Lesogaberan napadisylate - CAS# 477956-38-0


Catalog No. Size PriceQuantity
M34969-C Contact sales@xcessbio.com for quotation $100

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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