左色满卡林
中文名称 | 左色满卡林 |
---|---|
中文同义词 | 左色满卡林;左克罗卡林 |
英文名称 | LEVCROMAKALIM |
英文同义词 | (3S,4R)-3,4-DIHYDRO-3-HYDROXY-2,2-DIMETHYL-4-(2-OXO-1-PYRROLIDINYL)-2H-1-BENZOPYRAN-6-CARBONITRILE;(3s-trans)-yrrolidinyl);LEVCROMAKALIM;2h-1-benzopyran-6-carbonitrile,3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-p;brl38227;lemakalim;levcromakelim;(3S,4R)-3β-Hydroxy-4-(2-oxopyrrolizino)-2,2-dimethyl-3,4-dihydro-6-cyano-2H-1-benzopyran |
CAS号 | 94535-50-9 |
分子式 | C16H18N2O3 |
分子量 | 286.33 |
EINECS号 | |
相关类别 | |
Mol文件 | 94535-50-9.mol |
结构式 |
左色满卡林 性质
熔点 | 242-244° |
---|---|
比旋光度 | D26 -52.2° (c = 1 in chloroform) |
沸点 | 482.3±45.0 °C(Predicted) |
密度 | 1.31±0.1 g/cm3(Predicted) |
储存条件 | Store at RT |
溶解度 | DMSO:可溶≤10 mM |
酸度系数(pKa) | 13.18±0.60(Predicted) |
形态 | 固体 |
颜色 | 白色至米白色 |
K + channel
Levcromakalim ((-)-Cromakalim) inhibits spontaneous contractions completely in a glibenclamide-sensitive manner. LevCromakalim (5 µM) inhibits spontaneous contractions, which are recovered by glibenclamide. Levcromakalim (1, 5 and 10 µM) inhibits phasic contractions to 34±21.1%, 20.1±20.0% and 0% of the control (n=5, respectively; P<0.05). Glibenclamide reverses the inhibition of spontaneous isometric contractions caused by LevCromakalim (5 µM) to 84±1.5% of the control (n=5; P<0.05). Levcromakalim (20 and 100 µM) also inhibits oxytocin (OXT) (10 nM)-induced phasic contractions to 34±21.4% and 14±12.6% of the control (n=6 and 4, respectively; P<0.05). Glibenclamide reverses the inhibition of spontaneous isometric contractions by LevCromakalim (100 µM) to 79±3.5% of the control (n=4; P<0.05). Tonic contraction by OXT is also suppressed by Cromakalim in a glibenclamide-sensitive manner.The function of the K ATP channels is examined with the specific channel opener LevCromakalim (Cromakalim). LevCromakalim induces dose-dependent relaxation in both the young and old mesenteric artery (MAs); and there is no difference in relaxation with age. However, the relaxation is markedly reduced in response to the high-salt (HS) diet in the old MAs (P<0.05). Maximum dilations to Levcromakalim (10 -4 M) are 97 ± 3% in the young MAs versus 98 ± 1% in the young salt arteries, while dilations are 99±0.7% in the old MAs when compared with 85 ± 5% in the old salt arteries (P<0.05).
安全信息
安全说明 | 22-24/25 |
---|---|
WGK Germany | 3 |
RTECS号 | DJ2177500 |
提供商 | 语言 |
---|---|
英文
|
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/11/08 | HY-14255 | 左色满卡林 Levcromakalim | 94535-50-9 | 2 mg | 800元 |
2024/11/08 | HY-14255 | 左色满卡林 Levcromakalim | 94535-50-9 | 5mg | 1200元 |