| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Protein synthesis in cells and Escherichia coli extracts is specifically inhibited by streptomycin. E is quickly and reversibly inhibited by spectinomycin (50 μg/mL). Coli growth and the prompt blocking of the incorporation of amino acids [1]. Peptide synthesis stimulated by endogenous messenger RNA or MS-2 phage RNA is inhibited by spectinomycin (1 μg/mL or 3 μM), with a maximum inhibition rate of 70–80% in E. extracts from Coli [1]. Spectinomycin inhibits elongation factor G's binding to the ribosome, 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 spectinomycin [2]. Due to its dependence on pH variations and Mg2+ concentration, spezinominosinomycin shows inhibition of splicing, which may indicate electrostatic interactions with intronic RNA [3].
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|---|---|
| ln Vivo |
It has been demonstrated that in healthy chicks, permetinomycin (20 mg/kg; IM; 20-100 mg/kg; 9 days) is safe [4]. The majority of specinomycin (10 mg/kg; intravenous injection; single dose) is excreted by the kidneys, with around 55% of it leaving the urine unaltered [5]. Spectrinomycin pharmacokinetics in rats [5] Specification C0 μg/mL AUC0-∞ (μg^h/mL) Vd (liters per kilogram) CL (liters/hour/kg) MRT (hour) T1/2α (hours) T1 /β (h) T1/2γ (hour) Fe CLrenal (kg/h/L) Inratio Analysis that is not compartmentalized 1.00 44.3 16.8 0.756 0.602 0.757 / / / 0.553 0.359 Three-section model 37.8 15.7 0.7471.11 / 0.2377 0.754 19.5 //
|
| 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 |
Absorption, Distribution and Excretion
Rapidly and almost completely absorbed after intramuscular injection. Biological Half-Life 1 to 3 hours in patients with normal renal function and 10 to 30 hours in patients with impaired renal function with a creatinine clearance < 20 mL per minute. |
| Toxicity/Toxicokinetics |
Protein Binding
Not significant |
| References | |
| Additional Infomation |
Spectinomycin is a pyranobenzodioxin and antibiotic that is active against gram-negative bacteria and used (as its dihydrochloride pentahydrate) to treat gonorrhea. It is produced by the bacterium Streptomyces spectabilis. It has a role as an antimicrobial agent, a bacterial metabolite and an antibacterial drug. It is a cyclic hemiketal, a cyclic acetal, a cyclic ketone, a secondary amino compound, a pyranobenzodioxin and a secondary alcohol. It is a conjugate base of a spectinomycin(2+) and a spectinomycin(1+).
An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea. Spectinomycin has been reported in Streptomyces, Streptomyces netropsis, and other organisms with data available. Spectinomycin Hydrochloride is the hydrochloride salt form of spectinomycin, an aminocyclitol antibiotic derived from Streptomyces spectabilis with antibacterial property. Spectinomycin hydrochloride binds to the bacterial 30S ribosomal subunit, thereby inhibiting peptide elongation and protein synthesis, consequently leading to bacterial cell death. Spectinomycin is an aminocyclitol aminoglycoside antibiotic derived from Streptomyces spectabilis with bacteriostatic activity. Spectinomycin binds to the bacterial 30S ribosomal subunit. As a result, this agent interferes with the initiation of protein synthesis and with proper protein elongation. This eventually leads to bacterial cell death. An antibiotic produced by Streptomyces spectabilis. It is active against gram-negative bacteria and used for the treatment of gonorrhea. Drug Indication For use in the treatment of acute gonorrheal urethritis and proctitis in the male and acute gonorrheal cervicitis and proctitis in the female when due to susceptible strains of Neisseria gonorrhoeae. Mechanism of Action Spectinomycin is an inhibitor of protein synthesis in the bacterial cell; the site of action is the 30S ribosomal subunit. It is bactericidal in its action. |
| Molecular Weight |
332.35
|
|---|---|
| Exact Mass |
332.158
|
| CAS # |
1695-77-8
|
| Related CAS # |
Spectinomycin dihydrochloride;21736-83-4;Spectinomycin dihydrochloride pentahydrate;22189-32-8
|
| PubChem CID |
15541
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-3.1
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
23
|
| Complexity |
478
|
| 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
|
| InChi Key |
UNFWWIHTNXNPBV-WXKVUWSESA-N
|
| 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
|
| 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
|
| 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 |
| 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) |
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
|
|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (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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