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| Other Sizes |
| Targets |
Spectinomycin binds to the bacterial 30S ribosomal subunit, specifically near helix 34 of the 16S rRNA. By binding to this site, it prevents elongation factor G-mediated translocation of peptidyl-tRNA from the ribosomal A-site to the P-site, thereby inhibiting protein translation. Resistance mutations to spectinomycin align closely with those conferring streptomycin resistance, confirming the 30S subunit as its primary target. It also interacts with residues G1064 and C1192 in 16S rRNA.
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| ln Vitro |
Protein synthesis in cells and E is specifically inhibited by streptinomycin dihydrochloride pentahydrate. Spectinomycin dihydrochloride pentahydrate (50 μg/mL) inhibits E. coli extracts quickly and reversibly. coli development and prevents the incorporation of amino acids right away [1]. With a maximal inhibition rate of 70-80% in E, streptinomycin diHClide penta Hydro (1 μg/mL or 3 μM) inhibits peptide synthesis guided by endogenous messenger RNA or MS-2 phage RNA. Coli extracts [1]. By preventing elongation factor G from attaching to the ribosome, streptinomycin diHCl pentahydrate prevents the translocation of peptidyl tRNA from the A site to the P site [2]. Residues G1064 and 01192 in 16S rRNA are particularly interacting with and may be rendered inactive by streptinomycin diHClide penta Hydro [2]. Due to its dependence on pH variations and Mg2+ content, streptinomycin diHCl pentahydrate shows splicing inhibition, which may indicate electrostatic interactions with intronic RNA [3].
In vitro, Spectinomycin (50 μg/mL) rapidly and reversibly inhibits the growth of Escherichia coli B and immediately slows amino acid incorporation while RNA synthesis continues. In E. coli extracts, it inhibits peptide synthesis guided by endogenous messenger RNA or MS-2 phage RNA, with a maximum inhibition rate of 70-80%. It also shows splicing inhibition dependent on pH variations and Mg2+ content, suggesting electrostatic interactions with intronic RNA. |
| ln Vivo |
It has been demonstrated that in healthy chicks, spectinomycin dihydrochloride pentahydrate (20 mg/kg; IM; 20-100 mg/kg; 9 days) is safe [4]. The majority of the dose of specinomycin dihydrochloride pentahydrate (10 mg/kg; intravenous injection; single dose) is excreted unchanged into the urine by the kidneys [5]. Rat spectinomycin pentahydrate pharmacokinetics [5]: parameter C0 (μg/mL) AUC0-∞ (μg·h/mL) Vd (L/kg) CL (L/h/kg) MRT (h) T1/2α (h) T1/2β (h) fe CLrenal (L/h/kg) Eratio Non-compartmental analysis 44.3 16.8 0.756 0.602 0.757 / / / 0.553 0.359 1.00 Three-compartment model 37.8 15.7 0.747 0.649 1.11 / 0.2 37 0.754 19.5 //
In vivo, Spectinomycin has been shown to be safe in healthy chicks at doses of 20 mg/kg administered intramuscularly over 9 days, with mild toxicity observed at 60 mg/kg. In male Sprague-Dawley rats, following intravenous administration of 10 mg/kg, approximately 55% of the drug was excreted unchanged in the urine, with a peak plasma concentration of 37.8 μg/mL and a systemic exposure (AUC0-∞) of 15.7 μg·h/mL. |
| Enzyme Assay |
In vitro enzyme assays for Spectinomycin typically involve measuring its binding to the 30S ribosomal subunit or its inhibition of td intron RNA splicing. The compound binds near helix 34 of the 16S rRNA, preventing elongation factor G-mediated translocation. Its noncompetitive inhibition of td intron RNA (Ki = 7.2 mM) can be assessed using splicing assays, which are dependent on pH and Mg2+ concentration. These assays confirm its mechanism of action as a ribosomal inhibitor.
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| Cell Assay |
In vitro cellular assays for Spectinomycin typically involve determining the minimum inhibitory concentration (MIC) against a panel of bacterial strains using the broth microdilution method. In exponentially growing E. coli cultures, Spectinomycin at 50 μg/mL rapidly and reversibly inhibits growth. It also inhibits amino acid incorporation in E. coli extracts with a maximum inhibition rate of 70-80% at 1 μg/mL or 3 μM. Time-kill kinetics assays may also be performed to evaluate its bactericidal activity.
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| Animal Protocol |
Animal/Disease Models: Arbor Acres plus broiler chicken (15 days old) [4]
Doses: 20 mg/kg, 60 mg/kg, 100 mg/kg Route of Administration: intramuscularinjection (chest muscle) ; 9-day Experimental Results: complete blood count, biochemical parameters, histopathology, clinical signs, weight gain and feed conversion ratio (FCR) demonstrated biosafety of 20 mg/kg. Produces mild toxicity at 60 mg/kg. In vivo animal models for Spectinomycin include healthy Arbor Acres plus broiler chickens (15 days old) administered intramuscularly at doses of 20, 60, and 100 mg/kg over 9 days to assess biosafety. Complete blood count, biochemical parameters, histopathology, clinical signs, weight gain, and feed conversion ratio (FCR) demonstrated biosafety at 20 mg/kg, with mild toxicity at 60 mg/kg. In male Sprague-Dawley rats, IV administration of 10 mg/kg was used for pharmacokinetic studies. |
| ADME/Pharmacokinetics |
In male Sprague-Dawley rats (200-225 g), following intravenous administration of 10 mg/kg, Spectinomycin showed a peak plasma concentration of 37.8 μg/mL and a systemic exposure (AUC0-∞) of 15.7 μg·h/mL. Approximately 55% of the drug was excreted unchanged in the urine. In healthy chicks, intramuscular administration of 20 mg/kg over 9 days demonstrated biosafety, while 60 mg/kg produced mild toxicity. The compound is primarily eliminated renally.
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| Toxicity/Toxicokinetics |
Spectinomycin HCl hydrate has a well-established safety profile in veterinary applications. In healthy chicks, intramuscular administration of 20 mg/kg over 9 days demonstrated biosafety, while 60 mg/kg produced mild toxicity. It is generally well-tolerated at therapeutic doses. As with other aminocyclitol antibiotics, potential adverse effects may include nephrotoxicity and ototoxicity, though these are less commonly associated with spectinomycin compared to other aminoglycosides.
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| References |
[1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.
[2]. Brink MF, et al. Spectinomycin interacts specifically with the residues G1064 and C1192 in 16S rRNA, thereby potentially freezing this molecule into an inactive conformation. Nucleic Acids Res. 1994 Feb 11;22(3):325-31. [3]. Park IK, et al. Spectinomycin inhibits the self-splicing of the group 1 intron RNA. Biochem Biophys Res Commun. 2000 Mar 16;269(2):574-9. [4]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6. [5]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209. |
| Additional Infomation |
Spectinomycin hydrochloride hydrate is the pentahydrate form of spectinomycin hydrochloride. It is an antibiotic effective against Gram-negative bacteria and used to treat gonorrhea. It has antibacterial activity and is an antimicrobial drug. It is both a hydrate and a hydrochloride salt containing spectinomycin (2+).
Spectinomycin hydrochloride is the hydrochloride form of spectinomycin, an aminocyclic alcohol antibiotic derived from Streptomyces spectabilis, which has antibacterial activity. Spectinomycin hydrochloride binds to the bacterial 30S ribosomal subunit, thereby inhibiting peptide chain elongation and protein synthesis, ultimately leading to bacterial death. Anhydrous spectinomycin hydrochloride is the anhydrous hydrochloride form of spectinomycin, an aminocyclic alcohol aminoglycoside antibiotic derived from Streptomyces spectabilis, which has antibacterial activity. Spectinomycin binds to the bacterial 30S ribosomal subunit. Therefore, the drug interferes with the initiation of protein synthesis and normal protein elongation, ultimately leading to bacterial cell death. Spectinomycin is an antibiotic produced by Streptomyces spectabilis. It is effective against Gram-negative bacteria and is used to treat gonorrhea. See also: spectinomycin (containing the active fraction); spectinomycin pentahydrate dihydrochloride (note moved to); spectinomycin pentahydrate hydrochloride (note moved to). Spectinomycin HCl hydrate (CAS# 22189-32-8) is an aminocyclitol antibiotic derived from Streptomyces spectabilis. It is active against a broad range of Gram-positive and Gram-negative bacteria and is used in biomedical research to study ribosomal function and bacterial resistance mechanisms. The compound is a dihydrochloride pentahydrate salt with a molecular weight of 495.4 and is soluble in water (≥49.5 mg/mL), ethanol (≥3.61 mg/mL), and DMSO (≥92 mg/mL). It is for research use only and not for human use. |
| Molecular Formula |
C14H24N2O7
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|---|---|
| Molecular Weight |
332.3496
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| Exact Mass |
494.164
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| CAS # |
22189-32-8
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| Related CAS # |
Spectinomycin dihydrochloride;21736-83-4;Spectinomycin;1695-77-8
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| PubChem CID |
30971
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| Appearance |
White to off-white solid powder
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| Boiling Point |
583.1ºC at 760 mmHg
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| Melting Point |
205-207° (dec)
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| Flash Point |
306.4ºC
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| Vapour Pressure |
5.05E-16mmHg at 25°C
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| LogP |
-3.1
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
478
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| Defined Atom Stereocenter Count |
9
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| SMILES |
O1[C@]2(C(C([H])([H])[C@@]([H])(C([H])([H])[H])O[C@@]2([H])O[C@]2([H])[C@]([H])([C@@]([H])([C@@]([H])([C@@]([H])([C@@]12[H])N([H])C([H])([H])[H])O[H])N([H])C([H])([H])[H])O[H])=O)O[H]
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| InChi Key |
UNFWWIHTNXNPBV-WXKVUWSESA-N
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| InChi Code |
InChI=1S/C14H24N2O7/c1-5-4-6(17)14(20)13(21-5)22-12-10(19)7(15-2)9(18)8(16-3)11(12)23-14/h5,7-13,15-16,18-20H,4H2,1-3H3/t5-,7-,8+,9+,10+,11-,12-,13+,14+/m1/s1
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| Chemical Name |
(1R,3S,5R,8R,10R,11S,12S,13R,14S)-8,12,14-trihydroxy-5-methyl-11,13-bis(methylamino)-2,4,9-trioxatricyclo[8.4.0.03,8]tetradecan-7-one
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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 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)
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| Solubility (In Vitro) |
H2O : ~62.5 mg/mL (~126.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (100.94 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 | 3.0089 mL | 15.0444 mL | 30.0888 mL | |
| 5 mM | 0.6018 mL | 3.0089 mL | 6.0178 mL | |
| 10 mM | 0.3009 mL | 1.5044 mL | 3.0089 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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