Product Name :
Lesogaberan
Description:
Lesogaberan (AZD-3355) 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 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 inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.
CAS:
344413-67-8
Molecular Weight:
140.07
Formula:
C3H8FNO2P
Chemical Name:
[(2R)-3-amino-2-fluoropropyl](hydroxy)oxo-λ⁵-phosphanylium
Smiles :
NC[C@@H](F)C[P+](O)=O
InChiKey:
WVTGPBOMAQLPCP-GSVOUGTGSA-O
InChi :
InChI=1S/C3H7FNO2P/c4-3(1-5)2-8(6)7/h3H,1-2,5H2/p+1/t3-/m1/s1
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.
Additional information:
Lesogaberan (AZD-3355) 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 for rat GABAB and GABAA receptors, as measured by displacement of [3H]GABA binding in brain membranes: 5.{{β-Muricholic acid} medchemexpress|{β-Muricholic acid} Endogenous Metabolite|{β-Muricholic acid} Epigenetics|{β-Muricholic acid} Technical Information|{β-Muricholic acid} Formula|{β-Muricholic acid} manufacturer} 1 nM and 1.{{Mupirocin} MedChemExpress|{Mupirocin} Anti-infection|{Mupirocin} Protocol|{Mupirocin} In Vivo|{Mupirocin} supplier|{Mupirocin} Cancer} 4 μM, respectively. Lesogaberan inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action.|Product information|CAS Number: 344413-67-8|Molecular Weight: 140.07|Formula: C3H8FNO2P|Chemical Name: [(2R)-3-amino-2-fluoropropyl](hydroxy)oxo-λ⁵-phosphanylium|Smiles: NC[C@@H](F)C[P+](O)=O|InChiKey: WVTGPBOMAQLPCP-GSVOUGTGSA-O|InChi: InChI=1S/C3H7FNO2P/c4-3(1-5)2-8(6)7/h3H,1-2,5H2/p+1/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.PMID:32644399 |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.|