中文名 | 关附甲素 |
英文名 | Guan-fu base A |
别名 | 关附素A 关附甲素 关白附子甲素 关附甲素标准品 关附甲素对照品 盐酸关附甲素标准品 关附甲素,关白附子甲素 盐酸关附甲素,关白附子甲素 |
英文别名 | BRN 5165899 Acehytisine Kwan-fu base A Guan-fu base A Kwan-Fu Base A (2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)- Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)- (2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate Hetisan-2,11,13,14-tetrol, 2,11-diacetate, (2-alpha,11-alpha,13R)- (2alpha,9xi,11alpha,20xi)-11,14-dihydroxyhetisan-2,13-diyl diacetate |
CAS | 1394-48-5 |
化学式 | C24H31NO6 |
分子量 | 429.51 |
InChI | InChI=1/C24H31NO6/c1-10-5-22-8-14-17-21(4)6-13(30-11(2)26)7-23(17)18(22)16(28)15(10)19(31-12(3)27)24(22,29)20(23)25(14)9-21/h13-20,28-29H,1,5-9H2,2-4H3/t13-,14?,15+,16+,17+,18?,19?,20?,21-,22?,23?,24-/m0/s1 |
密度 | 1.43±0.1 g/cm3(Predicted) |
沸点 | 541.5±50.0 °C(Predicted) |
比旋光度 | (CHCl3)+49 |
闪点 | 281.3°C |
蒸汽压 | 5.55E-14mmHg at 25°C |
溶解度 | 可溶于甲醇、乙醇、DMSO等有机溶剂 |
折射率 | 1.648 |
酸度系数 | 12.97±0.70(Predicted) |
存储条件 | 2-8℃ |
外观 | 白色结晶 |
物化性质 | 白色结晶,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于毛茛科植物黄花乌头的块根(关白附)。 |
体外研究 | Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1. Guanfu base A is a potent inhibitor of CYP2D6, with an IC 50 recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM). The effects of Guanfu base A is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an IC 50 of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve. |
体内研究 | Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the C max of dextrorphan being one-third that of the saline-treated group and area under the plasma concentration-time curve half that of the saline-treated group. |
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