Spectinomycin (dihydrochloride pentahydrate)
CAS No. : 22189-32-8
(Synonyms: Spectinomycin (hydrochloride hydrate))
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| Cat. No. : | HY-B1828A |
| M.Wt: | 495.35 |
| Formula: | C14H36Cl2N2O12 |
| Purity: | >98 % |
| Solubility: | H2O : 62.5 mg/mL (ultrasonic) |
Spectinomycin dihydrochloride pentahydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride pentahydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride pentahydrate 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 pentahydrate selectively inhibits protein synthesis in cells and in extracts of Escherichia coli:
Spectinomycin dihydrochloride pentahydrate (50 μg/mL) inhibits Escherichia coli growth rapidly and reversibly, and suppresses amino acid incorporation immediately[1].
Spectinomycin dihydrochloride pentahydrate (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].
Spectinomycin dihydrochloride pentahydrate 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 pentahydrate interacts specifically with the residues G1064 and 01192 in 16S rRNA and potentially makes it inactive[2].
Spectinomycin dihydrochloride pentahydrate exhibits splicing inhibition and dependent on pH changes and Mg2+ concentration, indicating electrostatic interactions with the intron RNA[3].
In Vivo: Spectinomycin dihydrochloride pentahydrate (20 mg/kg; i.m.; 20-100 mg/kg; 9 d) shows the safety in healthy chicks[4].
Spectinomycin dihydrochloride pentahydrate (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 pentahydrate 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 | / | / |
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