| Stereochemistry | ACHIRAL |
| Molecular Formula | C17H24F3N3O3S |
| Molecular Weight | 407.451 |
| Optical Activity | NONE |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)S(=O)(=O)N[C@H]1CC[C@@H](CC1)C(=O)NC2=NC=C(C=C2)C(F)(F)F
InChI
InChIKey=WGEWUYACXPEFPO-AULYBMBSSA-N
InChI=1S/C17H24F3N3O3S/c1-16(2,3)27(25,26)23-13-7-4-11(5-8-13)15(24)22-14-9-6-12(10-21-14)17(18,19)20/h6,9-11,13,23H,4-5,7-8H2,1-3H3,(H,21,22,24)/t11-,13-
| Molecular Formula | C17H24F3N3O3S |
| Molecular Weight | 407.451 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Velneperit, also known as S-2367, is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist that was discovered by Shionogi Research Laboratories. It was developed for the oral treatment of obesity. Velneperit was in phase II trials, however, development was discontinued.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 5.3 nM [Ki] |
PubMed
Sample Use Guides
Obesity: tablet, 4 x 400 mg, taken once daily with morning meal, 54-weeks
Route of Administration:
Oral
Velneperit (S-2367) completely displaced the binding of [125I]PYY to membrane homogenates of CHO-K1 cells expressing mouse NPY Y5 receptor, with Ki value of 5.3 ± 0.4 nM. The
antagonistic effect of S-2367 for the NPY Y5 receptor was determined
using CHO-K1 cells expressing mouse NPY Y5 receptor in a cAMP assay. S-2367 inhibited NPY-mediated decrease in forskolin-induced cAMP formation in a concentration-dependent manner. The IC50 value of S-2367 was 169 ± 29 nM.
