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BETP
- Compound B
Axon 2259
CAS:
1371569-69-5
Purity:
99%
- Soluble in DMSO
- MF: C20H17F3N2O2S
- MW: 406.42
Description
Positive allosteric modulator (PAM) at the glucagon-like peptide 1 receptor (GLP-1; EC50 value 0.66 μM) with good selectivity over GLP-2, GIP, PTH, and glucagon receptors. BETP has a signifficant effect on cAMP accumulation, iCa2+ mobilization, and β-arrestin1 and β-arrestin2 recruitment in Flp-In-CHO cells stably expressing the human GLP-1R (pEC50 values 5.2, 5, 5.0, and 5.0, respectively). BETP induced glucose-dependent insulin secretion in vitro and in vivo, and increased calcium influx in CHO cells expressing GLP-1R.
More Information
| Parent CAS No. | 1371569-69-5 |
|---|---|
| Chemical Name | 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine |
| SMILES | C1C=C(COC2C=CC=C(C3N=C(S(=O)CC)N=C(C(F)(F)F)C=3)C=2)C=CC=1 |
| MFCD | N.A. |
| 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 |
| InChiKey | NTDFYGSSDDMNHI-UHFFFAOYSA-N |
| CID | 49868481 |
| Short Description | GLP-1 agonist |
References
- D. Wootten et al. Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands. Mol. Pharmacol. 2013, 83, 822-834.
- F.S. Willard et al. Small molecule allosteric modulation of the glucagon-like Peptide-1 receptor enhances the insulinotropic effect of oxyntomodulin. Mol. Pharmacol. 2012, 82, 1066-10673.
- Y.H. Cheong et al. Two small molecule agonists of glucagon-like peptide-1 receptor modulate the receptor activation response differently. Biochem. Biophys. Res. Commun. 2012, 417, 558-563.
- K.W. Sloop et al. Novel small molecule glucagon-like peptide-1 receptor agonist stimulates insulin secretion in rodents and from human islets. Diabetes. 2010, 59, 3099-3107.
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