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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

Chemical Information

{4-[4-(6-Carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid

AZD-7687 is under investigation in clinical trial NCT01119352 (AZD7687 Multiple Ascending Dose Study).

CAS Number1166827-44-6
PubChem CID42636350
IUPAC Name2-[4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
Molecular FormulaC21H25N3O3
Molecular Weight367.4
XLogP3.2
Topological Polar Surface Area106
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count5
Heavy Atom Count27
Formal Charge0
Complexity525
SMILES
CC1=C(N=C(C(=N1)C)C(=O)N)C2=CC=C(C=C2)C3CCC(CC3)CC(=O)O
InChI
InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)
InChIKey
YXFNPRHZMOGREC-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of {4-[4-(6-Carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl}acetic acid
CAS: 1166827-44-6
CID: 42636350
Formula: C21H25N3O3
MW: 367.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight367.4
XLogP33.2
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count5
Rotatable Bond Count5
Exact Mass367.18959167
Monoisotopic Mass367.18959167
Topological Polar Surface Area106 Ų
Heavy Atom Count27
Formal Charge0
Complexity525
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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