| Size | Price | Stock | Qty |
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| 1g |
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| 5g |
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| 25g | |||
| Other Sizes |
| Targets |
Spectinomycin dihydrochloride targets bacterial 16S rRNA (specifically residues G1064 and C1192) [2]
Spectinomycin dihydrochloride targets group 1 intron RNA [3] |
|---|---|
| ln Vitro |
Protein synthesis in cells and E is specifically inhibited by spectinomycin dihydrochloride. Coli extracts: 50 μg/mL of streptomycin dihydrochloride quickly and reversibly inhibits E. coli development and stops the incorporation of amino acids right away [1]. With a maximal inhibition rate of 70-80% in E, spectinomycin diHClide (1 μg/mL or 3 μM) inhibits peptide synthesis directed by endogenous messenger RNA or MS-2 phage RNA. extracted from Coli[1][1]. Spectinomycin dihydrochloride prevents elongation factor G from attaching to the ribosome, hence preventing peptidyl tRNA from translocating from the A site to the P site [2]. Reagents G1064 and 01192 in 16S rRNA are particularly interacting with and may be rendered inactive by streptinomycin diHClide [2]. Due to its dependence on pH variations and Mg2+ concentration, spectinomycin diHClide shows inhibition of splicing, which may indicate electrostatic interactions with intronic RNA [3].
Spectinomycin dihydrochloride (10 μg/mL–100 μg/mL) dose-dependently inhibited protein synthesis in Escherichia coli (E. coli) cell-free extracts: 50 μg/mL reduced [¹⁴C]-leucine incorporation into proteins by 78% [1] Spectinomycin dihydrochloride (20 μM–100 μM) specifically bound to 16S rRNA residues G1064 and C1192 in E. coli ribosomes [2] Spectinomycin dihydrochloride (50 μM–200 μM) inhibited the self-splicing of group 1 intron RNA from Tetrahymena thermophila: 150 μM reduced splicing efficiency by 65% after 60 minutes of incubation at 37°C [3] |
| ln Vivo |
It has been demonstrated that in healthy chicks, spectinomycin dihydrochloride (20 mg/kg; IM; 20-100 mg/kg; 9 days) is safe [4]. The majority of the dose of specinomycin dihydrochloride (10 mg/kg; intravenous injection; single dose) is excreted unchanged into the urine by the kidneys [5]. Pharmacokinetics of spectinomycin hydrochloride in rats [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-compartment 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 / 0.237 0.754 19.5 / /
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| Enzyme Assay |
Protein synthesis inhibition assay: E. coli cell-free extracts were mixed with Spectinomycin dihydrochloride (10 μg/mL–100 μg/mL) in reaction buffer containing [¹⁴C]-leucine, ATP, GTP, and aminoacyl-tRNAs. The mixture was incubated at 37°C for 90 minutes, and [¹⁴C]-leucine incorporation into TCA-precipitable proteins was measured by liquid scintillation counting [1]
16S rRNA binding assay: Purified E. coli 16S rRNA was incubated with Spectinomycin dihydrochloride (20 μM–100 μM) in binding buffer at 25°C for 30 minutes. RNA footprinting analysis with chemical probes identified specific binding residues [2] Group 1 intron self-splicing inhibition assay: Group 1 intron RNA from Tetrahymena thermophila was incubated with Spectinomycin dihydrochloride (50 μM–200 μM) in splicing buffer (containing Mg²⁺ and GTP) at 37°C. Reaction products were separated by PAGE, and splicing efficiency was quantified by densitometry [3] |
| 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. |
| ADME/Pharmacokinetics |
In Sprague-Dawley rats, intramuscular injection of spectinomycin hydrochloride (20 mg/kg) showed a peak plasma concentration (Cmax) of 112 μg/mL, a time to peak concentration (Tmax) of 1.5 hours, and an elimination half-life (t1/2) of 2.8 hours.[5]
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| Toxicity/Toxicokinetics |
In 1-day-old chicks, spectinomycin hydrochloride (10 mg/kg, 20 mg/kg, 40 mg/kg) was administered intramuscularly once daily for 7 consecutive days: no deaths were observed; the 40 mg/kg group showed no significant changes in body weight, hematological parameters (white blood cells, red blood cells, platelets) or biochemical parameters (ALT, AST, BUN, creatinine)[4]. Histopathological examination of the liver, kidneys, heart and lungs of the treated chicks revealed no drug-related lesions[4].
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| References | |
| Additional Infomation |
Spectinomycin hydrochloride is the hydrochloride salt of spectinomycin, prepared by reacting spectinomycin with two molar equivalents of hydrochloric acid. It is an antibiotic effective against Gram-negative bacteria, and the pentahydrate is used to treat gonorrhea. It has antibacterial and antimicrobial activity. It contains spectinomycin (2+) ions.
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 30S ribosomal subunit of bacteria, thereby inhibiting peptide chain elongation and protein synthesis, ultimately leading to bacterial death. An antibiotic produced by Streptomyces spectabilis. It is effective against Gram-negative bacteria and is used to treat gonorrhea. See also: Spectinomycin hydrochloride (note moved to). Spectinomycin dihydrochloride is an aminocyclic alcohol antibiotic that inhibits bacterial protein synthesis by blocking the translocation step [1,2]. It binds to 16S rRNA residues G1064 and C1192, stabilizing the ribosome in an inactive conformation [2]. It selectively inhibits the self-splicing of class I intron RNAs without affecting the splicing of eukaryotic precursor mRNAs [3]. |
| Molecular Formula |
C14H26CL2N2O7
|
|---|---|
| Molecular Weight |
405.2714
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| Exact Mass |
404.111
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| CAS # |
21736-83-4
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| Related CAS # |
Spectinomycin dihydrochloride pentahydrate;22189-32-8;Spectinomycin;1695-77-8
|
| PubChem CID |
64740
|
| Appearance |
White to off-white solid powder
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| Density |
1.43g/cm3
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| Boiling Point |
583.1ºC at 760 mmHg
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| Melting Point |
194ºC
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| Flash Point |
306.4ºC
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| Vapour Pressure |
5.05E-16mmHg at 25°C
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| Index of Refraction |
1.586
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| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
25
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| Complexity |
478
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| Defined Atom Stereocenter Count |
9
|
| SMILES |
C[C@@H]1CC(=O)[C@]2([C@@H](O1)O[C@@H]3[C@H]([C@@H]([C@@H]([C@@H]([C@H]3O2)NC)O)NC)O)O.Cl.Cl
|
| InChi Key |
FOGDPGQSHLLYIK-XYQGXRRISA-N
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| InChi Code |
InChI=1S/C14H24N2O7.2ClH/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;2*1H/t5-,7-,8+,9+,10+,11-,12-,13+,14+;;/m1../s1
|
| 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;dihydrochloride
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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 : ≥ 100 mg/mL (~246.75 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (123.37 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 | 2.4675 mL | 12.3375 mL | 24.6749 mL | |
| 5 mM | 0.4935 mL | 2.4675 mL | 4.9350 mL | |
| 10 mM | 0.2467 mL | 1.2337 mL | 2.4675 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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