| Identification | Back Directory | [Name]
7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione | [CAS]
488097-06-9 | [Synonyms]
VU 0650991
GLP-1R Antagonist 1
7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione
Pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione, 7-(4-chlorophenyl)-5,8-dihydro-1,3-dimethyl-5,5-bis(trifluoromethyl)- | [Molecular Formula]
C16H11ClF6N4O2 | [MDL Number]
MFCD03288400 | [MOL File]
488097-06-9.mol | [Molecular Weight]
440.728 |
| Hazard Information | Back Directory | [Description]
VU 0650991 is a non-competitive GLP-1 antagonist that is orally bioavailable and acts as a brain penetrant. | [Uses]
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM[1]. | [in vivo]
GLP-1R Antagonist 1 (compound 5d) (10 mg/kg, p.o.) increases the levels of blood glucose and decreases the levels of blood insulin in male Sprague-Dawley rats[1].
1.19 Pharmacokinetic Analysis in MC38 Syngeneic Model[1]| Route | Dose (mg/kg) | CLp (mL/min/kg) | t1/2 (min) | Vss (L/kg) | %F | | i.v., p.o. | 1, 3 | 4.79 | 587 | 3.57 | 50 |
| [storage]
Store at -20°C | [References]
[1] Kellie D. Nance, et al. Discovery of a novel series of orally bioavailable and CNS penetrant Glucagon-Like Peptide 1 Receptor (GLP-1R) non-competitive 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. 19 Jan 2017. DOI:10.1021/acs.jmedchem.6b01706 |
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BOC Sciences
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www.bocsci.com |
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