3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
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- CAS号:
- 174635-69-9
- 英文名:
- SB 222200
- 英文别名:
- CS-1124;SB 222200;SB-222200; SB222200;(S)-3-Methyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide;(S)-3-METHYL-2-PHENYL-N-(1-PHENYLPROPYL)-4-QUINOLINECARBOXAMIDE;3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide;3-METHYL-2-PHENYL-N-[(1S)-1-PHENYLPROPYL]-4-QUINOLINECARBOXAMIDE;4-Quinolinecarboxamide, 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-;SB222200//3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxaMide
- 中文名:
- 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
- 中文别名:
- SB-222200,非肽NK3拮抗剂;(S)-3-甲基-2-苯基-N-(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
- CBNumber:
- CB6358752
- 分子式:
- C26H24N2O
- 分子量:
- 380.48
- MOL File:
- 174635-69-9.mol
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3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺化学性质
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熔点:
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154℃
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沸点:
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553.5±50.0 °C(Predicted)
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密度:
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1.142
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储存条件:
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Sealed in dry,2-8°C
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溶解度:
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DMSO: ~28 mg/mL, soluble
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酸度系数(pKa):
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12.88±0.46(Predicted)
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形态:
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solid
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颜色:
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light yellow
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3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺性质、用途与生产工艺
SB-222200 是一种有效、选择性、口服活性的，具有血脑屏障 (BBB) 渗透性的 NK-3 受体 (NK-3 receptor) 拮抗剂。SB-222200 被开发用于中枢神经系统疾病的研究。
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).
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Animal Model:
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Male BALB/c mice (19-21 g)
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Dosage:
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5 mg/kg
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Administration:
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Oral administration
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Result:
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Produced 57% inhibition of senktide-induced behavioral responses in mice.
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Animal Model:
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Male Sprague-Dawley rats (300-400 g)
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Dosage:
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2.5 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:
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Intravenous injection and oral gavage
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Result:
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Oral bioavailability (46%), T
1/2
(2.4 h for i.v.; 2.1 h for p.o.), C
max
(427 ng/mL).
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3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-15722 | SB-222200 | | 5 mg | 755元 |
| 2024/04/30 | HY-15722 | 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
SB-222200 | 174635-69-9 | 10mg | 1171元 |
3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
生产厂家
174635-69-9, 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 相关搜索:
- 合成有机化合物配体
- G蛋白偶联受体&G蛋白
- SB-222200,非肽NK3拮抗剂
- (S)-3-甲基-2-苯基-N-(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
- 174635-69-9
- (S)-3-Methyl-2-phenyl-N-(1-phenylpropyl)quinoline-4-carboxamide
- 4-Quinolinecarboxamide, 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]-
- CS-1124
- SB-222200; SB222200
- SB 222200
- (S)-3-METHYL-2-PHENYL-N-(1-PHENYLPROPYL)-4-QUINOLINECARBOXAMIDE
- SB222200//3-Methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxaMide
- 3-Methyl-2-phenyl-N-((1S)-1-phenylpropyl)quinoline-4-carboxamide
- 3-METHYL-2-PHENYL-N-[(1S)-1-PHENYLPROPYL]-4-QUINOLINECARBOXAMIDE