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BETP

Cat. No. M8394
BETP Structure
Size Price Availability Quantity
5mg USD 105  USD105 In stock
10mg USD 160  USD160 In stock
25mg USD 320  USD320 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

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).

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Francis S Willard, et al. Discovery and pharmacology of the covalent GLP-1 receptor (GLP-1R) allosteric modulator BETP: A novel tool to probe GLP-1R pharmacology

[2] Sujan Piya, et al. BETP degradation simultaneously targets acute myelogenous leukemia stem cells and the microenvironment

[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

[5] Reinhard Krmer, et al. BetP of Corynebacterium glutamicum, a transporter with three different functions: betaine transport, osmosensing, and osmoregulation

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