| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Aminoglycoside
Isepamicin sulfate targets the bacterial 30S ribosomal subunit, similar to other aminoglycosides. By binding to the 30S ribosomal subunit, it results in an inability to read mRNA, ultimately producing a faulty or nonexistent protein. This inhibition of bacterial protein synthesis leads to the misreading of genetic information and ultimately bacterial cell death. The compound is notably effective against bacteria expressing AAC(6')-I type acetyltransferase. |
|---|---|
| ln Vitro |
Isepamicin sulfate demonstrates potent in vitro antibacterial activity against a spectrum of Gram-positive and Gram-negative bacteria, including Enterobacteriaceae and Staphylococci. It inhibits bacterial protein synthesis by targeting the bacterial 30S ribosomal subunit. The compound's stability against aminoglycoside-modifying enzymes contributes to its effectiveness against drug-resistant pathogens. It has considerable antimicrobial activity against some Gram-negative non-fermenting bacteria that are highly resistant to antibiotics.
|
| ln Vivo |
In vivo activity of isepamicin sulfate has been suggested by its broad-spectrum antibacterial properties. The compound is used in research on bacterial infections and antibiotic resistance. It has been shown to inhibit writhing reactions induced by acetic acid, regulate vascular blood flow and blood pressure, and inhibit spontaneous uterine movements. Further in vivo studies are needed to fully characterize its therapeutic potential.
|
| Enzyme Assay |
In vitro enzyme assays for isepamicin sulfate are not typically performed, as the compound's mechanism involves binding to the ribosomal subunit rather than enzyme inhibition. Its antibacterial activity is assessed using standard broth microdilution or agar diffusion methods to determine minimum inhibitory concentrations (MICs) against bacterial isolates.
|
| Cell Assay |
In vitro cellular assays for isepamicin sulfate involve culturing bacterial cells in the presence of varying concentrations of the compound. Antibacterial activity is assessed by measuring inhibition of growth using optical density measurements or colony counting. The compound's effectiveness against drug-resistant bacteria can be evaluated using clinical isolates expressing aminoglycoside-modifying enzymes.
|
| Animal Protocol |
In vivo animal experiments for isepamicin sulfate are not extensively documented. If used in animal models of bacterial infection, typical protocols would involve administering the compound to infected animals and evaluating efficacy by measuring bacterial load in tissues or clinical outcomes. Further studies are needed to characterize its in vivo activity.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for isepamicin sulfate are limited. As an aminoglycoside antibiotic, its absorption, distribution, metabolism, and excretion properties would be similar to other members of this class. The compound is typically administered parenterally. Its stability against aminoglycoside-modifying enzymes contributes to its pharmacokinetic profile.
|
| Toxicity/Toxicokinetics |
Toxicological data for isepamicin sulfate are consistent with those of other aminoglycoside antibiotics. Aminoglycosides can cause nephrotoxicity and ototoxicity at high doses. The compound should be handled with appropriate safety precautions in research settings. It is intended for research use only.
|
| References |
[1]. Samonis G, et al. Antimicrobial susceptibility of non-fermenting Gram-negative isolates to isepamicin in a region with high antibiotic resistance. Eur J Clin Microbiol Infect Dis. 2012 Nov;31(11):3191-8.
|
| Additional Infomation |
See also: Isepamicin sulfate (note moved to).
Isepamicin sulfate (Isepamicin sulfate; Sch 21420 sulfate) (CAS#: 67814-76-0) has the molecular formula C22H43N5O18S (for the sulfate salt) and a molecular weight of approximately 719.67. It is an aminoglycoside antibiotic derived from gentamicin B that targets the bacterial 30S ribosomal subunit. The compound is characterized by its stability against aminoglycoside-modifying enzymes. |
| Molecular Formula |
C22H43N5O12.XH2SO4
|
|---|---|
| Molecular Weight |
665.6657
|
| Exact Mass |
665.243
|
| CAS # |
67814-76-0
|
| Related CAS # |
Isepamicin;58152-03-7
|
| PubChem CID |
171883
|
| Appearance |
White to off-white solid powder
|
| Density |
1.53g/cm3
|
| Boiling Point |
926.8ºC at 760mmHg
|
| Flash Point |
514.3ºC
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
20
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
44
|
| Complexity |
880
|
| Defined Atom Stereocenter Count |
15
|
| SMILES |
S(=O)(=O)([O-])[O-].O([C@]1([H])[C@@]([H])([C@]([H])([C@](C([H])([H])[H])(C([H])([H])O1)O[H])N([H])C([H])([H])[H])O[H])[C@]1([H])[C@]([H])([C@@]([H])([C@]([H])(C([H])([H])[C@@]1([H])N([H])C([C@]([H])(C([H])([H])N([H])[H])O[H])=O)N([H])[H])O[C@]1([H])[C@@]([H])([C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])N([H])[H])O1)O[H])O[H])O[H])O[H]
|
| InChi Key |
DDXRHRXGIWOVDQ-MGAUJLSLSA-L
|
| InChi Code |
InChI=1S/C22H43N5O12.H2O4S/c1-22(35)6-36-20(15(33)18(22)26-2)39-17-8(27-19(34)9(28)4-23)3-7(25)16(14(17)32)38-21-13(31)12(30)11(29)10(5-24)37-21;1-5(2,3)4/h7-18,20-21,26,28-33,35H,3-6,23-25H2,1-2H3,(H,27,34);(H2,1,2,3,4)/p-2/t7-,8+,9-,10+,11+,12-,13+,14-,15+,16+,17-,18+,20+,21+,22-;/m0./s1
|
| Chemical Name |
(2S)-3-amino-N-[(1R,2S,3S,4R,5S)-5-amino-4-[(2R,3R,4S,5S,6R)-6-(aminomethyl)-3,4,5-trihydroxyoxan-2-yl]oxy-2-[(2R,3R,4R,5R)-3,5-dihydroxy-5-methyl-4-(methylamino)oxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxypropanamide;sulfate
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : 125 mg/mL
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5022 mL | 7.5112 mL | 15.0225 mL | |
| 5 mM | 0.3004 mL | 1.5022 mL | 3.0045 mL | |
| 10 mM | 0.1502 mL | 0.7511 mL | 1.5022 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
