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Actagardin tetracyclic antibiotic

Catalog No.C5245
Size Price Stock Qty
1mg
$303.00
In stock
5mg
$1,059.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

Actagardin

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Chemical Properties

Cas No. 59165-34-3 SDF Download SDF
Synonyms Antibiotic A 3802-IV-3,Gardimycin
Chemical Name D-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
Canonical SMILES O=C(CN1)N[[email protected]@H](CC2=CNC3=C2C=CC=C3)C(N[[email protected]@H](C(C)C)C(N[[email protected]](C(N[[email protected]]([[email protected]](C)SC[[email protected]](C(NCC(N[[email protected]@]([[email protected]@H]4C)([H])C(N[[email protected]@H](C(C)C)C(N[[email protected]@]5([H])[[email protected]@H](C)CC)=O)=O)=O)=O)([H])NC6=O)C(N[[email protected]@H](CC(C)C)C(N[[email protected]](C(N[[email protected]]([[email protected]@H](C)CC)([H])C(N[[email protected]]6CCC(O)=O)=O)=O)
Formula C81H124N20O24S4 M.Wt 1890.2
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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.