BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. BETP is a positive allosteric modulator of the GLP-1 receptor that potentiates cAMP accumulation and glucose-dependent insulin release in pancreatic islet cells, in the presence of the weak GLP-1 metabolite, GLP-1(9-36). BETP has additive effects on the endogenous GLP-1 receptor ligand GLP-1(7-36).
Molecular Weight | 406.42 |
Formula | C20H17F3N2O2S |
CAS Number | 1371569-69-5 |
Solubility (25°C) | DMSO ≥ 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Janice L Robertson. Interrogating the conformational dynamics of BetP transport
[4] Stanislav Maximov, et al. Stimulus analysis of BetP activation under in vivo conditions
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