拉诺康唑

概述生物活性靶点体内研究拉诺康唑试剂级价格

拉诺康唑

CAS号:101530-10-3
英文名:Lanoconazole
中文名:拉诺康唑
CBNumber:CB5333996
分子式:C14H10ClN3S2
分子量:319.83
MOL File:101530-10-3.mol

拉诺康唑化学性质

熔点 :141.50C
沸点 :477.6±55.0 °C(Predicted)
密度 :1.43±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :Chloroform (Slightly), Methanol (Slightly)
酸度系数(pKa) :3.76±0.10(Predicted)
颜色 :White
CAS 数据库 :101530-10-3(CAS DataBase Reference)

安全信息

危险品标志 :Xn
危险类别码 :22
WGK Germany :3
RTECS号 :NI3393500
毒性 :LD50 in male, female mice, rats (mg/kg): 3224, 2715, 993, 652 orally; 2158, 1743, 1655, 2596 i.p.; >5000 both species s.c.; LD50 dermally in rats: >5000 mg/kg (Munt)

拉诺康唑 MSDS

[4-(2-Chloro-phenyl)-1,3-dithiolan-2-ylidene]-2-imidazol-1-yl-acetonitrile

拉诺康唑性质、用途与生产工艺

概述拉诺康唑为咪唑类抗真菌药物，作用机制同其他咪唑类药物，主要通过抑制14-甲基羊毛甾醇的脱14-甲基阶段，从而达到抑制真菌细胞麦角固醇合成的目的而具有抗真菌作用。
生物活性 Lanoconazole 是一种强效口服咪唑类抗真菌 (antifungal) 试剂，具有广谱的体内外抗真菌活性。Lanoconazole 通过抑制 sterol 14-alpha 去甲基酶，阻断真菌膜上的 ergosterol 生物合成，从而干扰 ergosterol 的生物合成。Lanoconazole 可用于皮肤真菌病和甲真菌病的研究。
靶点

IC50: antifungal

体内研究

Lanoconazole (treatment for ear; 0.3%-3%; 6 days) dose‐dependently suppressesTPA-induced irritant dermatitis, suppresses the production of neutrophil chemotactic factors such as keratinocyte‐derived chemokine and macrophage inflammatory protein‐2, and inhibited neutrophil infiltration to the inflammation site.Lanoconazole (oral administration; 3, 10 or 30 mg/kg; once a day; 3 weeks) significantly inhibits C. neoformans compared with the saline control in normal mice. In addtion, it significantly reduces the growth of C. neoformans in the lungs and brains of MAIDS mice.

Animal Model:	BALB/c mice
Dosage:	0.3%-3% dosage
Administration:	Treatment for ear
Result:	Exhibited an inhibition effect of LCZ on ear swelling induced by topical application of TPA in mice.

Animal Model:	Four week old C57BL/6 mice infected intraperitoneally with LP-BM5 murine leukaemia virus
Dosage:	3, 10 or 30 mg/kg
Administration:	Oral adminstration
Result:	Inhibited C. neoformans growth in both normal and C. neoformans -induced encephalitis MAIDS mice .

化学性质淡黄色结晶。熔点141.5℃。急性毒性LD₅₀雄、雌小鼠，雄、雌大鼠(mg/kg)：3224，2715，993，652口服；2158，1743，1655，2596腹腔注射；全部＞5000皮下注射。急性毒性LD₅₀大鼠致死量：＞5000mg/kg。
用途抗真菌药。在临床研究中。
生产方法 2-(1-咪唑基)乙腈与二硫化碳和氢氧化钾在二甲基甲酰胺中反应得连二硫酸酯的二钾盐，然后和1-(2-氯苯基)-1，2-二(甲磺酰氧基)乙烷环合。经硅胶柱层析分离(E)和(Z)异构体，而得拉诺康唑。