SB 218795

Modify Date: 2024-01-11 16:00:35

SB 218795 Structure
SB 218795 structure
Common Name SB 218795
CAS Number 174635-53-1 Molecular Weight 396.44
Density 1.237g/cm3 Boiling Point 623.7ºC at 760 mmHg
Molecular Formula C25H20N2O3 Melting Point N/A
MSDS N/A Flash Point 331ºC

 Use of SB 218795


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].

 Names

Name methyl (2R)-2-phenyl-2-[(2-phenylquinoline-4-carbonyl)amino]acetate

 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

[1]. Giardina GA, et, al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J Med Chem. 1997 Jun 6;40(12):1794-807.

[2]. Medhurst AD, et, al. In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br J Pharmacol. 1997 Oct;122(3):469-76.

[3]. Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32(4):487-94.

 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

 Synthetic Route

~%

SB 218795 Structure

SB 218795

CAS#: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

~%

SB 218795 Structure

SB 218795

CAS#: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

~%

SB 218795 Structure

SB 218795

CAS#: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

~%

SB 218795 Structure

SB 218795

CAS#: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

~%

SB 218795 Structure

SB 218795

CAS#: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
Top Suppliers:I want be here


Get all suppliers and price by the below link:

SB 218795 suppliers

SB 218795 price