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Closantel Bacterial inhibitor

Name: Closantel
SKU: S4106
Availability: InStock
Rating: 5 (1 reviews)

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.

Chemical Structure

Molecular Weight: 663.07

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.22

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Chemical Information, Storage & Stability

Molecular Weight	663.07	Formula	C₂₂H₁₄Cl₂I₂N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	57808-65-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

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. ^[1] 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. ^[2] 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. ^[3]
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. ^[3] This compound (7.5 mg/kg) combined with broad-spectrum anthelmintic is very effective against H. contortus but ineffective against Trichostrongylus spp in lambs. ^[4] It significantly reduces isotope levels in closantel-resistant adult Haemonchus contortus infected sheep. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9873460/ [2] https://pubmed.ncbi.nlm.nih.gov/16882029/ [3] https://pubmed.ncbi.nlm.nih.gov/2315284/ [4] https://pubmed.ncbi.nlm.nih.gov/3954695/ [5] https://pubmed.ncbi.nlm.nih.gov/9138034/

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