VU 0650991

Name: VU 0650991
Brand: Tocris Bioscience
SKU: 6355

Tocris Bioscience, part of Bio-Techne | Catalog # 6355

Citations (1)

COA / SDS

Non-competitive GLP-1 antagonist; orally bioavailable and brain penetrant

Key Product Details

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)
Molecular Weight:	440.73

View Full Technical Details for VU 0650991

Technical Data
Citations

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
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 for VU 0650991

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	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.

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 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. 2017 PMID: 28103022