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Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM. Taspoglutide (R1583, BIM51077) activates the GLP-1 receptor. Taspoglutide has comparable affinity (affinity constant 1.1±0.2 nM) to the natural ligand (affinity constant 1.5±0.3 nM) for the hGLP-1 receptor and exhibits comparable potency in stimulating cAMP production.
Taspoglutide in Sprague-Dawley rats and diabetic db/db mice have shown a dose-related enhancement of glucose-dependent insulin release, which lower blood glucose in the db/db mouse model of type 2 diabetes.
| Molecular Weight | 3339.71 |
| Formula | C152H232N40O45 |
| CAS Number | 275371-94-3 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
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