174635-53-1
174635-53-1 structure
- Name: SB 218795
- Chemical Name: methyl (2R)-2-phenyl-2-[(2-phenylquinoline-4-carbonyl)amino]acetate
- CAS Number: 174635-53-1
- Molecular Formula: C25H20N2O3
- Molecular Weight: 396.44
- Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
- Create Date: 2017-04-25 01:55:33
- Modify Date: 2025-08-27 15:31:12
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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].
| Name | methyl (2R)-2-phenyl-2-[(2-phenylquinoline-4-carbonyl)amino]acetate |
|---|
| 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]. |
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| 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 |
| 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 |
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174635-53-1 |
| Literature: Giardina, Giuseppe A. M.; Raveglia, Luca F.; Grugni, Mario; Sarau, Henry M.; Farina, Carlo; Medhurst, Andrew D.; Graziani, Davide; Schmidt, Dulcie B.; Rigolio, Roberto; Luttmann, Mark; Cavagnera, Stefano; Foley, James J.; Vecchietti, Vittorio; Hay, Douglas W. P. Journal of Medicinal Chemistry, 1999 , vol. 42, # 6 p. 1053 - 1065 |
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174635-53-1 |
| Literature: Giardina, Giuseppe A. M.; Raveglia, Luca F.; Grugni, Mario; Sarau, Henry M.; Farina, Carlo; Medhurst, Andrew D.; Graziani, Davide; Schmidt, Dulcie B.; Rigolio, Roberto; Luttmann, Mark; Cavagnera, Stefano; Foley, James J.; Vecchietti, Vittorio; Hay, Douglas W. P. Journal of Medicinal Chemistry, 1999 , vol. 42, # 6 p. 1053 - 1065 |
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174635-53-1 |
| Literature: Giardina; Sarau; Farina; Medhurst; Grugni; Foley; Raveglia; Schmidt; Rigolio; Vassallo; Vecchietti; Hay Journal of Medicinal Chemistry, 1996 , vol. 39, # 12 p. 2281 - 2284 |
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174635-53-1 |
| Literature: Giardina, Giuseppe A. M.; Sarau, Henry M.; Farina, Carlo; Medhurst, Andrew D.; Grugni, Mario; Raveglia, Luca F.; Schmidt, Dulcie B.; Rigolio, Roberto; Luttmann, Mark; Vecchietti, Vittorio; Hay, Douglas W. P. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1794 - 1807 |
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174635-53-1 |
| Literature: Giardina, Giuseppe A. M.; Raveglia, Luca F.; Grugni, Mario; Sarau, Henry M.; Farina, Carlo; Medhurst, Andrew D.; Graziani, Davide; Schmidt, Dulcie B.; Rigolio, Roberto; Luttmann, Mark; Cavagnera, Stefano; Foley, James J.; Vecchietti, Vittorio; Hay, Douglas W. P. Journal of Medicinal Chemistry, 1999 , vol. 42, # 6 p. 1053 - 1065 |
| Precursor 5 | |
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| DownStream 0 | |