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Product Description
– Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. The affinity (Kis) of Lesogaberan napadisylate for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan napadisylate inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action[1].
Web ID
– HY-10061A
Shipping
– Room temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C13H17FNO5PS
References
– [1]Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12.|[2]Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539.
CAS Number
– 477956-38-0
Molecular Weight
– 349.31
SMILES
– O=S(C1=CC=C2C=CC=CC2=C1)(O)=O.O=P(C[C@H](F)CN)O
Clinical Information
– Phase 2
Research Area
– Metabolic Disease
Solubility
– 10 mM in DMSO
Target
– GABA Receptor
Pathway
– Membrane Transporter/Ion Channel;Neuronal Signaling
Product type
– Reference compound
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