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Actagardin

 
Catalog No.
C5245
四环抗生素
组合的产品项目
规格价格库存 数量
1mg
¥ 4,983.00
Ship with 10-15 days
5mg
¥ 17,387.00
Ship with 10-15 days

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A

背景

Actagardin is a tetracyclic antibiotic.

Actagardin is a tetracyclic antibiotic produced by several species of Actinoplanes.

In vitro: During the repeated fermentations of actagardin, two new compounds, named D and E, were isolated. Compound D was found to be twice as active as actagardin against Streptococcus pyogenes C 203 and four times more active than actagardin against Staphylococcus aureus ATCC 6538, S. pneumoniae UC 41, and S. aureus TOUR in the in-vitro tests [1].

In vivo: Animal study showed that compound D was also more effective than the parent compound actagardin against experimental infections in mice with either S. pyogenes C 203 or S. aureus TOUR, after sc administration. However, compound D was ineffective at doses up to 150 mg/kg when given orally to mice infected with S. pyogenes C 203. Moreover, compound D (LD50 1,250 mg/kg, mice, ip) was about 2.5 times more toxic than actagardine (3,310 mg/kg). In addition, compound E showed practically no in vitro activity up to 50 μg/ml against the tested organisms [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Malabarba A, Landi M, Pallanza R, Cavalleri B.  Physico-chemical and biological properties of actagardine and some acid hydrolysis products. J Antibiot (Tokyo). 1985 Nov;38(11):1506-11.

化学属性

Physical AppearanceA solid
StorageStore at -20°C
M.Wt1890.2
Cas No.59165-34-3
FormulaC81H124N20O24S4
SynonymsAntibiotic A 3802-IV-3,Gardimycin
SolubilitySoluble in ethanol;methanol;DMSO;dimethyl formamide
Chemical NameD-cysteinyl-L-serylglycyl-L-tryptophyl-L-valyl-L-cysteinyl-(2S,3S)-2-amino-3-mercaptobutanoyl-L-leucyl-(2S,3S)-2-amino-3-mercaptobutanoyl-L-isoleucyl-L-a-glutamyl-L-cysteinylglycyl-(2S,3S)-2-amino-3-mercaptobutanoyl-L-valyl-L-isoleucyl-L-cysteinyl-L-alany
SDFDownload SDF
Canonical SMILESO=C(CN1)N[C@@H](CC2=CNC3=C2C=CC=C3)C(N[C@@H](C(C)C)C(N[C@H](C(N[C@H]([C@H](C)SC[C@](C(NCC(N[C@@]([C@@H]4C)([H])C(N[C@@H](C(C)C)C(N[C@@]5([H])[C@@H](C)CC)=O)=O)=O)=O)([H])NC6=O)C(N[C@@H](CC(C)C)C(N[C@](C(N[C@]([C@@H](C)CC)([H])C(N[C@H]6CCC(O)=O)=O)=O)
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质量控制

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批次:

化学结构

Actagardin