3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺

生物活性靶点体外研究体内研究 3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺试剂级价格

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

3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺化学性质

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, soluble
酸度系数(pKa) :12.88±0.46(Predicted)
形态 :solid
颜色 :light yellow

安全信息

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。
靶点

NK3
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.

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).