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Ascomycin

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Chemical Structure| 104987-12-4 同义名 : 长川霉素 ;FK520;FR-900520;Immunomycin. Ascomycin;L 683590;Changchuanmycin;Immunomycin
CAS号 : 104987-12-4
货号 : A113253
分子式 : C43H69NO12
纯度 : 96%
分子量 : 792.008
MDL号 : MFCD06198665
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(50.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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 ... 展开 >> This study is not being conducted in the United States Various Cities, Japan 收起 <<
NCT00232011 Atopic Dermatitis Phase 3 Completed - Japan ... 展开 >> This study is not being conducted in the United States Various Cities, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.26mL

0.25mL

0.13mL

6.31mL

1.26mL

0.63mL

12.63mL

2.53mL

1.26mL
参考文献

[1]Revill WP, Voda J, et al. Genetically engineered analogs of ascomycin for nerve regeneration. J Pharmacol Exp Ther. 2002 Sep;302(3):1278-85.

[2]Hatanaka H, Kino T, et al. FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot (Tokyo). 1988 Nov;41(11):1592-601.

[3]Wang C, Wang J, Yuan J, et al. Generation of Streptomyces hygroscopicus cell factories with enhanced ascomycin production by combined elicitation and pathway-engineering strategies. Biotechnol Bioeng. 2019;116(12):3382-3395

[4]Hatanaka H, Kino T, Miyata S, et al. FR-900520 and FR-900523, novel immunosuppressants isolated from a Streptomyces. II. Fermentation, isolation and physico-chemical and biological characteristics. J Antibiot(Tokyo).1988;41(11):1592-1601

[5]Mollison KW, Fey TA, Krause RA, et al. Nephrotoxicity studies of the immunosuppressants tacrolimus (FK506) and ascomycin in rat models. Toxicology. 1998;125(2-3):169-181