3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 性质
| 熔点 | 154℃ |
|---|---|
| 沸点 | 553.5±50.0 °C(Predicted) |
| 密度 | 1.142 |
| 储存条件 | Sealed in dry,2-8°C |
| 溶解度 | DMSO：~28 mg/mL，可溶 |
| 酸度系数(pKa) | 12.88±0.46(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄色 |
3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 用途与合成方法
|
NK3
|
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.
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-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-04-30 | HY-15722 | 5 mg | 755 | ||
| 2024-04-30 | HY-15722 | 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 | 174635-69-9 | 10mg | 1171 |
