SB 218795
Modify Date: 2025-08-27 15:31:12
SB 218795 structure
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Common Name | SB 218795 | ||
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| 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 218795SB 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 |
| InChIKey | IUMQXQJZIHWLIN-HSZRJFAPSA-N |
| SMILES | COC(=O)C(NC(=O)c1cc(-c2ccccc2)nc2ccccc12)c1ccccc1 |
| Storage condition | -20°C |
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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 |
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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 |
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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 |
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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 |
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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 |
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Name: Primary cell-based high-throughput screening assay for identification of compounds th...
Source: Johns Hopkins Ion Channel Center
Target: regulator of G-protein signaling 4 isoform 2 [Homo sapiens]
External Id: JHICC_RGS_Act_HTS
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|
Name: qHTS to identify inhibitors of the New Delhi Metallo-beta-lactamase (NDM): assay vali...
Source: NCGC
External Id: adst_MBL_Abs_LOPAC_o1
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Name: NCATS Kinetic Aqueous Solubility Profiling
Source: NCGC
Target: N/A
External Id: ADME-solubility1
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|
Name: Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
Source: NCGC
Target: N/A
External Id: SERCaMPGLuc-p1-antagonist
|
|
Name: Luminescence-based cell-based primary high throughput screening assay to identify ago...
Source: The Scripps Research Institute Molecular Screening Center
Target: mu-type opioid receptor isoform MOR-1 [Homo sapiens]
External Id: OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN
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|
Name: QFRET-based biochemical primary high throughput screening assay to identify exosite i...
Source: The Scripps Research Institute Molecular Screening Center
Target: disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens]
External Id: ADAM17_INH_QFRET_1536_1X%INH PRUN
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Name: Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay
Source: ChEMBL
Target: N/A
External Id: CHEMBL1266185
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Name: Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
Source: NCGC
External Id: SNCA-p-activity-luciferase
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Name: qHTS Validation Assay for Inhibitors of Ubiquitin-specific Protease USP2a Using CHOP2...
Source: NCGC
Target: ubiquitin carboxyl-terminal hydrolase 2 isoform a [Homo sapiens]
External Id: UBCH001
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Name: Binding Affinity of [125I]NKA towards Tachykinin receptor 2-CHO cell membranes (n=3-8...
Source: ChEMBL
Target: Substance-K receptor
External Id: CHEMBL818109
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