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145435-72-9

145435-72-9 structure
145435-72-9 structure
  • Name: Gamithromycin
  • Chemical Name: gamithromycin
  • CAS Number: 145435-72-9
  • Molecular Formula: C40H76N2O12
  • Molecular Weight: 777.038
  • Catalog: API Antibiotics Peptide
  • Create Date: 2018-09-08 11:37:07
  • Modify Date: 2024-01-02 11:28:33
  • Gamithromycin is an antimicrobial agent which can inhibit the growth of MmmSC strains B237 and Tan8 with MICs of 0.00012 and 0.00006 μg/mL, respectively.

Name gamithromycin
Synonyms (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-7-azacylopentadecan-15-one
Zactran
(2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-2-Ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-15-oxo-7-propyl-11-{[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy}-1-oxa-7-azacyclopentadecan-13-yl 2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranoside
1-Oxa-7-azacyclopentadecan-15-one, 13-[(2,6-dideoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopyranosyl)oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-7-propyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-β-D-xylo-hexopyranosyl]oxy]-, (2R,3S,4R,5S,8R,10R,11R,12S,13S,14R)-
Gamithromycin
Description Gamithromycin is an antimicrobial agent which can inhibit the growth of MmmSC strains B237 and Tan8 with MICs of 0.00012 and 0.00006 μg/mL, respectively.
Related Catalog
Target

MIC: 0.00012 μg/mL (MmmSC strain B237), 0.00006μg/mL (MmmSC strain Tan8)[1]

In Vitro The MIC values in serum are significantly lower than those in artificial medium; at an initial inoculum size of 106 cfu/mL, these are 64-, 8- and 64-fold lower for gamithromycin, tylosin and tilmicosin, respectively, against MmmSC strain B237 in serum compare to artificial medium. A similar pattern emerges for Tan8. Heat-inactivation of serum results in an MIC for gamithromycin that is higher than in either non-treated serum or artificial medium[1].
In Vivo The proportion of foals that recover without the need for a change in treatment is significantly (P<0.048) higher for foals treated with Gamithromycin (GAM) (38 of 40; 95%) or AZM-RIF (39 of 40; 98%) compare to control foals (32 of 41; 78%). The clinical scores, number of abscesses and the abscess scores after 1 and 2 weeks of treatment are significantly lower for foals treated with Gamithromycin (GAM) or AZM-RIF compare to control foals. The WBC count of foals treated with Gamithromycin (GAM) is significantly higher than that of foals treated with AZM-RIF on week 3 of treatment[2].
Cell Assay Minimum inhibitory concentrations (MICs) for gamithromycin, tylosin and tilmicosin against MmmSC strains B237 and Tan8 are determined using a macrodilution technique. Equal volumes of MmmSC culture in logarithmic phase are added to each antimicrobial dilution to give an inoculum size of 107 cfu/mL, i.e. the intending initial titre for subsequent time-kill assays, in a volume of 4 mL. Cultures are incubated for 24 h at 37°C. At 0 and 24 h time points, samples are removed and serially diluted 10-fold down to 10-5. Aliquots (10 μL) of each dilution are transferred to solid medium; after incubation at 37°C in a humidified atmosphere of 5% carbon dioxide in air for at least 4 days, colonies are counted from the dilution that yields between 30 and 300 colonies per plate. Counts are converted into cfu/mL and MIC is defined as the lowest concentration of antimicrobial that prevents an increase in cfu/mL over 24 h[1].
Animal Admin Foals with ultrasonographic evidence of pulmonary abscesses are randomly assigned in 3 treatment groups: (1)gamithromycin at a dose of 6.0 mg/kg body weight is administered in the semimembranosus/semitendinosus muscles once a week (GAM; n=40); (2) azithromycin at a dose of 10 mg/kg PO once daily in combination with rifampin at a dose of 10 mg/kg PO once daily (AZM-RIF; n=40); and (3) no antimicrobial treatment (controls; n=41). All the foals in each treatment group also receive acetylcysteine at a dose of 10 mg/kg PO a day to provide the same daily manipulation of the foals in each group[2].
References

[1]. Mitchell JD, et al. In vitro pharmacodynamics of gamithromycin against Mycoplasma mycoides subspecies mycoides Small Colony. Vet J. 2013 Sep;197(3):806-11.

[2]. F. Hildebrand, et al. Efficacy of Gamithromycin for the Treatment of Foals with Mild to Moderate Bronchopneumonia. J Vet Intern Med. 2015 Jan-Feb; 29(1): 333–338.

Density 1.2±0.1 g/cm3
Boiling Point 833.0±65.0 °C at 760 mmHg
Molecular Formula C40H76N2O12
Molecular Weight 777.038
Flash Point 457.6±34.3 °C
Exact Mass 776.539856
PSA 180.08000
LogP 3.89
Vapour Pressure 0.0±0.6 mmHg at 25°C
Index of Refraction 1.535
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning
Hazard Statements H315-H319-H361d
Precautionary Statements P281-P305 + P351 + P338
Hazard Codes Xi
RIDADR NONH for all modes of transport