3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺
- CAS号:174635-69-9
- 英文名:SB 222200
- 中文名: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
- 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, soluble
- 酸度系数(pKa) :12.88±0.46(Predicted)
- 形态 :solid
- 颜色 :light yellow
- 安全说明 :22-24/25
- WGK Germany :3
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
- 生物活性 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。
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靶点
NK3
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体外研究
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.
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体内研究
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).
- 更新日期：2024/11/08
- 产品编号：HY-15722
- 产品名称：SB-222200
- CAS编号：
- 包装：5 mg
- 价格：755元
- 更新日期：2024/11/08
- 产品编号：HY-15722
- 产品名称：3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺 SB-222200
- CAS编号：174635-69-9
- 包装：10mg
- 价格：1171元
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
