VU 0650991

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Cat.No. 6355 - VU 0650991 | C16H11ClF6N4O2 | CAS No. 488097-06-9
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 488097-06-9
PubChem ID 1941609
InChI Key MFEIZMHODFOWAT-UHFFFAOYSA-N
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

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

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

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References

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 glucagon-like peptide-1 receptor (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 J.Med.Chem. 60 1611 PMID: 28103022


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