1. Anti-infection
  2. Bacterial
    Antibiotic
  3. Bicyclomycin benzoate

Bicyclomycin benzoate (Synonyms: FR2054)

Cat. No.: HY-101128 Purity: 99.85%
Handling Instructions

Bicyclomycin benzoate is an antibiotic exhibiting activity against a broad spectrum of Gram-negative bacteria and against the Gram-positive bacterium.

For research use only. We do not sell to patients.

Bicyclomycin benzoate Chemical Structure

Bicyclomycin benzoate Chemical Structure

CAS No. : 37134-40-0

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10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
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10 mg USD 216 In-stock
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25 mg USD 456 In-stock
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50 mg USD 816 In-stock
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100 mg USD 1440 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Bicyclomycin benzoate is an antibiotic exhibiting activity against a broad spectrum of Gram-negative bacteria and against the Gram-positive bacterium.

In Vitro

The primary action of bicyclomycin is due to interference with the biosynthesis of lipoprotein and its assembly to peptidoglycan in the cell envelope of E. coli. At the lethal level, bicyclomycin is shown to inhibit the synthesis of RNA and protein in the growing cells of E. coli 15 THU[1]. Bicyclomycin targets the rho transcription termination factor in Escherichia coli. Bicyclomycin is a modest rho inhibitor, can disrupt the rho molecular machinery thereby leading to a catastrophic effect caused by the untimely overproduction of proteins not normally expressed constitutively, thus leading to a toxic effect on the cells[2]. The inhibition of rho poly(C)-stimulated hydrolysis of ATP by bicyclomycin has been found to proceed by a non-competitive, reversible pathway with respect to ATP (Ki=20 μM)[3].

In Vivo

Bicyclomycin has low excretion rate after a single intramuscular dose of 50 mg/kg in rats. Bicyclomycin is well distributed in various tissues, and the highest concentration is observed in the kidney at 100 mg/kg[4].

Molecular Weight

406.39

Formula

C₁₉H₂₂N₂O₈

CAS No.

37134-40-0

SMILES

O[[email protected]]([[email protected]](NC1=O)(OCCC2=C)C(N[[email protected]]12O)=O)[[email protected]@](C)(O)COC(C3=CC=CC=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (246.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4607 mL 12.3035 mL 24.6069 mL
5 mM 0.4921 mL 2.4607 mL 4.9214 mL
10 mM 0.2461 mL 1.2303 mL 2.4607 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[3]

ATPase activity assays are carried out with rho (100 ng) except that either bicyclomycin (0–60 μM) or dihydrobicyclomycin (0–90 μM) is added to the reaction solution. The samples are preheated to 32°C (2.5 min), and the reaction is initiated by the addition of ATP (9.1–100 μM) and [g-32P]ATP (0.5mCi) to the side of the tube, briefly vortexed, centrifuged (2 s), and returns to the water bath. Aliquots (1 mL) are removed at five time points (15, 30, 45, 60, and 75 s), and spotted on Baker-Flex cellulosePEI TLC plates. The rates of reaction are determined by measuring the relative amount of radiolabeled inorganic phosphate and ATP and then plotting the amount of ATP hydrolyzed versus time. The initial rates for each ATP concentration plus or minus inhibitors are plotted as double reciprocal plots[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4]

Rats: A total of 25 SD male rats receives intramuscular administration of bicyclomycin at a single dose of 50mg/kg. Blood samples are taken by heart-puncture from 5 rats each at 0.5, 1, 2, 3, and 5 hours after the administration[4].

Mice: A total of 40 ICR male mice receives intramuscular administration of bicyclomycin at a single dose of 50mg/kg. Eight mice each are bled at 5, 10, 20, 30 and 60 minutes after administration by heart-puncture with heparin[4].

Rabbits: Five rabbits and 5 dogs are given bicyclomycin intramuscularly at a single dose of 50 mg/kg and blood samples are withdrawn from these animals at similar intervals. The samples are allowed to clot and sera are separated for assay by the cylinder plate method[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.85%

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Keywords:

BicyclomycinFR2054FR 2054FR-2054BacterialAntibioticInhibitorinhibitorinhibit

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Product Name:
Bicyclomycin benzoate
Cat. No.:
HY-101128
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