坎利酮

中文名称:

坎利酮

中文同义词:

雄甾-4,6-二烯-17β-醇-3-酮-17α-丙酸内酯;6-去氢睾(甾)酮-17α-丙酸-γ-内酯;坎利酮(CAS号:976-71-6);螺内酯EP杂质F;依普利酮杂质28;烯睾丙内酯;卡利酮;坎利酮溶液,100PPM

英文名称:

Canrenone

英文同义词:

phanurane;pregna-4,6-diene-21-carboxylicacid,17-hydroxy-3-oxo-,gamma-lactone,(17-alph;sc9376;spirolactonesc14266;CANRENOIC ACID GAMMA LACTONE;CANRENONE;CANRENONE-D4;4,6-ANDROSTADIEN[(17(B-1)-SPIRO-5)]-PERHYDROFURAN-2,3-DIONE

CAS号:

976-71-6

分子式:

C22H28O3

分子量:

340.46

EINECS号:

213-554-5

相关类别:

甾体激素原料中间体;医药原料药;小分子抑制剂;医药中间体;羰基化合物;心血管血液系统原料药;中间体刊利酮;Spironolacrone;Intermediates Fine Chemicals;Pharmaceuticals;Steroids;ASMANEX;原料中间体-原料药;药物杂质及中间体;医药原料

Mol文件:

976-71-6.mol

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)

CAS 数据库

976-71-6

NIST化学物质信息

Canrenone(976-71-6)

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

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。

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