中文名 | LEVCROMAKALIM |
英文名 | LEVCROMAKALIM |
别名 | 左色满卡林 左克罗卡林 |
英文别名 | brl38227 lemakalim LEVCROMAKALIM levcromakelim (3s-trans)-yrrolidinyl) 2h-1-benzopyran-6-carbonitrile,3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-p (3S,4R)-3β-Hydroxy-4-(2-oxopyrrolizino)-2,2-dimethyl-3,4-dihydro-6-cyano-2H-1-benzopyran (3S,4R)-3,4-DIHYDRO-3-HYDROXY-2,2-DIMETHYL-4-(2-OXO-1-PYRROLIDINYL)-2H-1-BENZOPYRAN-6-CARBONITRILE |
CAS | 94535-50-9 |
化学式 | C16H18N2O3 |
分子量 | 286.33 |
密度 | 1.31±0.1 g/cm3(Predicted) |
熔点 | 242-244° |
沸点 | 482.3±45.0 °C(Predicted) |
比旋光度 | D26 -52.2° (c = 1 in chloroform) |
溶解度 | DMSO: ≤ 10毫米,可溶 |
酸度系数 | 13.18±0.60(Predicted) |
存储条件 | Store at RT |
外观 | 固体 |
体外研究 | 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). |
安全术语 | S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
RTECS | DJ2177500 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.492 ml | 17.462 ml | 34.925 ml |
5 mM | 0.698 ml | 3.492 ml | 6.985 ml |
10 mM | 0.349 ml | 1.746 ml | 3.492 ml |
5 mM | 0.07 ml | 0.349 ml | 0.698 ml |
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