| Field | Specification |
|---|---|
| Mfr No | |
| Accession Number | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | 200 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 6-(naphthalen-1-ylmethylsulfanyl)-7H-purine.
- Also known as: PU 02
- CAS number: 313984-77-9
- Molecular formula: C16H12N4S.
- Purity: >98%
- Concentration: 0.1-10 µM.
- Form: Lyophilized powder.
- Solubility: 200 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: 5-HT3 receptors
- Source: Synthetic
- Activity: PU02 is a negative allosteric modulator of 5-HT31.
- Alternative names: PU 02
Scientific background
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine neurotransmitter synthesized from the amino acid Tryptophan by the enzyme tryptophan-decarboxylase. The 5-HT3 channel is a ligand gated ion channel receptor of the cys-loop channel family. It is a pentamer with five subunits surrounding a central channel1.PU02 is a synthetic, potent and selective negative allosteric modulator of the 5-HT3 receptor. PU02 has an effective concentration of 0.1-10 μM and an IC50 of approximately 1μM. PU02 acts through a transmembrane site situated between two subunits. The Ser248, Leu288, Ile290, Thr294, and Gly306 residues are identified as important molecular determinants of PU02 activity. It is suggested that the naphthalene group of PU02 docks into the hydrophobic cavity formed by these molecular determinants. Specific mutations of Ser248, Thr294, and Gly306 convert PU02 into a complex modulator, promoting and inhibiting 5-HT-evoked signaling through these mutated sites at low and high concentrations, respectively. The PU02 binding site in the 5-HT3 receptor corresponds to allosteric sites in other anionic Cys-loop receptors. The dramatic changes in the functional properties of PU02 induced by subtle changes in its binding site exhibit that delicate structural can alternate between allosteric inhibition and potentiation of 5-HT and other Cys-loop receptors2.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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