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.
Product information
CAS Number: 477956-38-0
Molecular Weight: 349.31
Formula: C13H17FNO5PS
Chemical Name: [(2R)-3-amino-2-fluoropropyl]phosphinic acid; naphthalene-2-sulfonic acid
Smiles: NC[C@@H](F)CP(O)=O.OS(=O)(=O)C1=CC2=CC=CC=C2C=C1
InChiKey: GEUAKFFEFNASOW-ZYRQIYSTSA-N
InChi: InChI=1S/C10H8O3S.C3H9FNO2P/c11-14(12,13)10-6-5-8-3-1-2-4-9(8)7-10;4-3(1-5)2-8(6)7/h1-7H,(H,11,12,13);3,8H,1-2,5H2,(H,6,7)/t;3-/m.1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro.
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. Oral Lesogaberan (0.08?mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice. 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.
Products are for research use only. Not for human use.
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