| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H18F6N4O |
| Molecular Weight | 444.3735 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@@](CC1=NC=C(CC2(CC2)C(F)(F)F)N1)(C3=CC=C(C=C3)N4C=CC=N4)C(F)(F)F
InChI
InChIKey=UJINBEQCDMOAHM-SFHVURJKSA-N
InChI=1S/C20H18F6N4O/c21-19(22,23)17(6-7-17)10-14-12-27-16(29-14)11-18(31,20(24,25)26)13-2-4-15(5-3-13)30-9-1-8-28-30/h1-5,8-9,12,31H,6-7,10-11H2,(H,27,29)/t18-/m0/s1
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
In mouse model of obesity, MK-5046 (25 mg/kg/day by sc infusion) caused reductions in body weight (8-9% as compared to vehicle-dosed animals) thatwere sustained for 14 days with no evidence of tachyphylaxis.
Route of Administration:
Other
Receptor binding was performed using membranes from CHO or HEK293 cells overexpressing the bombesine receptor. A 30 pM concentration of [125I]-[D-Tyr6,β-Ala11,Phe13,Nle14]-bombesin(6-14) (human assay) and 660 pM [3H]Bag-3 (rat and mouse assays) were used. For functional assays, agonist induced mobilization of intracellular Ca2+ was measured HEK293AEQ cells overexpressing BRS-3, using an aequorin bioluminescence assay.
ACTIVE MOIETY
