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Lesogaberan hydrochloride

Chemical Structure : Lesogaberan hydrochloride

CAS No.: 2925644-17-1

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Lesogaberan hydrochloride (AZD3355 hydrochloride)

Catalog No.: PC-22282Not For Human Use, Lab Use Only.

Lesogaberan (AZD3355) hydrochloride is a potent, selective, peripherally acting GABAB receptor agonist with Ki of 5 nM and EC50 of 8.6 nM, 274-fold selectivity over GABAA (Ki=1.4 uM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Lesogaberan (AZD3355) hydrochloride is a potent, selective, peripherally acting GABAB receptor agonist with Ki of 5 nM and EC50 of 8.6 nM, 274-fold selectivity over GABAA (Ki=1.4 uM).
Lesogaberan (AZD3355) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) through a peripheral mode of action in vivo, shows potential for treatment of GERD.

Physicochemical Properties

M.Wt 177.54
Formula C3H10ClFNO2P
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

P-[(2R)-3-amino-2-fluoropropyl]Phosphinic acid hydrochloride

References

1. Boeckxstaens GE, et al. Gut. 2011 Sep;60(9):1182-8.

2. Alstermark C, et al. J Med Chem. 2008 Jul 24;51(14):4315-20.

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