3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide
SB-222200
CAS: 174635-69-9
Molecular Formula: C26H24N2O
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide - Names and Identifiers
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide - Physico-chemical Properties
| Molecular Formula | C26H24N2O |
| Molar Mass | 380.48 |
| Density | 1.142 |
| Melting Point | 154℃ |
| Boling Point | 553.5±50.0 °C(Predicted) |
| Solubility | DMSO: ~28mg/mL, soluble |
| Appearance | solid |
| Color | light yellow |
| pKa | 12.88±0.46(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| MDL | MFCD00944072 |
| Use | SB 222200 |
| In vitro study | SB-222200 inhibits 125 I-[MePhe 7 ]neurokinin B (NKB) binding to CHO cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K i of 4.4 nM and antagonizes NKB-induced Ca 2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC 50 of 18.4 nM. SB-222200 is selective for hNK-3 receptors compared with hNK-1 (K i >100,000 nM) and hNK-2 receptors (K i =250 nM). SB-222200 (10 nM-1 μM) produces a concentration-dependent, surmountable inhibition of NKB-induced Ca 2+ mobilization in HEK 293-hNK-3R cells. |
| In vivo study | 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. SB-222200 exhibits terminal elimination half-lives (rat about 2 h) and high systemic plasma clearance (56 mL/min/kg), with a moderately large volume of distribution (3-5 L/kg). Animal Model: Male BALB/c mice (19-21 g) 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) 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%), T 1/2 (2.4 h for i.v.; 2.1 h for p.o.), C max (427 ng/mL). |
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 3 |
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.628 ml | 13.141 ml | 26.283 ml |
| 5 mM | 0.526 ml | 2.628 ml | 5.257 ml |
| 10 mM | 0.263 ml | 1.314 ml | 2.628 ml |
| 5 mM | 0.053 ml | 0.263 ml | 0.526 ml |
Last Update：2024-01-02 23:10:35
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CAS: 174635-69-9
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CAS: 174635-69-9
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View History
3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide
4-methyl-6-chloro-7-azaisatin
2,4-Thiazolidinedione, 5-[[5-(4-fluoro-2-hydroxyphenyl)-2-furanyl]Methylene]-
4-methyl-6-chloro-7-azaisatin
2,4-Thiazolidinedione, 5-[[5-(4-fluoro-2-hydroxyphenyl)-2-furanyl]Methylene]-