Lesogaberan
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.
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- CAS No.: 344413-67-8
- Formule: C3H9FNO2P
- Masse moléculaire:141.08
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Ki: 5.1±1.2 nM (rat GABAB), 1.4±0.3 μM (rat GABAA)[1]
EC50: 8.6±0.77 nM (human GABAB receptor)[1]
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
8.64 nM
Compound: (R)-7
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Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR
Agonist activity at human recombinant GABABreceptor expressed in CHO-K1 cells assessed as inhibition of intracellular calcium release by FLIPR
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[PMID: 18578471] |
Lesogaberan (3-30 nM) enhances human islet cell proliferation in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human islet cells
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Concentration:3, 10, and 30 nM
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Incubation Time:4 days
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Result:Had a small but nonsignificant promitotic effect at 3 nM, while treatment at higher dosages (10 and 30 nM) led to a 2-3-fold increase in proliferation relative to that of islets cultured in medium alone.
Oral Lesogaberan (0.08 mg/mL; 48 hours) protects human islet β-cells from apoptosis in islet grafts in mice[2].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diabetic NOD/scid mice were implanted with human islets[2]
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Dosage:0.08 mg/mL
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Administration:Oral feeding; 48 hours
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Result:Significantly reduced the percentages of apoptotic islet cells and increased the frequency of insulin+ β-cells in human islet grafts.
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Animal Model:Female Sprague Dawley rats[1]
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Dosage:7 μmol/kg (Pharmacokinetic Analysis)
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Administration:Oral
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Result:High oral availability (88% in the dog and 100% in the rat) and relatively low systemic clearance. Plasma protein binding was 1% in rat and human plasma.
Chemical Information
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CAS No. 344413-67-8
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Masse moléculaire 141.08
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Formule C3H9FNO2P
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SMILES
O=P(O)C[C@H](F)CN
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Synonyms
AZD-3355
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Lehmann A, et al. (R)-(3-amino-2-fluoropropyl) phosphinic acid (AZD3355), a novel GABAB receptor agonist, inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action. J Pharmacol Exp Ther. 2009 Nov;331(2):504-12. [Content Brief]
[2]. Tian J, et al. Repurposing Lesogaberan to Promote Human Islet Cell Survival and β-Cell Replication. J Diabetes Res. 2017;2017:6403539. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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