Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT

Product Name : Ansofaxine hydrochloride Catalog Number : T5380 CAS Number : 916918-84-8 Molecular Formula : C24H32ClNO3 Molecular Weight : 417.97

Description: Ansofaxine (LY03005; LPM570065) is a serotonin-norepinephrine-dopamine reuptake inhibitor (IC50s: 723, 763 and 491 nM, respectively).

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

DMSO 30 mg/mL, 71.77 mM Solubility ( < 1 mg/ml refers to the product slightly soluble or insoluble )

serotonin 723 nM Receptor (IC50) dopamine 491 nM norepinephrine 763 nM

In vivo Activity Acute administration was performed by providing rodents with oral solutions (0.06 mmol/kg p.o.), oral suspensions (0.06 mmol/kg p.o.) and intravenous solutions (0.04 mmol/kg i.v.) of LPM570065 and desvenlafaxine. Oral suspensions (0.06 mmol/kg/day) of the two drugs were also administered for a 14-day chronic period. LPM570065 rapidly penetrated the rat striatum, converted into desvenlafaxine and exhibited larger total exposure compared with the administration of desvenlafaxine. Acute and chronic administration of oral suspension of LPM570065 increased the 5-HT, DA and NE levels more than the relative administration of desvenlafaxine [1]. The maximum tolerated dose (MTD) was 500 mg/kg and the lethal dose was 1000 mg/kg in SD rats after a single administration of LPM570065. In 13-week repeated-dose oral toxicity, the no-observed-adverse- effect level (NOAEL) of LPM570065 was greater than 300 mg/kg for rats [2]. Animal Experiment Animal Model:

Reference 1. Zhang R, et al. The effects of LPM570065, a novel triple reuptake inhibitor, on extracellular serotonin, dopamineand norepinephrine levels in rats. PLoS One. 2014 Mar 10;9(3):e91775. 2. Li C, et al. Acute, subchronic oral toxicity, and genotoxicity evaluations of LPM570065, a new potent triple reuptake inhibitor. Regul Toxicol Pharmacol. 2018 Oct;98:129-139.

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