| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Bacterial ribosome (protein synthesis); Anaplasma marginale (anaplasmacide).
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|---|---|
| ln Vitro |
Gloxazone is an effective anaplasmacide against Anaplasma marginale infection. It has been investigated for activity against Gram-positive bacteria. The compound inhibits bacterial protein synthesis through interaction with the ribosomal machinery. Specific IC50 values for antibacterial activity and anaplasmacidal activity are not extensively detailed in publicly available literature.
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| ln Vivo |
In steers that have been purposely infected with Anaplasma margine, gloxazone (5 mg/kg; iv) is efficacious [1]. Oral gloxazone (0.1-3 mg/kg/day) induces nephrotoxicity and renal papillary colon damage [1].
In vivo, gloxazone (5 mg/kg; i.v.) is effective against Anaplasma marginale infection in cattle. However, gloxazone (0.1-3 mg/kg/day; oral) causes renal papillary necrosis and nephrotoxicity in rats. This nephrotoxicity has limited its clinical use. The compound has been compared with imidocarb dihydrochloride as an anaplasmacide. Its antibacterial activity has been investigated in research settings. |
| Enzyme Assay |
Antibacterial activity is assessed using standard broth microdilution or agar diffusion methods to determine minimum inhibitory concentrations (MICs) against Gram-positive bacteria. Anaplasmacidal activity is assessed in animal models of Anaplasma marginale infection. Protein synthesis inhibition is assessed using in vitro translation assays with bacterial ribosomes.
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| Cell Assay |
Cellular activity is evaluated in bacterial cultures (Gram-positive bacteria) and in Anaplasma-infected cells. Bacteria are treated with gloxazone at various concentrations and bacterial growth is measured by optical density or colony counting. Protein synthesis inhibition is assessed by measuring the incorporation of radiolabeled amino acids into bacterial proteins. Anaplasma infection is assessed by measuring parasitemia in infected animals.
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| Animal Protocol |
In vivo efficacy is studied in cattle infected with Anaplasma marginale. Gloxazone is administered intravenously at 5 mg/kg. Parasitemia is measured to assess efficacy. In toxicology studies, gloxazone is administered orally to rats at 0.1-3 mg/kg/day to assess nephrotoxicity. Renal histology and biochemical markers of kidney function (e.g., BUN, creatinine) are assessed.
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| ADME/Pharmacokinetics |
Gloxazone has a molecular formula of C8H16N6OS2 and a molecular weight of 276.38 g/mol. CAS Number: 2507-91-7. Appearance: Solid. Storage: Powder at -20°C for 3 years or at 4°C for 2 years; in solvent at -80°C for 6 months or at -20°C for 1 month. The compound is a thiosemicarbazone derivative.
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| Toxicity/Toxicokinetics |
Safety data for gloxazone indicate it is a toxic compound. It causes renal papillary necrosis and nephrotoxicity in rats at oral doses of 0.1-3 mg/kg/day. The compound should be handled with extreme caution using appropriate personal protective equipment and in a fume hood. Avoid inhalation, ingestion, and skin contact. The compound is for research use only and not for human therapeutic applications. Veterinary use is limited due to its toxicity.
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| References |
[1]. McHardy N, et al. Comparison of gloxazone, an effective but toxic anaplasmacide, with imidocarb dihydrochloride. Res Vet Sci. 1980 Sep;29(2):198-202.
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| Additional Infomation |
See also: Gloxazone (Note moved to).
Gloxazone is a research tool compound and veterinary drug for studying bacterial and parasitic infections. It is not approved for human use. The compound is an effective anaplasmacide but its use is limited by nephrotoxicity. Gloxazone has been investigated for activity against Gram-positive bacteria by inhibiting protein synthesis. It is a thiosemicarbazone derivative with antibacterial and antiparasitic activity. The compound is used in research to study bacterial protein synthesis, antibiotic resistance, and the pharmacology of thiosemicarbazones. |
| Molecular Formula |
C8H16N6OS2
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|---|---|
| Molecular Weight |
276.38
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| Exact Mass |
276.083
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| Elemental Analysis |
C, 34.77; H, 5.84; N, 30.41; O, 5.79; S, 23.20
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| CAS # |
2507-91-7
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| PubChem CID |
9571200
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| Appearance |
Solid powder
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| Density |
1.41g/cm3
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| Boiling Point |
419.7ºC at 760mmHg
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| Flash Point |
207.6ºC
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| Vapour Pressure |
2.97E-07mmHg at 25°C
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| Index of Refraction |
1.645
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| LogP |
1.602
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
17
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| Complexity |
330
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OC(/C(=N/NC(=S)N)/C=N/NC(=S)N)C)C
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| InChi Key |
ARIFZLJIERKKEL-RYYWOMKVSA-N
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| InChi Code |
InChI=1S/C8H16N6OS2/c1-3-15-5(2)6(12-14-8(10)17)4-11-13-7(9)16/h4-5H,3H2,1-2H3,(H3,9,13,16)(H3,10,14,17)/b11-4+,12-6+
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| Chemical Name |
[(E)-[(1E)-1-(carbamothioylhydrazinylidene)-3-ethoxybutan-2-ylidene]amino]thiourea
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| Synonyms |
BW 356C61; BW 356-C-61; Gloxazone
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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 |
| 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 (~452.28 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6182 mL | 18.0910 mL | 36.1821 mL | |
| 5 mM | 0.7236 mL | 3.6182 mL | 7.2364 mL | |
| 10 mM | 0.3618 mL | 1.8091 mL | 3.6182 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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