Product Overview
AZD7687 | T14382 | TargetMol Chemicals
CAS: 1166827-44-6
Smiles: Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Formula: C21H25N3O3
Pathway: Others
Target: Others
Receptor: N/A
Bioactivity: AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship [2]. Postprandial serum TAG excursion was measured during 8 h after a standardized mixed meal with fat energy content of 60% (SMM 60%; five cohorts, 1-20 mg), before (baseline) and after dosing, to assess effects on gut DGAT1 activity. in vivo: Multiple doses of AZD7687 (1, 2.5, 5, 10 and 20 mg/day, n=6 or n=12 for each) or placebo (n=20) were administered for 1 week. With AZD7687 doses >5 mg/day, gastrointestinal (GI) side effects increased; 11/18 of these participants discontinued treatment owing to diarrhoea[3]. Dose-dependent reductions in postprandial serum TAG were demonstrated with AZD7687 doses ā„5mg compared with placebo (p<0.01). Significant (p<0.001) increases in plasma GLP-1 and PYY levels were seen at these doses, but no clear effect on gastric emptying was demonstrated at the end of treatment.
Molecular Weight: 367, 449
