Lesogaberan (hydrochloride) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.

Product information

Molecular Weight: 177.54

Formula: C3H10ClFNO2P

Chemical Name: ((R)-3-amino-2-fluoropropyl)phosphinic acid hydrochloride

Smiles: Cl.NC[C@@H](F)CP(O)=O

InChiKey: BPIWCTHWQLSCJT-AENDTGMFSA-N

InChi: InChI=1S/C3H9FNO2P.ClH/c4-3(1-5)2-8(6)7;/h3,8H,1-2,5H2,(H,6,7);1H/t3-;/m1./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 (hydrochloride) (3-30 nM) enhances human islet cell proliferation in vitro.

In Vivo:

Lesogaberan (hydrochloride) potently stimulates recombinant human GABAB receptors and inhibits transient lower esophageal sphincter relaxation (TLESR) in dogs, with a biphasic dose-response curve. Oral Lesogaberan (hydrochloride) (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice. Lesogaberan (hydrochloride) (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.