SB 218795
Names
[ CAS No. ]:
174635-53-1
[ Name ]:
SB 218795
Biological Activity
[Description]:
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit[1][2].
[Related Catalog]:
[Target]
hNK3:13 nM (Ki)
hNK2:1220 nM (Ki)
[In Vitro]
SB 218795 (3-30 nM) antagonizes the contractile responses induced by the NK3 receptor agonist senktide in a surmountable and concentration-dependent manner[2]. SB 218795 (0.3-3 μM) does not affect the contractile responses of the NK3 receptor agonist [MePhe7]-NKB in the rabbit iris sphincter muscle[2].
[In Vivo]
SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%[2].
[References]
Chemical & Physical Properties
[ Density]:
1.237g/cm3
[ Boiling Point ]:
623.7ºC at 760 mmHg
[ Molecular Formula ]:
C25H20N2O3
[ Molecular Weight ]:
396.44
[ Flash Point ]:
331ºC
[ Exact Mass ]:
396.14700
[ PSA ]:
68.29000
[ LogP ]:
4.93680
[ Vapour Pressure ]:
1.78E-15mmHg at 25°C
[ Index of Refraction ]:
1.643
[ Storage condition ]:
-20°C