| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Closantel sodium targets the same enzymes and pathways as Closantel. It is a potent and specific inhibitor of filarial chitinases, such as Onchocerca chitinase (OvCHT1). It also inhibits the AMP transferase FICD. Additionally, it is an allosteric inhibitor of SPAK and OSRI. Its mechanism of action in parasites involves the inhibition of fumarate reductase.
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| ln Vitro |
In contrast to protozoan and human chitinases, as well as human chitinase, cyclomethrin sodium is a well-known anthelmintic medication that exhibits a high degree of specificity for filarial family chitinases [1].
In vitro, Closantel sodium is a potent inhibitor of Onchocerca chitinase with an IC50 of 1.6 µM and a Ki of 468 nM. It inhibits FICD-mediated BiP/GRP78 AMPylation in intact cells. It is highly specific for filarial family chitinases compared to those from protozoans and the human chitinase. |
| ln Vivo |
In vivo, Closantel sodium (7.5 mg/kg) in combination with a broad-spectrum anthelmintic shows moderate efficacy against caprine Trichostrongylus spp, but is highly effective against Haemonchus contortus. It is effective against liver fluke, bloodsucking nematodes, and larval stages of some arthropods in sheep and cattle.
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| Enzyme Assay |
Closantel sodium is evaluated in cell-free enzymatic assays using purified chitinase or FICD enzymes. The compound is incubated with the enzyme and a substrate, and the inhibition of enzyme activity is measured. IC50 and Ki values are determined to quantify the potency of inhibition.
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| Cell Assay |
Closantel sodium is assessed in cell-based assays to study its effects on parasite viability and enzyme inhibition. Parasite cultures are treated with Closantel sodium, and the inhibition of growth and viability is measured. Its effects on FICD-mediated AMPylation are evaluated in intact cells.
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| Animal Protocol |
Closantel sodium is administered orally or by injection in animal models to evaluate its anthelmintic efficacy. It is effective against Haemonchus contortus and other parasites in sheep and cattle. Efficacy is assessed by measuring parasite load reduction and fecal egg counts. It is used in veterinary medicine.
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| ADME/Pharmacokinetics |
Closantel sodium has a molecular weight of 685.06 and a molecular formula of C22H13Cl2I2N2NaO2. It has a CAS number of 61438-64-0. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Closantel sodium is a veterinary anthelmintic and is not intended for human therapeutic use. No detailed toxicity data is available for this compound beyond its veterinary applications. It is used in veterinary medicine.
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| References |
[1]. Amanda L Garner, et al. Design, synthesis, and biological activities of closantel analogues: structural promiscuity and its impact on Onchocerca volvulus. J Med Chem. 2011 Jun 9;54(11):3963-72.
[2]. G E Swan, et al. The pharmacology of halogenated salicylanilides and their anthelmintic use in animals. J S Afr Vet Assoc. 1999 Jun;70(2):61-70. |
| Additional Infomation |
Closantel sodium is the sodium salt form of Closantel. It is a salicylanilide compound with narrow-spectrum anthelmintic actions. It is effective against certain roundworms, flukes, and myiases. It is not approved for clinical use.
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| Molecular Formula |
C22H14CL2I2N2NAO2
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|---|---|
| Molecular Weight |
686.0635
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| Exact Mass |
683.834
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| CAS # |
61438-64-0
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| Related CAS # |
Closantel;57808-65-8;Closantel-13C6;1325559-20-3
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| PubChem CID |
23683671
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| Appearance |
White to yellow solid powder
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| Boiling Point |
590.5ºC at 760 mmHg
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| Melting Point |
>230ºC (dec.)
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| Flash Point |
310.9ºC
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| LogP |
4.512
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
659
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| Defined Atom Stereocenter Count |
0
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| SMILES |
IC1=C([H])C(=C([H])C(=C1O[H])C(N([H])C1=C([H])C(=C(C([H])=C1C([H])([H])[H])C([H])(C#N)C1C([H])=C([H])C(=C([H])C=1[H])Cl)Cl)=O)I.[Na+]
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| InChi Key |
LREGMDNUOGTSIK-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C22H14Cl2I2N2O2.Na/c1-11-6-15(17(10-27)12-2-4-13(23)5-3-12)18(24)9-20(11)28-22(30)16-7-14(25)8-19(26)21(16)29;/h2-9,17,29H,1H3,(H,28,30);/q;+1/p-1
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| Chemical Name |
sodium;2-[[5-chloro-4-[(4-chlorophenyl)-cyanomethyl]-2-methylphenyl]carbamoyl]-4,6-diiodophenolate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~182.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4576 mL | 7.2880 mL | 14.5760 mL | |
| 5 mM | 0.2915 mL | 1.4576 mL | 2.9152 mL | |
| 10 mM | 0.1458 mL | 0.7288 mL | 1.4576 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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