|(3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-8-乙基-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-十六氢-5,19-二羟基-3-[(1E)-2-[(1R,3R,4R)-4-羟基-3-甲氧基环己基]-1-甲基乙基]-14,16-二甲氧基-4,10,12,18-四甲基-15,19-环氧-3H-吡啶[2,1-c][1,4]氧杂环tricosine-11,7,20,21(4H,23H)-三酮|CsnPharm

CAS No.: 104987-12-4

Ascomycin/子囊霉素 Catalog No. CSN10340

Synonyms: Immunomycin;FR-900520;FK520

Ascomycin is a naturally occuring macrolide produced by the fermentation of Streptomyces hygroscopicus and an ethyl analog of tacrolimus (FK506), exhibiting strong immunosuppressant properties.

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技术信息

生物活性

描述Ascomycin (FK520) is a macrocyclic antibiotic that also exhibits antifungal and immunosuppressive activity^[3]. Ascomycin (Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties. IC50 values of FR-900520 for mouse mixed lymphocyte reaction was 0.55 nM. FR-900520, the major component, clearly prolonged skin allograft survival in rats^[4]. Ascomycin also had a 3-fold lower immunosuppressive potency in a popliteal lymph node hyperplasia assay, resulting in an equivalent therapeutic index consistent with a common mechanistic dependence on calcineurin inhibition. In 14-day studies, nephrotoxicity was not induced by continuous i.p. infusion of ascomycin at 10 mg/kg/day or daily oral administration (up to 50 mg/kg/day) in rats on a normal diet, nor by continuous i.v. infusion (up to 6 mg/kg/day) in rats on a low salt diet to enhance susceptibility^[5].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00231998	Atopic Dermatitis	Phase 3	Completed	-	Japan ... more >> This study is not being conducted in the United States Various Cities, Japan Collapse <<
NCT00232011	Atopic Dermatitis	Phase 3	Completed	-	Japan ... more >> This study is not being conducted in the United States Various Cities, Japan Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.2626 mL
- 6.3131 mL
- 12.6261 mL
- 5 mM
- 0.2525 mL
- 1.2626 mL
- 2.5252 mL
- 10 mM
- 0.1263 mL
- 0.6313 mL
- 1.2626 mL

技术信息

CAS号

104987-12-4

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C43H69NO12

运输

蓝冰

分子量

792.01

别名

Immunomycin;FR-900520;FK520;Changchuanmycin;L-683590;子囊霉素

溶解度

DMSO	490.0 mg/mL (618.7 mM)
Water	insoluble

动物实验配方

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Ascomycin/子囊霉素 Catalog No. CSN10340

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