BETP, GLP-1R Potentiator


Catalog No. size PriceQuantity
M60196-2S 2 mg solid $129
M60196-10S 10mg solid $535

Description

BETP is positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor. It covalently modifies cysteines 347 and 438 in GLP-1R. Specificity studies have shown that it has no activity on GLP-2, GIP, PTH or glucagon receptors. BETP has been shown to potentiate GLP-1R–dependent intracellular calcium mobilization but not cAMP accumulation in response to GLP-1(7-36)NH2 in recombinant cell lines. Conversely, BETP can enhance cAMP efficacy of GLP-1(9-36)NH2 at GLP-1R but not intracellular calcium mobilization. BETP also potentiates cAMP production of the dual-acting GLP-1R/glucagon (GCG) receptor (GCGR) agonist oxyntomodulin at GLP-1R. It promotes GLP-1(9-36)NH2–mediated glucose-dependent insulin secretion in rodent and human islet preparations as well as in rodent models following intravenous administration.

Product information

CAS Number: 1371569-69-5

Molecular Weight: 406.42

Formula: C20H17F3N2O2S

Chemical Name: 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine

Smiles: CCS(=O)C1N=C(C=C(N=1)C1=CC(=CC=C1)OCC1C=CC=CC=1)C(F)(F)F

InChiKey: NTDFYGSSDDMNHI-UHFFFAOYSA-N

InChi: InChI=1S/C20H17F3N2O2S/c1-2-28(26)19-24-17(12-18(25-19)20(21,22)23)15-9-6-10-16(11-15)27-13-14-7-4-3-5-8-14/h3-12H,2,13H2,1H3

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

BETP was used at 5-20 µM in vitro and cellular assays.

In Vivo:

BETP was administered through intravenous administration at 5 mg/kg to Wistar rats for IVGTT (In Vivo Intravenous Glucose Tolerance Test). Formulation: 10% ethanol-Solutol, 20% polyethylene glycol-400, and 70% phosphate-buffered saline, pH 7.4.

References:

  1. Sloop KW, et al. Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. (2010) Diabetes. 59(12):3099-107.
  2. Cheong YH, et al. Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently. (2012) Biochem Biophys Res Commun. 417(1):558-63.
  3. Willard FS, et al. Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin. (2012) Mol Pharmacol. 82(6):1066-73.

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed