Atipamezole-MPV-1248-DataSheet-生命科學試劑-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作靶點: Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗

2、DMSO : 30 mg/mL (141.32 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)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。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲?/p>

3、液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.78 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (11.78 mM); Clear solution1/2 Master

4、 of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.78 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Atipamezole是合成的2-腎上腺素受體拮抗劑，Ki值為1.6 nM。IC50 & Target Ki: 1.6 nM 1體外研究 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.體內研究 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.戶使本產(chǎn)品發(fā)表的科研獻 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