Desvenlafaxine succinate hydrate

SKU: orb1300997

Description

Desvenlafaxine succinate hydrate (WY 45233 Succinate) is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in antidepressant research. This compound is applied in both in vitro binding assays and in vivo behavioral studies to investigate mechanisms of depression and anxiety.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 386750-22-7
• MW: 399.48
• Purity: 99.26%
• Formula: C₂₀H₃₃NO₇
• SMILES: OC(=O)CCC(O)=O.CN(C)CC(c1ccc(O)cc1)C1(O)CCCCC1
• Target: Serotonin Transporter,Norepinephrine,5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.01 mM);DMSO:50 mg/mL (125.16 mM)

Bioactivity

• Target IC50:
  Norepinephrine:558.4 nM(Ki)|5-HT:40.2 nM(Ki)
• In Vivo:
  Desvenlafaxine Succinate rapidly penetrates the male rat brain and hypothalamus. Desvenlafaxine Succinate significantly increases extracellular NE levels compared with baseline in the male rat hypothalamus but had no effect on DA levels using microdialysis. Desvenlafaxine Succinate exhibits a linear and dose-proportional pharmacokinetic single-dose profile in a dose range from 100 to 600 mg/day. The absolute bioavailability of the oral formulation is 80.5%.
• In Vitro:
  Desvenlafaxine succinate is the succinate salt monohydrate of O-desmethylvenlafaxine, an active metabolite of venlafaxine. Desvenlafaxine Succinate is a serotonin-norepinephrine reuptake inhibitor and is the active metabolite of the antidepressant venlafaxine. Similar to venlafaxine, Desvenlafaxine Succinate inhibits the neuronal uptake of serotonin and norepinephrine. Desvenlafaxine Succinate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter. Desvenlafaxine Succinate inhibits [3H]5-HT or [3H]NE uptake for the hSERT or hNET with IC50 of 47.3 and 531.3 nM, respectively. Desvenlafaxine Succinate has the potential to inhibit CYP2D6, which could result in increased concentrations of drugs metabolized through this pathway. Induction of CYP3A4 is also possible with Desvenlafaxine Succinate, which could impact the metabolism of drugs metabolized via this enzyme.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5-HT, 5HT Receptor, O-Desmethylvenlafaxine succinate, O-Desmethylvenlafaxine succinate hydrate, Norepinephrine (NE), WY45233 Succinate, WY-45233 Succinate, SerotoninTransporter, Serotonin Transporter

Compound Identifiers

PubChem CID

9800068