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AZD7687

CAT: 0931-T14382-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0931-T14382-01Size:25 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1166827-44-6
Target
Others, Acyltransferase
Related Pathways
Metabolism, Others
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 ≥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.
Smiles
Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Molecular Formula
C21H25N3O3
Molecular Weight
367.44
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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