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Noncompetitive glucagon-like peptide-1 (GLP-1) receptor antagonist (IC50 = 0.65 - 0.69 μM). Displays >40-fold selectivity for GLP-1 receptor over glucagon receptors. Blocks activity of Exendin-4 (Cat. No. 1933) in potentiating insulin secretion from primary mouse pancreatic islets in vitro. Decreases blood insulin and increases blood glucose levels in vivo. Brain penetrant and orally bioavailable.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 440.73. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.27 mL||11.34 mL||22.69 mL|
|5 mM||0.45 mL||2.27 mL||4.54 mL|
|10 mM||0.23 mL||1.13 mL||2.27 mL|
|50 mM||0.05 mL||0.23 mL||0.45 mL|
References are publications that support the biological activity of the product.
Nance et al (2017) Discovery of a novel series of orally bioavailable and CNS penetrant GLP-1R noncompetitive antagonists based on a 1,3-disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione core. J.Med.Chem. 60 1611 PMID: 28103022
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Keywords: VU 0650991, VU 0650991 supplier, VU0650991, GLP1, glucagon, like, peptide, 1, receptor, antagonism, antagonists, brain, penetrant, orally, bioavailable, Glucagon-Like, Peptide, Receptors, 6355, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.