Antibacterial; coccidiostat; feed additives
Lasalocid sodium targets the cell membranes of susceptible organisms, such as coccidian parasites. As an ionophore, it forms stable, lipid-soluble complexes with monovalent cations (e.g., Na⁺, K⁺) and facilitates their transport across biological membranes. This ionophoric activity disrupts the normal ion gradients across the parasite's cell membrane, leading to an influx of Na⁺ and efflux of K⁺. This collapse of the ionic gradient impairs vital cellular functions, including nutrient uptake and energy production, ultimately leading to parasite death. Its selectivity is based on the higher sensitivity of coccidian parasites to ion gradients compared to host cells.

The cell wall is one major determinant of plant cell morphology, and is an attractive bioresource. Here, we report a novel strategy to modify plant cell wall property by small molecules. Lasalocid sodium (LS) was isolated by chemical screening to identify molecules that affect the cell morphology of tobacco BY-2 cells. LS treatment led to an increase in cell wall thickness, whilst the quantity and sugar composition of the cell wall remained unchanged in BY-2 cells. The chemical also disordered the cellular arrangement of hypocotyls of Arabidopsis plants, resulting in a decrease in hypocotyl length. LS treatment enhanced enzymatic saccharification efficiency in both BY-2 cells and Arabidopsis plants. Microarray analysis on Arabidopsis showed that exposure to LS upregulated type III peroxidase genes, of which some are involved in lignin biogenesis, and jasmonic acid response genes, and phloroglucinol staining supported the activation of lignification by the LS treatment. As jasmonic acid-mediated lignification is a typical reaction to cell wall damage, it is possible that LS induces cell wall loosening, which can trigger cell wall damage response. Thus, LS is a unique chemical for modification of cell wall and morphology through changes in cell wall architecture.[1]

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It is thought that monensin increases the efficiency of feed utilization by cattle by altering the rumen fermentation. We studied the effect of monensin and the related ionophore antibiotic Lasalocid sodium (Hoffman-LaRoche) on the growth of methanogenic and rumen saccharolytic bacteria in a complex medium containing rumen fluid. Ruminococcus albus, Ruminococcus flavefaciens, and Butyrivibrio fibrisolvens were inhibited by 2.5 mug of monensin or lasalocid per ml. Growth of Bacteroides succinogenes and Bacteroides ruminicola was delayed by 2.5 mug of monensin or lasalocid per ml. Populations of B. succinogenes and B. ruminicola that were resistant to 20 mug of either drug per ml were rapidly selected by growth in the presence of each drug at 5.0 mug/ml. Selenomonas ruminantium was insensitive to 40 mug of monensin or lasalocid per ml. Either antibiotic (10 mug/ml) inhibited Methanobacterium MOH, Methanobacterium formicicum, and Methanosarcina barkeri MS. Methanobacterium ruminantium PS was insensitive to 40 mug of monensin or 20 mug of lasalocid per ml. The methanogenic strain 442 was insensitive to 40 mug of monensin but sensitive to 10 mug of lasalocid per ml. The results suggest that monensin or lasalocid acts in the rumen by selecting for succinate-forming Bacteroides and for S. ruminantium, a propionate producer that decarboxylates succinate to propionate. The selection could lead to an increase in rumen propionate formation. Selection against H(2) and formate producers, e.g. R. albus, R. flavefaciens, and B. fibrisolvens, could lead to a depression of methane production in the rumen[2].
In vitro, Lasalocid sodium exhibits potent anticoccidial activity against various Eimeria species. Its activity is assessed by its ability to inhibit the growth and development of coccidian parasites in cell culture or in oocyst sporulation assays. The compound's ionophoric activity can be demonstrated in model membrane systems, where it facilitates the transport of cations. Detailed IC₅₀ values against specific parasites are not extensively provided in the referenced sources.

In vivo, Lasalocid sodium is used to prevent and treat coccidiosis in poultry and livestock. It is administered orally in feed. Its efficacy is demonstrated by reduced mortality, improved weight gain, and decreased oocyst shedding in treated animals. It is a well-established veterinary drug with a long history of use in animal health.

Non-cell-based assays for Lasalocid sodium are not typical, as its mechanism is ionophoric. However, its ion transport activity can be studied in artificial membrane systems, such as lipid bilayers or liposomes, by measuring the movement of cations across the membrane using ion-selective electrodes or fluorescent dyes.

Cellular assays for Lasalocid sodium are performed using coccidian parasite cultures to assess its anticoccidial activity. Parasites are treated with the compound, and their growth and development are monitored. The compound's effects on host cells are also assessed to determine its selectivity and potential cytotoxicity.

In vivo animal models for Lasalocid sodium involve poultry or livestock infected with coccidia. The compound is administered in the feed, and its efficacy is assessed by measuring clinical signs, mortality, weight gain, and oocyst shedding. These studies are essential for establishing its efficacy and safety in veterinary applications.

Lasalocid sodium has a molecular weight of 590.70 g/mol and a molecular formula of C₃₄H₅₃NaO₈. Its CAS number is 25999-20-6. The compound is a solid. It is soluble in organic solvents. Purity is typically ≥98%. Storage conditions: -20°C. The compound is supplied for research use only. Detailed pharmacokinetic parameters are not extensively reported.

The oral LD50 for mice was 146 mg/kg. (Kirk-Osmer Encyclopedia of Chemical Technology, 3rd Edition, edited by M. Grayson and D. Eckroth, New York: John Wiley & Sons, 1978, Vol. 3, No. 47). The intraperitoneal LD50 for mice was 64 mg/kg. (Kirk-Osmer Encyclopedia of Chemical Technology, 3rd Edition, edited by M. Grayson and D. Eckroth, New York: John Wiley & Sons, 1978, Vol. 3, No. 47).
Lasalocid sodium is a veterinary drug with a well-established safety profile when used as a feed additive at approved levels. However, it can be toxic to other species, particularly horses and dogs, and must be used with caution. The compound is intended for research use only in the context of this request and is not for human consumption. Standard laboratory safety precautions should be followed.

[1]. Sci Rep. 2016 Oct 3:6:34602. doi: 10.1038/srep34602.
[2]. Appl Environ Microbiol . 1979 Jul;38(1):72-7. doi: 10.1128/aem.38.1.72-77.1979.

Lasalocid is a polyether antibiotic used for the prevention and treatment of coccidiosis in poultry. It possesses multiple functions, including anticoccidiosis, action against bacterial metabolites, and ion carrier activity. It is a monohydroxybenzoic acid, β-hydroxy ketone, secondary alcohol, oxacyclopentane compound, monocarboxylic acid, oxacycloalkane compound, tertiary alcohol, and polyether antibiotic. It is the conjugate acid of lasalloxicillin (1-). Lasalocid is a drug with antibacterial and anticoccidioidal activity. It is produced by certain strains of the genus Streptomyces lasaliensis. There are reports and data regarding the presence of lasalloxicillin in Streptomyces. This cationic ion carrier antibiotic, extracted from Streptomyces lasaliensis, can, among other effects, block the flow of calcium ions in muscle fibers. It is used as an anticoccidial drug, particularly suitable for poultry. See also: Lasaloxine Sodium (in salt form); Bacitracin Zinc; Lasaloxine (ingredient); Banbemycin; Lasaloxine (ingredient)... See more...
Lasalocid sodium is a polyether antibiotic and ionophore used as a coccidiostat in veterinary medicine. It is the sodium salt of lasalocid acid. It is a research compound with a well-established history of use in animal health. Its CAS number is 25999-20-6.

C34H53NAO8

612.77

612.364

C, 66.64; H, 8.72; Na, 3.75; O, 20.89

25999-20-6

Lasalocid;25999-31-9

5360807

Typically exists as White to yellow solid at room temperature

1.119g/cm3

735.7ºC at 760mmHg

180ºC (dec.)(lit.)

224.8ºC

1.01E-22mmHg at 25°C

1.528

4.507

4

8

13

42

910

10

O=C([O-])C1=C(CC[C@@H](C)[C@H](O)[C@H](C)C([C@@H]([C@H]2O[C@@]([C@H]3CC[C@](O)(CC)[C@H](C)O3)(CC)C[C@@H]2C)CC)=O)C=CC(C)=C1O.[Na+]

BBMULGJBVDDDNI-OWKLGTHSSA-N

InChI=1S/C34H54O8/c1-9-25(31-21(6)18-34(11-3,42-31)26-16-17-33(40,10-2)23(8)41-26)30(37)22(7)28(35)19(4)12-14-24-15-13-20(5)29(36)27(24)32(38)39/h13,15,19,21-23,25-26,28,31,35-36,40H,9-12,14,16-18H2,1-8H3,(H,38,39)/t19-,21+,22+,23+,25+,26-,28+,31+,33-,34+/m1/s1

6-[(3R,4S,5S,7R)-7-[(2S,3S,5S)-5-ethyl-5-[(2R,5R,6S)-5-ethyl-5-hydroxy-6-methyloxan-2-yl]-3-methyloxolan-2-yl]-4-hydroxy-3,5-dimethyl-6-oxononyl]-2-hydroxy-3-methylbenzoic acid

NSC-243046; NSC 243046; Lasalocid A sodium salt; 25999-20-6; Bovatec; Lasalocid A Sodium; Sodium lasalocid; Avatec; Lasalocid sodium salt; Lasalocid sodium

2934.99.9001

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.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~163.19 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (4.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (4.08 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)