L-365260 hemihydrate

L-365260半水合物

L-365260 hemihydrate

L659047-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B) , with K i s of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner Appearance:Solid IC50& Target:Ki: 1.9 nM (gastrin); 2.0 nM (CCK-B) . In Vitro:L-365260 hemihydrate exhibits a similar high affinity for brain CCK-B receptors of rats, mice and man, and a lower affinity for gastrin and brain CCK-B (IC 50 =20-40 nM) receptors in dog tissues. L-365260 (1 μM) hemihydrate strongly attenuates the CC In Vivo:L-365260 hemihydrate (0.1-30mg/kg; p.o.) antagonizes gastrin-stimulated acid secretion in mice (ED 50 =0.03mg/kg), rats (ED 50 =0.9mg/kg) and guinea pigs (ED 50 =5.1mg/kg). L-365260 hemihydrate (0.01-10mg/kg; s.c.) enhances analgesia induced by Biological Activity:L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B) , with K i s of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner

C24H24N4O3

407.47 g/mol

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=CC=C4)=N2)=O.[1/2].O