For research use only. Not for therapeutic Use.
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].
GLP-1R Antagonist 1 (compound 5d) (0.3-10 μM) inhibits the activity of glucagon-like peptide 1 (GLP-1) (7-36) amide in a dose-dependent manner in human TREx293 HEK cells[1].
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
| Catalog Number | I018783 |
| CAS Number | 488097-06-9 |
| Synonyms | 7-(4-chlorophenyl)-1,3-dimethyl-5,5-bis(trifluoromethyl)-8H-pyrimido[4,5-d]pyrimidine-2,4-dione |
| Molecular Formula | C16H11ClF6N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H11ClF6N4O2/c1-26-11-9(12(28)27(2)13(26)29)14(15(18,19)20,16(21,22)23)25-10(24-11)7-3-5-8(17)6-4-7/h3-6H,1-2H3,(H,24,25) |
| InChIKey | MFEIZMHODFOWAT-UHFFFAOYSA-N |
| SMILES | CN1C2=C(C(=O)N(C1=O)C)C(N=C(N2)C3=CC=C(C=C3)Cl)(C(F)(F)F)C(F)(F)F |
| Reference | [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. |
