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作靶點(diǎn): 5-HT Receptor作通路: GPCR/G Protein; Neuronal Signaling儲(chǔ)存式: Please store the product under the recommended conditio

2、ns inthe COA.溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 31.25 mg/mL (74.77 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清

3、的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.98 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.98 mM); Clear solution3. 請(qǐng)依序添

4、加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.98 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Ansofaxine hydrochloride (LY03005; LPM570065)三重 重 吸收抑制劑; 抑制清素，多巴胺和去甲腎上腺素的 IC50 值分別為723，491 和 763 nM。IC50 & Target IC50: 723 nM (serotonin), 491 nM (dopa

5、mine), 763 nM (norepinephrine) 1體內(nèi)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