Absorption, Distribution and Excretion
When kanamycin was administered subcutaneously to rabbits at a dose of 100 mg/kg, the bactericide disappeared from the bloodstream within 8 hours, with 96% of the injected material excreted in the urine within 8 hours. The highest concentration of kanamycin in the urine (43 mg/mL) was observed after 45 minutes. In mice, after oral administration of 100 mg/kg kanamycin, absorption was rapid, with 43% to 68% of the drug excreted in the urine within 6 hours. In humans, after intramuscular injection of 1.0 g kanamycin, approximately 63% of the bactericide was excreted unchanged in the urine within 8 hours. Metabolic studies in rats showed that the average radioactive recovery rate after 168 hours of exposure was 91% to 97%, with the majority of the dose excreted in feces (81.9% to 93.9%) and urine (1.26% to 3.07%) within 48 hours. The highest plasma concentrations of kanamycin in both male and female rats occurred approximately 1 hour after a single low- or high-dose administration. Following a single administration of low or high doses of kanamycin, kanamycin accumulates in the kidneys, bladder, and lymph nodes more readily than in the blood within 1 to 6 hours, but is almost undetectable in these tissues after 168 hours. Absorption and metabolism of kanamycin in rats are limited (less than 5% of the dose) and are unaffected by sex, dose level, or duration of administration. The parent compound is the major component detected in urine, feces, liver, kidneys, and plasma. The metabolite kanamycin diglycosamine is present in low amounts (less than 1% of the dose) in urine, liver, kidneys, and plasma, but is undetectable in feces. Kanamycin is primarily excreted in feces (88% to 95%), indicating low absorption. Kanamycin is not excreted via bile (no enterohepatic circulation occurs). Metabolism/Metabolites: In tomato metabolism studies, the metabolite profiles of tomato fruits and leaves are similar. …The main metabolic pathways of kanamycin in plants include conjugation of the parent compound, conversion to kanamycin acid, and subsequent conjugation of kanamycin acid. The conversion of kanamycin to 2-N-acetylkanamycin and kanamycin diamine is considered a minor metabolic pathway. The parent compound (kasugamycin itself) was the major identified component in all samples across all collection time periods. In rat metabolic studies, the mean radioactive recovery rate at 168 hours post-exposure was 91% to 97%, with the majority of the dose recovered via feces (81.9% to 93.9%) and urine (1.26% to 3.07%) within 48 hours. …Absorption and metabolism of ksugamycin in rats are limited (less than 5% of the dose) and are not affected by sex, dose level, or duration of administration. The parent compound is the major identified component in urine, feces, liver, kidney, and plasma. A small amount (less than 1% of the dose) of the metabolite ksugamycin diamine was detected in urine, liver, kidney, and plasma, but not in feces.

Toxicity Data
LC50 (Rat) > 2,400 mg/m³/4h

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Non-human Toxicity Values LD50 (Mice, Dermal) > 10 g/kg
LD50 (Mice, Oral) > 5000 mg/kg
LD50 (Rat, Oral) > 11,400 mg/kg
LD50 (Rat, Oral) > 5000 mg/kg / Kasugamycin hydrochloride hydrate, data from tables /
For more complete non-human toxicity data for kasugamycin (8 types), please visit the HSDB record page.

[1]. Simultaneous determination of kasugamycin and validamycin-A residues in cereals by consecutive solid-phase extraction combined with liquid chromatography-tandem mass spectrometry. Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2018 Mar;35(3):487-497. ".

Kasugamycin is an aminocyclic glycoside isolated from Streptomyces kasugaensis, possessing antibacterial and fungicidal activity. It functions as a bacterial metabolite, protein synthesis inhibitor, and antifungal pesticide. It is an aminocyclic glycoside, aminoglycoside antibiotic, monosaccharide derivative, carboxymidine compound, and antibiotic fungicide. Kasugamycin has been reported to exist in Streptomyces celluloflavus and Streptomyces kasugaensis, and relevant data exist. Mechanism of Action: In cell-free systems, ksugamycin significantly inhibits protein synthesis in Pyricularia oryzae and Pseudomonas fluorescens, but its inhibitory effect is much weaker in rat liver formulations. This antibiotic has been shown to interfere with the binding of aminoacyl-tRNA to the 30S ribosomal subunit of E. coli…Kanamycin inhibits Phytophthora oryzae in acidic (pH=5) medium but has no inhibitory effect in neutral medium. …Kanamycin affects the accuracy of in vitro translation. The drug reduces the histidine-to-alanine incorporation in the MS2 phage coat protein, even though the MS2 gene does not contain a histidine codon. The antibiotic inhibits the reading of the MS2 coat cistrans. …Kanamycin concentrations do not inhibit coat protein biosynthesis. The kanamycin-resistant mutant (ksgA) lacking two adjacent adenosine dimethylation in 16S ribosomal RNA exhibits increased leakage of nonsense and frameshift mutations (in the absence of antibiotics).

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Therapeutic Use
Kanamycin…is effective against Pseudomonas, Erwinia, Xanthomonas, and Corynebacterium bacteria.
Based on its extremely low toxicity, kanamycin has been tested and proven effective against human Pseudomonas aeruginosa urinary tract infections.

C14-H25-N3-O9

379.42

379.159

6980-18-3

78822-08-9 (sulfate);6980-18-3;

65174

Typically exists as solid at room temperature

2.0±0.1 g/cm3

585.9±60.0 °C at 760 mmHg

203ºC (dec)

308.2±32.9 °C

0.0±3.7 mmHg at 25°C

1.738

-2.06

8

11

4

26

532

8

O=C(O)C(N[C@@H]1[C@@H](C)O[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]2O)[C@@H](N)C1)=N

PVTHJAPFENJVNC-UQTMRZPGSA-N

InChI=1S/C14H25N3O9/c1-3-5(17-12(16)13(23)24)2-4(15)14(25-3)26-11-9(21)7(19)6(18)8(20)10(11)22/h3-11,14,18-22H,2,15H2,1H3,(H2,16,17)(H,23,24)/t3-,4+,5+,6?,7+,8+,9-,10+,11?,14-/m1/s1

2-amino-2-[(2R,3S,5S,6R)-5-amino-2-methyl-6-[(2S,3S,5S,6R)-2,3,4,5,6-pentahydroxycyclohexyl]oxyoxan-3-yl]iminoacetic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

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

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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