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Wf-516

Catalog No. T13339 CAS 310392-94-0

Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant activity.

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Wf-516, CAS 310392-94-0

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,820.00
50 mg	8-10 weeks	$ 2,380.00
100 mg	8-10 weeks	$ 3,100.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	Wf-516 is a 5-HT reuptake inhibitor (Kis: 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively), and with potent antidepressant activity.
Targets&IC50	5-HT1A receptor (human):ki:5 nM , 5-HT2A receptor (human):40 nM (ki)
In vitro	Wf-516 shows high affinity for 5-HT1A receptors in the hippocampus and raphe nucleus of rats(Ki of 8.1 nM and 7.9 nM, respectively)[2].
In vivo	Wf-516 (0.5 mg/kg, i.v.) does not induce any change in the firing activity of 5-HT neurons, but significantly blocks the inhibitory effect of 8-OHDPAT (a 5-HT autoreceptor agonist) by 70%. A full dose-response relationship between the suppression of DRN firing activity and different doses of LSD shows a significant fourfold shift to the right in the Wf-516 pretreated rats (ED50?=?32.4?±?1.0 μg/kg) as compared to controls with ED50?of?7.5?±?1.2 μg/kg. After intravenous administration of successive doses of 1.25 mg/kg of Wf-516 (up to 10 mg/kg), the effect of microiontophoretically applied 5-HT is prolonged and reaches statistical significance at 7.5 mg/kg. At this dose, the RT50 value is increased by 53% and, by 75% at the highest dose of 10 mg/kg of Wf-516 used[1].Compared with baseline, oral administration of 30 mg/kg Wf-516 to these 5,7-DHT-treated rats induced a significant decrease in hippocampal BPND, but no further decrease in BPND was observed in the grooved nuclei. The oral ED50 values of Wf-516 in the hippocampus and grooved nuclei were 5.3 mg/kg and 4.2 mg/kg, respectively [2].

Molecular Weight	502.39
Formula	C25H25Cl2N3O4
CAS No.	310392-94-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. El Mansari M, et al. In vivo electrophysiological assessment of the putative antidepressant Wf-516 in the rat raphe dorsalis, locus coeruleus and hippocampus. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jan;376(5):351-61. Epub 2007 Nov 30. 2. Saijo T, et al. Presynaptic selectivity of a ligand for serotonin 1A receptors revealed by in vivo PET assays of rat brain. PLoS One. 2012;7(8):e42589.

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Keywords

Wf-516 310392-94-0 GPCR/G Protein Neuroscience 5-HT Receptor Wf516 Wf 516 inhibitor inhibit

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