坎利酮

生物活性靶点体外研究体内研究坎利酮试剂级价格

坎利酮

CAS号:976-71-6
英文名:Canrenone
中文名:坎利酮
CBNumber:CB0147626
分子式:C22H28O3
分子量:340.46
MOL File:976-71-6.mol

坎利酮化学性质

熔点 :158-1600C
比旋光度 :D +24.5° (chloroform)
沸点 :416.25°C (rough estimate)
密度 :1.1236 (rough estimate)
折射率 :1.5000 (estimate)
储存条件 :room temp
溶解度 :DMSO: soluble20mg/mL, clear
形态 :powder
颜色 :white to beige
旋光性 (optical activity) :[α]/D +17 to +24°, c = 1 in chloroform-d
水溶解性 :272.4ug/L(25 ºC)
InChI :InChI=1/C22H28O3/c1-20-9-5-15(23)13-14(20)3-4-16-17(20)6-10-21(2)18(16)7-11-22(21)12-8-19(24)25-22/h3-4,13,16-18H,5-12H2,1-2H3/t16-,17+,18+,20+,21+,22-/s3
InChIKey :UJVLDDZCTMKXJK-MUWITHSMNA-N
SMILES :[C@@]12(CCC(=O)O1)CC[C@@]1([H])[C@]3([H])C=CC4=CC(=O)CC[C@]4(C)[C@@]3([H])CC[C@]21C |&1:0,8,10,20,22,26,r|
LogP :2.54 at 25℃
CAS 数据库 :976-71-6
NIST化学物质信息 :Canrenone(976-71-6)

安全信息

危险品标志 :Xn,N
危险类别码 :40-51/53
安全说明 :36/37-61
危险品运输编号 :UN 3077 9 / PGIII
WGK Germany :3
海关编码 :29329990

坎利酮性质、用途与生产工艺

生物活性 Canrenone (Aldadiene; SC9376; SC14266) 是广泛用作利尿剂的醛固酮 (aldosterone) 拮抗剂。
靶点

Human Endogenous Metabolite
体外研究

Canrenone inhibits the production of eortieosterone, 18-hydroxydesoxyeortieosterone, 18-hydroxycorticosterone and aldosterone in a dose-dependent manner. Canrenone dose-dependently reduces platelet-derived growth factor–induced cell proliferation and motility. Canrenone inhibits the activity of the Na ⁺ /H ⁺ exchanger 1 induced by platelet-derived growth factor.
体内研究

Canrenone is the principal active metabolite of Spironolactone in the rat only for a limited period. During chronic treatment a difference developed between the effect of Spironolactone and Canrenone on the RAAS indicating a decrease in the anti-mineralocorticoid activity of Canrenone and an increase in the efficacy of Spironolactone.
化学性质微黄色或乳白色结晶性粉末（乙酸乙酯）。熔点149-151℃，165℃固化并重熔。
用途安体舒通的中间体。本身为醛甾酮拮抗剂。
用途
坎雷诺酮(螺内酯EP杂质F)是醛固酮拮抗剂。利尿剂。用于治疗心衰水肿和肝硬变腹水。
生产方法可用17-羟基-3-氧代-17α-孕甾-4-烯-21-羧酸-γ-内酯经脱氢制得。而前者则可从17α-炔基-3β,17β-二羟基雄甾-5-烯（即乙炔雄甾烯二醇）经炔基以甲基碘化镁置换、水解、成盐并催化氢化，生成3β,17β二羟基雄甾-5-烯-17α-丙酸钾，然后经内酯化及3-位羟基氧化制得该品。