Lesogaberan napadisylate
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.
For research use only. We do not sell to patients.
- CAS No.: 477956-38-0
- Formula: C13H17FNO5PS
- Molecular Weight:349.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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]
In Vitro
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.
In Vivo
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 477956-38-0
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Molecular Weight 349.31
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Formula C13H17FNO5PS
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SMILES
O=S(C1=CC=C2C=CC=CC2=C1)(O)=O.O=P(C[C@H](F)CN)O
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Synonyms
AZD-3355 napadisylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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)
Lesogaberan napadisylate Related Classifications
HY-10061A Related Classifications
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