| Size | Price | |
|---|---|---|
| 500mg | ||
| Other Sizes |
| Targets |
The primary molecular target of Kasugamycin hydrochloride hydrate is the bacterial ribosome, specifically the 30S and 70S ribosomal subunits. The compound binds to the ribosome and inhibits protein synthesis. It mimics mRNA nucleotides to disrupt tRNA binding and inhibit canonical translation initiation. By binding to the 30S subunit, Kasugamycin prevents the proper initiation of translation, leading to the inhibition of bacterial protein synthesis and bacterial growth. The compound does not bind to the 50S subunit. Its selectivity for bacterial ribosomes makes it a useful antibiotic and research tool.
|
|---|---|
| ln Vitro |
In vitro studies demonstrate that Kasugamycin hydrochloride hydrate is an antibiotic that binds to 30S and 70S ribosomes but not to the 50S subunit. It inhibits bacterial protein synthesis by mimicking mRNA nucleotides to disrupt tRNA binding and inhibit canonical translation initiation. The compound has anti-infective activity. In bacterial cell cultures, Kasugamycin inhibits the growth of various bacterial strains. Its mechanism of action has been characterized using biochemical and structural studies. The compound is used as a selective agent in molecular biology to select for cells carrying resistance genes.
|
| ln Vivo |
In vivo studies of Kasugamycin hydrochloride hydrate have demonstrated its efficacy in animal models of bacterial infection. As an antibiotic, it is used to treat bacterial infections. The compound's efficacy and safety have been evaluated in preclinical studies. In vivo protocols typically involve administration of Kasugamycin via oral, subcutaneous, or intraperitoneal injection. Endpoints include assessment of bacterial load, survival, and histopathological examination. However, detailed in vivo protocols and efficacy data are not extensively reported in the public domain.
|
| Enzyme Assay |
For antibacterial susceptibility assays, Kasugamycin hydrochloride hydrate is tested against various bacterial strains using broth microdilution or agar dilution methods to determine the minimum inhibitory concentration (MIC). The compound is dissolved in water or appropriate buffer and serially diluted in growth medium. Bacterial cultures are added to the wells, and the plates are incubated at 37°C for 18-24 hours. The MIC is determined as the lowest concentration of the compound that inhibits visible bacterial growth. For mechanistic studies, bacterial ribosomes are isolated, and the binding of Kasugamycin to ribosomal subunits is assessed using radiolabeled or fluorescently labeled compound.
|
| Cell Assay |
For cellular studies, bacterial cells are cultured in appropriate medium and treated with Kasugamycin hydrochloride hydrate at varying concentrations (0.1-100 µg/mL). Bacterial growth is monitored by measuring optical density at 600 nm. For protein synthesis assays, bacterial cells are labeled with [³⁵S]-methionine or other labeled amino acids, and the incorporation of label into protein is measured. The inhibition of protein synthesis by Kasugamycin is assessed. For resistance studies, bacterial cells carrying resistance genes are tested for their susceptibility to Kasugamycin.
|
| Animal Protocol |
For in vivo efficacy studies, animal models of bacterial infection are used. Kasugamycin hydrochloride hydrate is formulated in vehicle and administered orally, subcutaneously, or intraperitoneally at doses determined from preliminary studies. Bacterial load is measured in tissues by colony counting. Survival is monitored. Histopathological examination of tissues is performed to assess infection and tissue damage. For pharmacokinetic studies, blood and tissue samples are collected at various time points for compound quantification by LC-MS.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Kasugamycin hydrochloride hydrate indicate that it is an aminoglycoside antibiotic with limited oral bioavailability. The compound is typically administered parenterally. It is distributed to various tissues and excreted renally. The compound's pharmacokinetic properties support its use as an antibiotic. However, detailed pharmacokinetic parameters are not extensively reported in the public domain.
|
| Toxicity/Toxicokinetics |
Toxicological data for Kasugamycin hydrochloride hydrate are limited. As an aminoglycoside antibiotic, the compound may have potential nephrotoxicity and ototoxicity, which are common side effects of this class of antibiotics. The compound's safety profile has been evaluated in preclinical studies. No acute toxicity, mutagenicity, or carcinogenicity data have been reported in the public domain. As with all research compounds, appropriate safety precautions should be taken when handling Kasugamycin hydrochloride hydrate.
|
| Additional Infomation |
Kasugamycin hydrochloride hydrate (CAS 200132-83-8), also known as Ksg hydrochloride hydrate, is an antibiotic that binds both the 30S and 70S ribosomes but not the 50S subunit. It has a molecular formula of C₁₄H₂₈ClN₃O₁₀ and a molecular weight of 433.84. The compound mimics mRNA nucleotides to disrupt tRNA binding and inhibit translation initiation. It has anti-infective activity. Kasugamycin is used in research to study bacterial translation and as a selective agent. It is strictly for research use only.
|
| Molecular Formula |
C14H25N3O9.HCL.H2O
|
|---|---|
| Molecular Weight |
433.83922
|
| Exact Mass |
433.146
|
| CAS # |
200132-83-8
|
| Related CAS # |
Kasugamycin hydrochloride;19408-46-9
|
| PubChem CID |
57369825
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
10
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
28
|
| Complexity |
532
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
OC(C(N[C@@H](C[C@@H]1N)[C@@H](C)O[C@]1([H])O[C@@H]2[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@H]2O)=N)=O.[H]Cl.O
|
| InChi Key |
URDOPMVCASNBEZ-VHRLMMNYSA-N
|
| InChi Code |
InChI=1S/C14H25N3O9.ClH.H2O/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);1H;1H2/t3-,4+,5+,6?,7+,8+,9-,10+,11?,14-;;/m1../s1
|
| Chemical Name |
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;hydrate;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~25 mg/mL (~57.62 mM)
DMSO : ~1.67 mg/mL (~3.85 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 8.33 mg/mL (19.20 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3050 mL | 11.5250 mL | 23.0500 mL | |
| 5 mM | 0.4610 mL | 2.3050 mL | 4.6100 mL | |
| 10 mM | 0.2305 mL | 1.1525 mL | 2.3050 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
