Name: AZD7687
Rating: 5 (10 reviews)

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HIT ID:HIT212669410
Cas No:1166827-44-6
常用名:AZD7687
IUPAC:2-[(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
IUPAC:2-[(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
InChI key:YXFNPRHZMOGREC-SHTZXODSSA-N

分子式:C21H25N3O3
分子量:367.449
氢键供体数 (HBD):2
氢键受体数 (HBA):5
LogP:2.5965428
SMILES:Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1 |wU:17.18,wD:20.22,(1.33,-5.39,;1.33,-6.93,;,-7.7,;,-9.24,;-1.33,-10.01,;1.33,-10.01,;2.67,-9.24,;2.67,-7.7,;4,-6.93,;5.33,-7.7,;4,-5.39,;1.33,-11.55,;2.67,-12.32,;2.67,-13.86,;1.33,-14.63,;,-13.86,;,-12.32,;1.33,-16.17,;2.67,-16.94,;2.67,-18.48,;1.33,-19.25,;1.33,-20.79,;,-21.56,;,-23.1,;-1.33,-20.79,;,-18.48,;,-16.94,)|
SMILES:Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1 |wU:17.18,wD:20.22,(1.33,-5.39,;1.33,-6.93,;,-7.7,;,-9.24,;-1.33,-10.01,;1.33,-10.01,;2.67,-9.24,;2.67,-7.7,;4,-6.93,;5.33,-7.7,;4,-5.39,;1.33,-11.55,;2.67,-12.32,;2.67,-13.86,;1.33,-14.63,;,-13.86,;,-12.32,;1.33,-16.17,;2.67,-16.94,;2.67,-18.48,;1.33,-19.25,;1.33,-20.79,;,-21.56,;,-23.1,;-1.33,-20.79,;,-18.48,;,-16.94,)|

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.

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