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 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 |
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 用途与合成方法
Neurotensin receptor 1 (NTS1)
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.
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).
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)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2022-07-01 | HY-105189 | 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 | 146362-70-1 | 5mg | 4800 |
2022-07-01 | HY-105189 | 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 | 146362-70-1 | 10mM * 1mLin DMSO | 6199 |