| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H24FN7O5S |
| Molecular Weight | 505.523 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)C1=NOC(=N1)C2CCN(CC2)C3=C(C(NC4=CC=C(C=C4F)S(C)(=O)=O)=NC=N3)[N+]([O-])=O
InChI
InChIKey=DGBKNTVAKIFYNU-UHFFFAOYSA-N
InChI=1S/C21H24FN7O5S/c1-12(2)18-26-21(34-27-18)13-6-8-28(9-7-13)20-17(29(30)31)19(23-11-24-20)25-16-5-4-14(10-15(16)22)35(3,32)33/h4-5,10-13H,6-9H2,1-3H3,(H,23,24,25)
| Molecular Formula | C21H24FN7O5S |
| Molecular Weight | 505.523 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
The potent, selective and orally active GPR119 agonist discovered at Arena Pharmaceuticals, Inc., AR231453 significantly increased insulin release in HIT-T15 cells (a hamster insulinoma-derived line with robust GPR119 expression) and in rodent islets. By contrast, no effect of this compound could be seen in islets isolated from GPR119-deficient mice, confirming that its effects were indeed mediated by GPR119.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
PubMed
Sample Use Guides
in mice: A total of 100 syngenic C57BL/6 mouse islets were transplanted under the left kidney of each chemically induced diabetic C57BL/6 mouse. Starting from the day of transplantation, these recipients were given bromodeoxyuridine BrdU) daily with or without AR231453 at 10 mg/kg/d.
Route of Administration:
Oral
