SB 222200
SB 222200 Basic information
- Product Name:
- SB 222200
- Synonyms:
-
- 3-METHYL-2-PHENYL-N-[(1S)-1-PHENYLPROPYL]-4-QUINOLINECARBOXAMIDE
- 3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide
- SB222200//3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxaMide
- (S)-3-METHYL-2-PHENYL-N-(1-PHENYLPROPYL)-4-QUINOLINECARBOXAMIDE
- SB 222200
- SB-222200; SB222200
- CS-1124
- 4-Quinolinecarboxamide, 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-
- CAS:
- 174635-69-9
- MF:
- C26H24N2O
- MW:
- 380.48
- Mol File:
- 174635-69-9.mol
SB 222200 Chemical Properties
- Melting point:
- 154℃
- Boiling point:
- 553.5±50.0 °C(Predicted)
- Density
- 1.142
- storage temp.
- Sealed in dry,2-8°C
- solubility
- DMSO: ~28 mg/mL, soluble
- form
- solid
- pka
- 12.88±0.46(Predicted)
- color
- light yellow
Safety Information
- Safety Statements
- 22-24/25
- WGK Germany
- 3
SB 222200 Usage And Synthesis
Uses
3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide is a chemical agent used in the preparation of acylpiperazinyl-pyrazoles as antagonists to the NK3 receptor as antipsychotics (1,2).
Definition
ChEBI: 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-4-quinolinecarboxamide is a member of quinolines.
Biological Activity
Potent and selective non-peptide NK 3 receptor antagonist. K i values are 4.4, >100,000 and 250 nM for human NK 3 , NK 1 and NK 2 receptors respectively. Brain penetrant and active in vivo .
in vivo
SB-222200 (5 mg/kg; 30 min pretreatment) produces inhibition of behavioral responses induced by NK-3 receptor-selective agonist senktide (HY-P0187) in mice[1].
SB-2222006 exhibits moderate oral bioavailability (rat 46%) and Cmax (rat 427 ng/mL) following oral administration (rat 10 mg/kg)[1].
SB-2222006 exhibits terminal elimination half-life (rat 1.9 h) due to high plasma clearance (56 mL/min/kg) following intravenous administration (rat 2.5 mg/kg)[1].
| Animal Model: | Male BALB/c mice (19-21 g)[1] |
| Dosage: | 5 mg/kg |
| Administration: | Oral administration |
| Result: | Produced 57% inhibition of senktide-induced behavioral responses in mice. |
| Animal Model: | Male Sprague-Dawley rats (300-400 g)[1] |
| Dosage: | 2.5 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral gavage |
| Result: | Oral bioavailability (46%), T1/2 (1.9 h), Cmax (427 ng/mL). |
IC 50
NK3
storage
Store at RT
SB 222200Supplier
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