Product Details
| Product Name:
SKF83959 |
CAS No.:
80751-85-5 |
| Purity:
99.96% |
Supply Ability:
10g |
| Release date:
2025/12/05 |
Product Introduction
Bioactivity
| Name | SKF83959 |
| Description | SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease. |
| In vitro | SKF83959 (0.1-30 micromol/L) improved H2O2-reduced cell viability in a dose-dependent manner. Moreover, SKF83959 treatment significantly inhibited H2O2-activated glycogen synthase kinase-3beta (GSK-3beta) which was associated with the drug's neuroprotective effect. Moreover, the application of either SKF83959 or a pharmacological inhibitor of GSK-3beta attenuated the inhibition by H2O2 on the expression of inducible NO synthase and the production of NO. In addition, SKF83959 also effectively decreased the level of lipid peroxidation and increased the activity of GSH-peroxidase altered by H2O2. These results suggest that SKF83959 exerts its neuroprotective effect through both receptor-dependent and independent mechanisms: Inhibition of GSK-3beta and consequently increasing the expression of inducible NO synthase via putative PI-linked DAR; and its anti-oxidative activity which is independent of DAR.[5] |
| In vivo | SKF83959 (0.5, 1 mg/kg; i.p.; 1 h; Male ICR male mice) alleviates scopolamine-induced cognitive impairments in the passive avoidance task and Y-Maze test.[1]
SKF83959 (1 mg/kg; i.p.; 30 minutes; Male ICR male mice) memory-enhancing effects are hindered by the blockade of the brain-derived neurotrophic factor system.[1]
SKF83959 exhibits anti-amnesic activities and reinstates the scopolamine-induced decrease in the BDNF signaling pathway in the hippocampus of mice.[1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 90 mg/mL (283.19 mM), Sonication is recommended.
|
| Keywords | DopamineReceptor | Dopamine Receptor | D1 receptor |
| Inhibitors Related | Trifluoperazine dihydrochloride | Olanzapine | Clozapine N-Oxide | Mirtazapine | Butyrophenone | Octopamine hydrochloride | Citicoline | Oxeladin citrate | Amitriptyline hydrochloride | Oxolinic acid | Mianserin hydrochloride | Fluphenazine dihydrochloride |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Anti-Alzheimer's Disease Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States