Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Lesogaberan is an effective and selective GABAB receptor agonist (EC50: 8.6 nM for human recombinant GABAB receptors). For rat brain GABAB and GABAA receptors, the binding affinity (Kis) is 5.1 nM and 1.4 μM, respectively. |
Targets&IC50 | GABAA (rat):1.4±0.3 μM(ki), GABAB (rat):(ki)5.1±1.2 nM, GABAB receptor (human):(EC50)8.6±0.77 nM |
In vitro | Lesogaberan (3-30 nM) increases a human islet cell proliferation in vitro[2]. |
In vivo | Lesogaberan effectively stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve[1]. Lesogaberan (7 μmol/kg) displays high oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance in female SpragueDawley rats[1]. Lesogaberan (0.08?mg/mL; 48 hours; p.o.) treatment, protects human islet β-cells from apoptosis in islet grafts in mice[2]. |
Synonyms | AZD-3355 |
Molecular Weight | 141.08 |
Formula | C3H9FNO2P |
CAS No. | 344413-67-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Lesogaberan 344413-67-8 Membrane transporter/Ion channel Neuroscience GABA Receptor AZD 3355 AZD3355 AZD-3355 inhibitor inhibit