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146362-70-1

中文名称 2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
英文名称 SR 48692
CAS 146362-70-1
分子式 C32H31ClN4O5
分子量 587.07
MOL 文件 146362-70-1.mol
146362-70-1 结构式 146362-70-1 结构式

基本信息

中文别名
麦克林坦
美兰纳坦
2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
2-[[[1-(7-氯-4-喹啉)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-三环[3.3.1.13,7]癸烷-2-羧酸
英文别名
CS-334
SR 48692
Meclinertant
merclinertant
2-CARBOXYLIC ACID
meclinertant, CID 119192
2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]adamantane-2-carboxylic acid
2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Tricyclo[3.3.1.13,7]decane-2-carboxylic acid, 2-[[[1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-
所属类别
有机原料:羧酸类化合物及衍生物

物理化学性质

密度1.50
储存条件-20°C
溶解度在DMSO中的溶解度≥2mg/mL(加热)
形态粉末
颜色白色至米色

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302
WGK Germany3
RTECS号YD1988500
2-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2022/07/01HY-1051892-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
Meclinertant
146362-70-15mg4800元
2022/07/01HY-1051892-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
Meclinertant
146362-70-110mM * 1mLin DMSO6199元
2022/04/29HY-1051892-[[[1-(7-氯-4-喹啉基)-5-(2,6-二甲氧基苯基)-1H-吡唑-3-基]羰基]氨基]-金刚烷-2-羧酸
Meclinertant
146362-70-110mg11000元

常见问题列表

生物活性
Meclinertant (SR 48692) 是一种有效的,选择性的,非肽和口服活性神经降压素受体 (NTS1) 拮抗剂。在人结肠癌细胞中,Meclinertant 竞争性拮抗神经降压素诱导的细胞内 Ca2+ 动员,pA2 值为 8.13。Meclinertant 具有抗焦虑,抗上瘾和记忆障碍的作用。
靶点

Neurotensin receptor 1 (NTS1)

体外研究

In vitro, Meclinertant (SR 48692) competitively inhibits 125 I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC 50 values of 0.99 nM (guinea pig), 4.0 nM (rat mesencephalic cells), 7.6 nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7 nM (newborn mouse brain), 17.8 nM (newborn human brain), 8.7 nM (adult human brain), and 30.3 nM (HT-29 cells). Meclinertant also displaces 125 I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8 nM for adult mouse brain and 82.0 nM for adult rat brain).
In guinea pig striatal slices, Meclinertant blocks K + -evoked release of [ 3 H]dopamine stimulated by neurotensin with a potency (IC 50 = 0.46 nM) that correlates with its binding affinity.

体内研究

Meclinertant (SR 48692) treatment reverses at 80 μg/kg the turning behavior induced by intrastriatal injection of neurotensin in mice and with a long duration of action (6 hours).

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