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Closantel Bacterial inhibitor

Cat.No.S4106

Closantel (R-31520,nsc 335306) is a gram positive antibacterial activity inhibitor, inhibiting the KinA/Spo0F system with IC50 of 3.8 μM.
Closantel Bacterial inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 663.07

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Quality Control

Batch: S410601 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.22%
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99.22

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (150.81 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 663.07 Formula

C22H14Cl2I2N2O2

 Storage (From the date of receipt)
CAS No. 57808-65-8 Download SDF Storage of Stock Solutions

Synonyms R-31520,nsc 335306 Smiles CC1=CC(=C(C=C1NC(=O)C2=C(C(=CC(=C2)I)I)O)Cl)C(C#N)C3=CC=C(C=C3)Cl

Mechanism of Action

In vitro

Closantel inhibits drug resistant S. aureus and E. faecium with MICs of 1 μg/mL and 1 μg/mL. This compound inhibits MRSA and E.faecalis with MICs of 2 μg/mL and 1 μg/mL. It completely blocks the infection of host cells with E. chaffeensis or A. phagocytophilum, treatment of infected cells 1 day post infection with this chemical clears infection in dose-dependent manner. This compound inhibits the autokinase activities of the three E. chaffeensis sensor kinases from E. chaffeensis. This chemical (50 μg/mL) causes an initial burst of contractions of much greater amplitude and frequency than normal in tissue vessel, the stimulation of amplitude and frequency lasted for nearly 15 min and is accompanied by a rise in muscle tone, which reaches a maximum at 16 min, at a level greater than 1.5 times the maximal normal amplitude.

In vivo

Closantel (10 mg/kg) results in gross surface damage from 24 hours onwards in rats administrated with 25 metacercarial cysts of F. hepatica, in the form of erosion of the anterior and posterior extremities of the fluke and large-scale sloughing of the tegument on both dorsal and ventral surfaces. This compound (7.5 mg/kg) combined with broad-spectrum anthelmintic is very effective against H. contortus but ineffective against Trichostrongylus spp in lambs. It significantly reduces isotope levels in closantel-resistant adult Haemonchus contortus infected sheep.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/3954695/
  • [5] https://pubmed.ncbi.nlm.nih.gov/9138034/

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