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Closthioamide

Catalog No.GC32291

Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.

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Closthioamide Chemical Structure

Cas No.: 1227367-59-0

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

The MIC is determined for the laboratory strains as follows. The assays are performed in sterile 96-well polystyrene microplates in 200 mL of cation-adjusted Mueller-Hinton (MH) broth. A serial dilution of the compound to test is made in 100 mL of medium and inoculated with 100 mL of fresh cell culture containing ~105 cfu/mL and incubated at 37°C for 20 h. The MIC is defined as the lowest concentration of antibiotic that inhibit visible growth[1].

References:

[1]. Chiriac AI, et al. Mode of action of closthioamide: the first member of the polythioamide class of bacterial DNA gyrase inhibitors. J AntimicrobChemother. 2015Sep;70(9):2576-88.
[2]. Lincke T, et al. Closthioamide: an unprecedented polythioamide antibiotic from the strictly anaerobic bacterium Clostridium cellulolyticum.Angew Chem Int Ed Engl. 2010 Mar 8;49(11):2011-3.

Background

Closthioamide is a potent inhibitor of bacterial DNA gyrase and highly active against Ec, MRSA, VRE and Mv), with MICs of 9.00 μM, 0.58 μM, 0.58 μM and 72.03 μM respectively.

Closthioamide is a potent inhibitor of bacterial DNA gyrase, isolated from the strictly anaerobic banterium Clostridium cellulolyticum and belongs to a new class of natural products[1]. In a standardized antimicrobial assay, it is found that closthioamide is highly active against a pathogenic, methicillin-resistant Staphylococcus aureus (MRSA) strain with a minimum inhibitory concentration (MIC) of 0.4 μg/mL-1 (0.58 μM). Closthioamide is even active against vancomycin-resistant Enterococcus faecalis (VRE) with the same low MIC value, and is thus significantly more potent against these bacteria than ciprofloxacin, the standard drugused against VRE, with remarkable strain selectivity. Furthermore, in a standardized cytotoxicity assay, closthioamide shows moderate antiproliferative and cytotoxic effects[2].

[1]. Chiriac AI, et al. Mode of action of closthioamide: the first member of the polythioamide class of bacterial DNA gyrase inhibitors. J AntimicrobChemother. 2015Sep;70(9):2576-88. [2]. Lincke T, et al. Closthioamide: an unprecedented polythioamide antibiotic from the strictly anaerobic bacterium Clostridium cellulolyticum.Angew Chem Int Ed Engl. 2010 Mar 8;49(11):2011-3.

Chemical Properties

Cas No. 1227367-59-0 SDF
Canonical SMILES S=C(C1=CC=C(O)C=C1)NCCC(NCCC(NCCCNC(CCNC(CCNC(C2=CC=C(O)C=C2)=S)=S)=S)=S)=S
Formula C29H38N6O2S6 M.Wt 695.04
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.4388 mL 7.1938 mL 14.3877 mL
5 mM 0.2878 mL 1.4388 mL 2.8775 mL
10 mM 0.1439 mL 0.7194 mL 1.4388 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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