Tildipirosin

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CAS:328898-40-4

Takaddun shaida:GMP & ISO

Shiryawa:25kg/drum

Misali:Akwai

 

 


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Tildipirosin

Tildipirosin wani sabon nau'in maganin rigakafi ne na zobe macrolide mai memba 16, wanda ya samo asali ne daga tylosin.

Pharmacological mataki

Tasirin ƙwayoyin cuta na Tildipirosin yana kama da na tylosin, kuma yana da tasirin hanawa mai ƙarfi akan ƙwayoyin gram-positive da wasu ƙwayoyin cuta na Gram-negative.Tsarin antibacterial na Tildipirosin daidai yake da na macrolides.Yana iya haɗawa tare da sashin 50S na ribosome na ƙwayoyin cuta masu mahimmanci don hana haɗakar sarƙoƙi na peptide riboprotein, ta haka yana shafar haɓakar sunadaran ƙwayoyin cuta.Harkokin hulɗar nau'in piperidine guda biyu na musamman ga Tildipirosin ya bambanta tsarin aikin wannan miyagun ƙwayoyi daga tylosin da tilmicosin, inda 20-piperidine ya jagoranci cikin lumen don tsoma baki tare da ci gaban peptides masu tasowa.

Saboda tediroxine yana da ƙungiyoyin amino na asali guda 3, yana iya ƙirƙirar nau'ikan caji daban-daban a ƙarƙashin yanayin pH daban-daban.Adadin cajin shine maɓalli mai mahimmanci don lalata narkewar lipids na kwayan cuta kuma ya shiga cikin membrane na waje na ƙwayoyin cuta na Gram, don haka aikin bacteriostatic na Tildipirosin in vitro yana da tasiri sosai ta pH.A ƙarƙashin yanayin acidic, ƙungiyar amino ɗin tana haɓakawa, wanda ke haifar da raguwar ayyukan ƙwayoyin cuta na tediroxine, yayin da a ƙarƙashin yanayin alkaline, yana da ƙarfin aikin ƙwayoyin cuta.

Macrolides sun hana ɓoyewar cytokines na proinflammatory, ayyukan phospholipase, da sakin leukotriene, kuma suna da tasirin anti-mai kumburi a cikin macrophages da neutrophils.Tediroxine yana rage masu shiga tsakani masu kumburi da aka samar a lokacin wasu abubuwan kumburi ko damuwa.

Antibacterial bakan

Tildipirosin yana da tasiri a kan kwayoyin cutar da ke haifar da cututtuka na numfashi a cikin aladu da shanu (irin su Pasteurella multocida, Actinobacillus pleuropneumoniae, Bordetella bronchiseptica, Haemophilus parasuis, Mannheim spp. da dai sauransu) aikin antibacterial na tilmicosin ya kasance sau 2-32 fiye da na tilmi. , da kuma aikin antibacterial akan Escherichia coli na hanji ya fi tylosin da tilmicosin kyau.Hakanan yana kula da wasu nau'ikan mycoplasma, spirochetes, brucella, da sauransu. Nazarin ya nuna cewa tediroxine yana da tasirin bacteriostatic mai ƙarfi akan Haemophilus parasuis da Bordetella bronchiseptica fiye da florfenicol, amma mafi raunin bacteriostatic sakamako akan Actinobacillus pleuropneumoniae da Pasteurella mulchTildipirosin yana kashe kwayoyin cuta ga wasu kwayoyin cuta (kamar Haemophilus parasuis da Actinobacillus pleuropneumoniae), yayin da yake da yawa bacteriostatic ga wasu kwayoyin cuta (kamar Pasteurella multocida).Don ƙwayoyin cuta na hanji, tare da raguwar darajar pH (daga 7.3 zuwa 6.7), MIC na Tildipirosin ya karu, alal misali, MIC na Tildipirosin da Salmonella Enteritidis da Escherichia coli na iya karuwa daga 2 ~ 8ug / m zuwa 64 ~ 256ug / mL. .Sabili da haka, ya kamata a yi la'akari da tasirin pH a cikin vivo yayin gudanar da gwajin ƙwayoyin cuta na in vivo na Tildipirosin.Bugu da ƙari, MIC na Tildipirosin akan nau'in nau'in nau'in Pasteurella multocida shine 0.5ug / mL a cikin jini, wanda ya kasance 0.25 sau da yawa fiye da na in vitro, wanda zai iya danganta da tasirin maganin.

Enterococcus-Streptococcus a cikin shanun kiwo yana da matukar juriya ga tediroxine.Tildipirosin ba shi da hankali ga Pasteurella multocida da Mannheimia haemolyticus mai ɗauke da kwayoyin halitta.Hakazalika, nau'in M. bovis da suka rikiɗe suna jure wa maganin rigakafi na macrolide ciki har da Tildipirosin.An kuma gano wasu nau'ikan Haemophilus parasuis suna da juriya ga tediroxine a zahiri.Mycoplasma bovis na iya samun juriya da sauri zuwa Tildipirosin, amma saboda jinkirin girma na Mycoplasma, gwajin kamuwa da ƙwayoyin cuta na in vitro na iya jinkirta jiyya.Nazarin ya nuna cewa yankin II (nucleotide 748) da yankin V (Maye-sauye a cikin nucleotides 2059 da 2060) suna da alaƙa da haɓaka juriya ga macrolides.Saboda haka, ana iya samun saurin kamuwa da M. bovis zuwa magungunan macrolide ta hanyar gwajin kwayoyin halitta na wannan maye gurbi.

Tiamulin-Hydrogen-Fumarate1

Abun ciki

≥ 98%

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