, planning, learning, and recall in experimental animals, but not necessarily on short-termworking memory 1.户使本产品发表的科研献 Protein Cell. 2019 Mar;10(3):178-195.See more customer validations on HYPERLINK / www

8、.MedChemEREFERENCES1. Pertovaara A, et al.Pharmacological properties, central nervous system effects, and potential therapeutic applicationsof atipamezole, aselective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo