| Chemical Name |
Lesogaberan |
| CAS Number |
344413-67-8 |
| MDL Number |
MFCD14636504 |
| Molecular Formula |
C3H9FNO2P |
| Molecular Weight |
141.08 |
| Synonyms |
AZD-3355 |
Introduction of 344413-67-8 :
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1]. IC50 & Target: Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1] EC50: 8.6±0.77 nM (human GABAB receptor)[1] In Vitro: Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2]. In Vivo: Lesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1].
Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2].
Lesogaberan (7 μmol/kg) shows high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1].
| Purity |
NLT 98% |
| Storage |
at 20ºC 2 years |
*The above information is for reference only.
