VU 0650991

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Description: Non-competitive GLP-1 antagonist; orally bioavailable and brain penetrant
Chemical Name: 7-(4-Chlorophenyl)-5,8-dihydro-1,3-dimethyl-5,5-bis(trifluoromethyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for VU 0650991

VU 0650991 is a 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.

Technical Data for VU 0650991

M. Wt 440.73
Formula C16H11ClF6N4O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 488097-06-9
PubChem ID 1941609
Smiles CN1C(N(C2=C(C(C(F)(F)F)(C(F)(F)F)N=C(C3=CC=C(C=C3)Cl)N2)C1=O)C)=O

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.

Solubility Data for VU 0650991

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 44.07 100

Preparing Stock Solutions for VU 0650991

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for VU 0650991

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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Citations for VU 0650991

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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* your copy today!

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Peptides Involved in Appetite Modulation Scientific Review

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.