| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: N-(1-azabicyclo[2.2.2]octan-3-yl)-6-chloro-4-methyl-3-oxo-1,4-benzoxazine-8-carboxamide;hydrochloride.
- Also known as: Y-25130 hydrochloride
- CAS number: 123040-16-4
- Molecular formula: C17H21Cl2N3O3.
- Purity: >98%
- Concentration: 0.1-100 nM.
- Form: Lyophilized powder.
- Solubility: 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: 100 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
- 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: Azasetron hydrochloride is a potent 5-HT3 channel blocker with a Ki ~2.9 nM1.
- Alternative names: Y-25130 hydrochloride
Scientific background
Azasetron hydrochloride (Y-25130 hydrochloride) is a potent 5-HT3 receptor antagonist. It selectively and competitively binds 5-HT3 receptors thereby blocking the serotonin binding site. Azasetron is classified as a derivative of benzamide. It has a different chemical structure from other 5-HT3 receptor blockers. The significant difference is found in the pharmacokinetic profiles resulting in a longer duration of action and a higher affinity for the 5-HT3 receptor1,2. Azasetron has an IC50 value ~4.9x10-10 M4 and half life of 5.4 hours3.The 5-HT3 receptor subtype is a member of the Cys-loop ligand-gated cation channels which are expressed throughout the central and peripheral nervous systems and mediate a variety of physiological functions5.Azasetron is mostly administered orally and by I.V (60-70%) and excreted in the urine in an unmetabolized form. Orally-administered azasetron is shown to be absorbed and secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability (approximately 90%)2.5-HT3 receptor antagonists have been established in a number of clinical trials as effective agents in the management and prevention of nausea and vomiting caused by cancer chemotherapy as well as postoperative nausea and emesis after anesthesia and surgery1,3.
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
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
