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Lesogaberan

Chemical Structure : Lesogaberan

CAS No.: 344413-67-8

Lesogaberan (AZD-3355)

Catalog No.: PC-62764Not For Human Use, Lab Use Only.

Lesogaberan (AZD-3355) 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 (AZD-3355) 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); 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.

Other Indication

Phase 2 Discontinued

Physicochemical Properties

M.Wt 141.082
Formula C3H9FNO2P
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

((R)-3-Amino-2-fluoropropyl)phosphinic acid

References

1. Lehmann A, et al. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12.

2. Brändén L, et al. Eur J Pharmacol. 2010 May 25;634(1-3):138-41.

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

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