VU 0650991

Catalog #: 6355 Datasheet / COA / SDS

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VU 0650991 | CAS No. 488097-06-9 | Glucagon-Like Peptide 1 Receptor Antagonists

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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%

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Biological Activity

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

M.Wt:

440.73

Formula:

C₁₆H₁₁ClF₆N₄O₂

Solubility:

Soluble to 100 mM in DMSO

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

488097-06-9

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.

Background References

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.
Nance et al.
J.Med.Chem., 2017;60:1611

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