Spectinomycin (dihydrochloride) [21736-83-4]

Référence HY-B0438-5g

Conditionnement : 5g

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Spectinomycin dihydrochloride is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM-.

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Spectinomycin dihydrochloride Chemical Structure

Spectinomycin dihydrochloride Chemical Structure

CAS No. : 21736-83-4

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Based on 3 publication(s) in Google Scholar

Other Forms of Spectinomycin dihydrochloride:

  • Spectinomycin dihydrochloride pentahydrate In-stock
  • Spectinomycin Obtenir un devis

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Description

Spectinomycin dihydrochloride is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM[1]-[5].

IC50 & Target

bacterial ribosomal subunit[5]

In Vitro

Spectinomycin dihydrochloride selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin dihydrochloride (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately[1].
Spectinomycin dihydrochloride (1 μg/mL or 3 μM) inhibits polypeptide synthesis directed either by endogenous messenger RNA or by MS-2 bacteriophage RNA, with maximum inhibition of 70-80% in extracts of Escherichia coli[1][1].
Spectinomycin dihydrochloride blocks the translocation of peptidyl-tRNAs from A-site to P-site by inhibiting the binding of elongation factor G to the ribosome[2].
Spectinomycin dihydrochloride interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2].
Spectinomycin dihydrochloride exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Spectinomycin dihydrochloride (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4].
Spectinomycin dihydrochloride (10 mg/kg; i.v.; single dose) has the major elimination pathway by renal excretion, approximately 55% is excreted into the urine in unchanged form[5].
Pharmacokinetics of Spectinomycin dihydrochloride in Rat[5]

Parameter C0 (μg/mL) AUC0-∞ (μg•h/mL) Vd (L/kg) CL (L/h/kg) MRT (h) T1/2α (h) T1/2β (h) T1/2γ (h) fe CLrenal (L/h/kg) Eratio
Non atrioventricular 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 / /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Arbor Acres plus broiler chicks (15-day-old)[4]
Dosage: 20 mg/kg, 60 mg/kg, 100 mg/kg
Administration: Intramuscular injection (chest muscles); 9 days
Result: Showed biosecurity of 20 mg/kg by complete blood count, biochemical parameters, histopathological, clinical signs, body weight gain, and feed conversion ratio (FCR).
Resulted minor toxicity of 60 mg/kg.
Masse moléculaire

405.27

Formule

C14H26Cl2N2O7

CAS No.

21736-83-4

Appearance

Solid

Color

White to off-white

SMILES

CN[C@@H]([C@H]([C@@H](NC)[C@@H]1O)O)[C@]2(02)[C@]1(02)O[C@@](O[C@H](C)C3)(02)[C@](O)(C3=O)O2.Cl.Cl

Structure Classification
  • Antibiotics
  • Disease Research
  • Antibacterial
  • Antibiotics
  • Other Antibiotics
  • Antibiotics
  • Mammalian Cell Culture
  • Antibiotics
  • Resistance Selection
Initial Source
  • Microorganisms

bacterium Streptomyces spectabilis

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

H2O : ≥ 100 mg/mL (246.75 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (123.37 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Pureté et documentation

Purity: 99.61%

Références
  • [1]. Davies J, et al. Inhibition of protein synthesis by spectinomycin. Science. 1965 Sep 3;149(3688):1096-8.  [Content Brief]

    [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.  [Content Brief]

    [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.  [Content Brief]

    [4]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209.  [Content Brief]

    [5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.  [Content Brief]

  • [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]. Khan EA, et al. Safety evaluation study of lincomycin and spectinomycin hydrochloride intramuscular injection in chickens. Toxicol Rep. 2022 Jan 29;9:204-209.

    [5]. Madhura DB, et al. Pharmacokinetic profile of spectinomycin in rats. Pharmazie. 2013 Aug;68(8):675-6.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.4675 mL 12.3375 mL 24.6749 mL 61.6873 mL
5 mM 0.4935 mL 2.4675 mL 4.9350 mL 12.3375 mL
10 mM 0.2467 mL 1.2337 mL 2.4675 mL 6.1687 mL
15 mM 0.1645 mL 0.8225 mL 1.6450 mL 4.1125 mL
20 mM 0.1234 mL 0.6169 mL 1.2337 mL 3.0844 mL
25 mM 0.0987 mL 0.4935 mL 0.9870 mL 2.4675 mL
30 mM 0.0822 mL 0.4112 mL 0.8225 mL 2.0562 mL
40 mM 0.0617 mL 0.3084 mL 0.6169 mL 1.5422 mL
50 mM 0.0493 mL 0.2467 mL 0.4935 mL 1.2337 mL
60 mM 0.0411 mL 0.2056 mL 0.4112 mL 1.0281 mL
80 mM 0.0308 mL 0.1542 mL 0.3084 mL 0.7711 mL
100 mM 0.0247 mL 0.1234 mL 0.2467 mL 0.6169 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Spectinomycin dihydrochloride Related Classifications

Help & FAQs

Keywords:

Spectinomycin21736-83-4BacterialAntibioticbiosecurityaminocyclitolbroad-spectrumgram-positivegram-negativeorganismbacterial ribosomeEscherichia coliamino acid incorporationMS-2 bacteriophagepeptidyl-tRNAelectrostatic interactionInhibitorinhibitorinhibit

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