Ansofaxine-hydrochloride-LY03005-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAnsofaxine hydrochlorideCat. No.: HY-U00096CAS No.: 916918-84-8Synonyms: LY03005; LPM570065分式: CHClNO分量: 417.97作靶点: 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: Please store the product under the recommended conditio

2、ns inthe COA.溶解性数据体外实验 DMSO : 31.25 mg/mL (74.77 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3925 mL 11.9626 mL 23.9252 mL5 mM 0.4785 mL 2.3925 mL 4.7850 mL10 mM 0.2393 mL 1.1963 mL 2.3925 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

3、的储备液，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: 2.08 mg/mL (4.98 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.98 mM); Clear solution3. 请依序添

4、加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.98 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Ansofaxine hydrochloride (LY03005; LPM570065)三重 重 吸收抑制剂; 抑制清素，多巴胺和去甲肾上腺素的 IC50 值分别为723，491 和 763 nM。IC50 & Target IC50: 723 nM (serotonin), 491 nM (dopa

5、mine), 763 nM (norepinephrine) 1体内研究 Ansofaxine rapidly penetrates the rat striatum, converts into desvenlafaxine and exhibits larger total exposurecompared with the administration of desvenlafaxine. Acute and chronic administration of oral suspension ofansofaxine increases the 5-HT, dopamine and no

6、repinephrine levels more than the relative administration ofdesvenlafaxine. Unlike desvenlafaxine, acute administration of an intravenous ansofaxine solution does notinduce the undesirable 90% decrease in extracellular 5-HT levels. The acute administration of ansofaxineshows a capped increase in ext

7、racellular 5-HT levels when combined with WAY-100635. Acute and chronicadministration of ansofaxine reduces the immobility time more than the relative administration ofdesvenlafaxine 1.PROTOCOLAnimal Rats: Acute administration to examine the effects of ansofaxine and desvenlafaxine on extracellular

8、5-HT,Administration 1 DA and NE levels is performed by administering oral solutions, oral suspensions and intravenous solutions ofansofaxine and desvenlafaxine. An equal number of animals are used to examine the acute effects ofansofaxine and desvenlafaxine on extracellular 5-HT levels under the blo

9、ckade of 5-HT1A receptors bypretreatment with WAY-100635. For the 14-day chronic administration, animals are randomly divided intothree groups. Oral suspensions of ansofaxine, desvenlafaxine and vehicle are administered daily for 14 days.On the 14th day of chronic administration, the effects of anso

10、faxine and desvenlafaxine on the extracellular5-HT, DA and NE levels are examined 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhang R, et al. The effects of LPM570065, a novel triple reuptake inhibitor, on extracellular serotonin, dopamineand norepinephrinelevels in rats. PLoS One. 2014 Mar 10;9(3):e91775.McePdfHeightCaution: Product has not been fully