Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm afoxolaner hmoov hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo afoxolaner hmoov rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Afoxolaner hmoov, raws li hom tshiab ntawm isoxazoline compound, tau nyiam ntau yam hauv thaj chaw ntawm cov kws kho tsiaj vim nws cov kev tswj zoo heev ntawm cov kab mob ectoparasites xws li dev mub thiab zuam hauv dev thiab miv. Cov mis mos molecular yog C26H17ClF9N3O3, CAS 1093861-60-9, thiab qhov hnyav molecular yog 625.87 g / mol. Nws cov qauv tshuaj muaj cov isoxazoline nplhaib core, uas tau hloov kho nrog cov khoom siv tshwj xeeb (xws li 3-chloro-5-trifluoromethylphenyl, trifluoromethyl, trifluoromethylamino) kom muaj txiaj ntsig rau nws nrog kev ua haujlwm lom neeg tshwj xeeb. Qhov sib xyaw no belongs rau cov dawb mus rau dawb crystalline khoom nrog cov yam ntxwv siab melting point, thiab nthuav tawm cov khoom ruaj khov ntawm chav tsev kub.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
| Khoom npe | Afoxolaner ntsiav tshuaj | Afoxolaner hmoov |
| Yam khoom | Tablet | Hmoov |
| Khoom Purity | Ntau dua lossis sib npaug li 99% | Ntau dua lossis sib npaug li 99% |
| Khoom Specifications | Customizable | Customizable |
| Pob khoom | Customizable |
Customizable |
Afoxolaner +. COA
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Certificate of Analysis |
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Compound npe |
Afoxolaner | |
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CAS Nr. |
1093861-60-9 | |
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Qib |
Pharmaceutical qib | |
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Ntau |
Customized | |
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Ntim txheem |
Customized | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
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Ntau No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Qauv |
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| TEST STANDARD | GB/T24768-2009 Kev lag luam. Stnndard | |
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Yam khoom |
Enterprise txheem |
Kev txheeb xyuas qhov tshwm sim |
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Qhov tshwm sim |
Dawb los yog yuav luag dawb hmoov |
Ua raws |
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Cov ntsiab lus dej |
Tsawg dua lossis sib npaug li 4.5% |
0.30% |
| Poob rau ziab |
Tsawg dua lossis sib npaug li 1.0% |
0.15% |
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Hnyav Hlau |
Pb Tsawg dua lossis sib npaug li 0.5ppm |
N.D. |
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Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Hg Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Cd Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Purity (HPLC) |
Ntau dua lossis sib npaug li 99.0% |
99.5% |
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Ib leeg impurity |
<0.8% |
0.48% |
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Residue ntawm ignition |
<0.20% |
0.064% |
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Tag nrho microbial suav |
Tsawg dua lossis sib npaug li 750cfu / g |
80 |
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E. Coli |
Tsawg dua lossis sib npaug li 2MPN / g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (los ntawm GC) |
Tsawg dua lossis sib npaug li 5000ppm |
400ppm ua |
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Cia |
Khaws rau hauv qhov chaw kaw, tsaus thiab qhuav ntawm -20 degrees |
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Kev siv cov tshuaj Afoxolane
Lub neural cell membrane ntawm arthropods (fleas, zuam, mites) muaj GABA gated chloride ion channels thiab glutamate tswj chloride ion channels (GluCls), uas yog cov qauv tseem ceeb rau neural signal transduction;Afoxolaner hmoovxaiv khi rau ob hom channel protein conformational qhov chaw uas tau hais los saum toj no, thaiv cov tshuaj chloride ion influx thiab tiv thaiv cov neurons los ntawm kev ua kom tiav hyperpolarization repolarization, ua rau muaj kev cuam tshuam tsis zoo, cov leeg nqaij rigidity spasms, thiab thaum kawg parasite tuag tes tuag taw.
Kev kho mob thiab tag nrho lub voj voog tiv thaiv kab mob dev mub hauv dev thiab miv
Fleas (Ctenocephalides felis, tseem hu ua dev flea) yog cov ectoparasites ntau tshaj plaws hauv cov dev. Cov neeg laus tom tuaj yeem ua rau muaj kev tsis haum dermatitis, khaus hnyav, plaub hau poob, thiab lwm yam pyoderma. Poj niam fleas nteg ntau dua 50 qe ib zaug, thiab lawv cov qe txuas ntxiv mus rau hauv ib puag ncig, ua rau muaj kab mob rov qab. Txoj kev deworming ib txwm tsuas tua cov neeg laus thiab tsis tuaj yeem txiav tawm ntau tiam neeg.
Kev siv tshuaj kho mob rau cov kab mob yoov tshaj cum
Clinical standard dosage: Afoxolane 2.5-4mg/kg body weight, single oral administration of beef flavored chewable tablets; Efficacy data: Fleas were killed 2 hours after taking the medication, and the flea killing rate on the surface of the tested dogs was 100% at 6 hours, completely stopping skin damage caused by adult blood sucking; For severe whole body flea outbreaks (single dog body surface>500 tus neeg laus), ib qho kev tswj hwm ntawm 72 teev tuaj yeem tshem tawm tag nrho cov yoov tshaj cum nyob tsis muaj kev puas tsuaj tshiab, hloov cov kev kho mob nyuaj xws li tshuaj da dej thiab tshuaj tua kab mob. Cov ntaub ntawv soj ntsuam los ntawm cov tsev kho mob tsiaj hauv tsev los ntawm 2022 txog 2024: 1247 tus neeg mob ntawm cov kab mob dev mub loj hauv cov dev tau kho nrog Afoxolaner, nrog kev kho tus nqi ntawm 98.3%, zoo dua li cov tshuaj uas tsis yog prednisolone (81.6% kho tus nqi).
Lub sij hawm ntev tiv thaiv thiab thaiv cov dev mub yug me nyuam
Tom qab ib qho kev tswj hwm qhov ncauj, cov tshuaj tswj tau qhov tsis tu ncua -lub xeev cov concentration hauv cov ntshav plasma rau 30-35 hnub. Thaum lub sij hawm no, cov dev mub tshiab tuag nyob rau hauv ob peb teev tom qab tom thiab nqus ntshav. Fleas raug tua ua ntej lawv ua tiav qe, thaiv kev yug me nyuam ntawm ib puag ncig lub qe los ntawm qhov chaw thiab rhuav tshem tag nrho lub neej voj voog ntawm fleas (qe → larvae → pupae → laus), ua tiav xoom tshiab fleas nyob rau hauv ib puag ncig. Pom zoo los ntawm European thiab Asmeskas cov kws kho tsiaj cov lus qhia: Kev tswj hwm txhua hli thoob plaws hauv lub xyoo tuaj yeem tshem tawm tag nrho cov dev mub colonization nyob rau hauv ib puag ncig; Hauv thaj chaw ntub dej thiab los nag (xws li cov cheeb tsam yav qab teb plum nag thiab cov ntug dej hiav txwv), lub voj voog 35 hnub tuaj yeem khaws cia yam tsis muaj qhov sib txawv raws caij nyoog.
Blocking indirect siv cov kab mob dev mub mediated tapeworm
VThe canine tapeworm siv flea larvae ua tus tswv tsev nruab nrab, thiab kev noj cov dev mub uas muaj kab mob tapeworm los ntawm dev tuaj yeem ua rau mob plab hnyuv kab mob; Afoxolaner tua cov dev mub thoob plaws tag nrho lub voj voog, ua rau txo qis tus kab mob ntawm cov kab mob hauv cov dev. Raws li cov ntaub ntawv los ntawm Teb Chaws Asmeskas Lub Chaw Tiv Thaiv thiab Tiv Thaiv Kab Mob hauv 2024, cov dev tau noj Afoxolaner txhua hli tau pom tias txo qis ntawm cov kab mob tapeworm los ntawm 27.6% hauv cov dev tsis dewormed mus rau 3.1%, txo qhov zaus ntawm kev siv cov tshuaj tua kab mob hauv plab.
Afoxolaner hmoovyog ib qho tshuaj tua kab mob isoxazoline hauv qhov ncauj / acaricide tsuas yog siv rau kev tiv thaiv thiab tswj cov kab mob ntawm cov dev. Nws cov txheej txheem synthesis muaj ntau haiv neeg, thiab ntau txoj kev sib xyaw ua ke yuav raug qhia hauv qab no.
(1) Synthesis cov kauj ruam
Aldol condensation yog:
Pib los ntawm 1-naphthalenedione, nruab nrab kuv tau txais los ntawm aldol condensation cov tshuaj tiv thaiv nrog 3,5-dichloro-trifluoroacetophenone, thiab cov txiaj ntsig ntawm cov kauj ruam no tuaj yeem ncav cuag 82.2%.
Ring reaction:
Intermediate I tau txais lub nplhaib cov tshuaj tiv thaiv nrog hydroxylamine kom tau txais qhov tseem ceeb nruab nrab II, nrog cov txiaj ntsig ntawm 87.5% hauv cov kauj ruam no.
Cov tshuaj tiv thaiv Formylation:
Qhov tseem ceeb nruab nrab II tau dhau los ua cov tshuaj tiv thaiv ntxiv kom tau txais qhov tseem ceeb nruab nrab III nrog cov txiaj ntsig ntawm 88.4%.
Cov tshuaj tiv thaiv zaum kawg:
Intermediate III reacts nrog 2-amino-N - (2,2,2-trifluoroethyl) acetamide hydrochloride thiab oxidant kom tau Aflana.
(2) Kev txheeb xyuas qhov zoo thiab qhov tsis zoo
Qhov zoo:
Txoj kev hluavtaws no pib nrog cov naphthophenone uas yog cov khoom siv raw, uas yog qhov yooj yim kom tau txais. Cov tawm los ntawm txhua kauj ruam yog siab, thiab tag nrho cov synthesis efficiency yog zoo, uas yog conducive rau industrial ntau lawm.
Qhov tsis zoo:
Cov txheej txheem synthesis suav nrog ntau yam tshuaj tiv thaiv, xav tau kev tswj xyuas meej ntawm cov tshuaj tiv thaiv xws li qhov kub thiab txias, lub sijhawm tshuaj tiv thaiv, ntau npaum li cas reagent, thiab lwm yam, uas ua rau muaj kev xav tau siab ntawm kev sim ua haujlwm. Lub caij no, cov oxidants thiab lwm yam reagents siv yuav ua rau muaj kev pheej hmoo thiab yuav tsum tau ceev faj txog kev nyab xeeb.
(1) Synthesis cov kauj ruam
Aldol condensation yog:
Pib los ntawm 1- (4-bromo-1-naphthyl) ethanone, nws nkag mus rau aldol condensation cov tshuaj tiv thaiv nrog 3,5-dichloro-trifluoroacetophenone kom tau nruab nrab IV (ie . 1- (4-bromo-naphthyl-1-yl) -3-5 (3-chloromethyl) -4,4,4-trifluoro-2-buten-1-ib), nrog rau cov txiaj ntsig ntawm 85.6%.
Ring reaction:
Intermediate IV tau txais lub nplhaib cov tshuaj tiv thaiv nrog hydroxylamine kom tau txais cov ntsiab lus nruab nrab 4- {5- [3-chloro-5- (trifluoromethyl) phenyl] -5-trifluoromethyl-4,5-dihydroisoxazole-3-yl} naphthalene-1-carboxaldehyde (intermediate V) nrog 8 . Cov kauj ruam ntxiv yuav tsum tau ua kom tau Afurana.
(2) Kev txheeb xyuas qhov zoo thiab qhov tsis zoo
Qhov zoo:
Cov khoom pib 1- (4-bromo-1-naphthyl) ethanone muaj qee yam reactivity, uas yog qhov zoo rau cov tshuaj tiv thaiv tom qab. Cov txiaj ntsig ntawm aldol condensation thiab cyclization tshwm sim kuj tseem muaj txiaj ntsig, muab txoj hauv kev ua tau zoo rau kev sib txuas ntawm Aflana.
Qhov tsis zoo:
Tus nqi ntawm bromonaphthyl ethyl ketone tej zaum kuj siab, uas ua rau kom tus nqi synthesis. Ntxiv mus, txoj kev synthesis no tseem muaj ntau cov kauj ruam tshuaj tiv thaiv, xav tau kev tswj xyuas meej ntawm cov tshuaj tiv thaiv, thiab cov txheej txheem synthesis yog qhov nyuaj.
(1) Ib txoj kev hluavtaws pib los ntawm 4-acetyl-1-naphthoic acid thiab 2-amino-N - (2,2,2-trifluoroethyl) acetamide
Cov tshuaj tiv thaiv condensation:
4-acetyl-1-naphthoic acid thiab 2-amino-N - (2,2,2-trifluoroethyl) acetamide yog condensed kom tau 4-acetyl-N - (2-oxo-2- (2,2,2-trifluoroethyl) amino-1.
Cov tshuaj tiv thaiv tom qab:
Qhov nruab nrab tau txais cov tshuaj tiv thaiv condensation nrog 1- (3-chloro-5- (trifluoromethyl) phenyl) -2,2,2-trifluoroethyl-1-ib nyob rau hauv qhov kev txiav txim ntawm lub hauv paus los npaj (Z) -4- (3- (3-chloro-5- (trifluoromethyl) 4, phenyl-4, phenyl-4, phenyl) N - (2-oxo-2- (2,2,2-trifluoroethyl) amino) ethyl) -1-naphthalimide. Thaum kawg, lub compound tau hnov mob nrog hydroxylamine sulfate los npaj Aflana.
(2) Ib txoj kev hluavtaws pib los ntawm nitromethane nruab nrab thiab 1-chloro-3- (trifluoromethyl) -5- (3,3,3-trifluoropropy-1-en-2-yl) benzene compound
Dipole cycloaddition cov tshuaj tiv thaiv: Nitromethane intermediate undergoes dipole cycloaddition cov tshuaj tiv thaiv nrog 1-chloro-3- (trifluoromethyl) -5- (3,3,3-trifluoropropy-1-en-2-yl) benzene compound. Cov khoom pib nitromethane yog npaj los ntawm kev sib txuas cov tshuaj tiv thaiv ntawm bromobenzene derivatives thiab nitromethane nyob rau hauv qhov kev txiav txim ntawm palladium catalyst thiab ligand.
Lub cev lub cev thiab cov yam ntxwv zoo li no:
Afoxolaner hmoovzoo nkaus li dawb mus rau dawb crystalline hmoov nyob rau hauv tus qauv tej yam kev mob, uas ua rau nws yooj yim mus sib tov nrog lwm yam excipients nyob rau hauv formulation txoj kev loj hlob. Nws cov morphology siv lead ua tuaj yeem ua tus yam ntxwv ntxiv los ntawm X-ray diffraction (XRD) los txiav txim siab crystal stability. Nyob rau hauv kev tsim cov formulations, cov particle loj tis ntawm cov hmoov yuav tsum tau nruj me ntsis tswj kom lub uniform dispersion ntawm cov tshuaj nyob rau hauv chewable ntsiav tshuaj. Piv txwv li, NexGard chewable ntsiav tshuaj yog ua rau lub teeb liab mus rau reddish xim av ncig los yog square ntsiav tshuaj siv ib tug tshwj xeeb txheej txheem los xyuas kom meej cov tshuaj stability thiab txhim khu palatability.
Solubility thiab hnyav selectivity:
Cov dej solubility ntawm Aflana yog qhov tsawg kawg nkaus, nrog kev solubility ntawm tsuas yog 3.4 × 10 ⁻⁵ g / L ntawm 25 degree, uas txwv txoj kev loj hlob ntawm nws cov dej -raws li formulations. Txawm li cas los xij, nws pom zoo solubility hauv cov kuab tshuaj organic, tshwj xeeb tshaj yog nyob rau hauv dimethyl sulfoxide (DMSO) qhov twg cov solubility tuaj yeem ncav cuag ntau dua lossis sib npaug li 250 mg / mL (399.44 mM). Cov yam ntxwv no muab kev yooj yim rau kev tshawb fawb hauv chav kuaj, piv txwv li, hauv kev sim tshuaj pharmacokinetic, DMSO feem ntau yog siv los ua cov kuab tshuaj los npaj cov kev daws teeb meem. Tsis tas li ntawd, kev tshawb fawb ntxiv yog xav tau ntawm kev solubility hauv cov kuab tshuaj xws li ethanol thiab acetone los txhim kho cov txheej txheem formulation.
Thermal stability thiab cia tej yam kev mob:
Txoj kev tshawb fawb thermal stability ntawm Aflana qhia tau hais tias nws tuaj yeem tswj tau tshuaj lom neeg ruaj khov rau lub sijhawm ntev ntawm chav tsev kub, tab sis kev degradation yuav tshwm sim nyob rau hauv qhov kub thiab txias. Yog li, nws raug pom zoo kom khaws cia ntawm -20℃lossis 2-8℃hauv qhov tsaus ntuj kom tsis txhob poob ntawm cov khoom xyaw nquag. Hauv kev ntsuam xyuas kev ruaj ntseg ntawm cov qauv, nws yog ib qho tsim nyog los saib xyuas cov kev hloov pauv hauv nws cov ntsiab lus ntawm qhov sib txawv ntawm qhov kub thiab txias (xws li 40℃/ 75% RH nrawm ntsuas) kom ntseeg tau tias cov khoom zoo hauv nws lub txee lub neej. Piv txwv li, hnub tas sij hawm ntawm Nicosin chewable ntsiav tshuaj yog 24 lub hlis, thiab nws lub ntim ntim tsim tau zoo cais cov dej noo thiab oxygen, txuas ntxiv kev ruaj ntseg tshuaj.
PH thiab pKa tus nqi:
Lub acidity coefficient (pKa) ntawm Aflana yog 12.45 ± 0.46 (tus nqi kwv yees), qhia tias nws muaj nyob rau hauv daim ntawv anionic nyob rau hauv physiological pH. Cov yam ntxwv no cuam tshuam rau nws txoj kev nqus ntawm lub plab zom mov, piv txwv li, hauv cov dev, Aflana nkag mus rau hauv cov hlab ntsha los ntawm kev tsis sib haum xeeb thiab cov neeg nqa khoom nruab nrab thauj. Nws tus nqi pKa siab kuj piav qhia nws qhov kev ruaj ntseg hauv cov kua qaub (xws li kua txiv hmab txiv ntoo), tab sis ionization yuav tshwm sim nyob rau hauv alkaline tej yam kev mob, thiab kev siv cov pH regulators yuav tsum tau txiav txim siab nyob rau hauv formulation tsim.
Spectral yam ntxwv thiab kev txheeb xyuas:
Lub InChIKey ntawm Afrana yog OXDDDHGGRFRLEE-UFFAOYSA-N, thiab SMILES code yog C1(C(NCC(=O)NCC(F)(F)F)=O)=C2C(C=CC=C2)=C(C2C) C(C3=CC(C(F)(F)F)=CC(Cl)=C3)(C(F)(F)F)ON=2)C=C1. Cov cim cim tshwj xeeb no tuaj yeem siv rau kev khaws cov ntaub ntawv thiab kev siv cov qauv siv. Nws UV pom kev nqus spectrum muaj cov yam ntxwv nqus siab siab ntawm cov wavelengths tshwj xeeb, uas tuaj yeem siv rau kev txiav txim siab cov ntsiab lus. Piv txwv li, siab -kev ua tau zoo ntawm cov kua chromatography (HPLC) feem ntau yog siv los txheeb xyuas cov purity (Ntau dua lossis sib npaug li 98%) thiab xyuas kom meej cov khoom zoo.
Lub cev muaj feem xyuam nrog kev tsim:
Hauv kev tsim kho, cov khoom siv lub cev ntawm Aflana ncaj qha cuam tshuam rau cov txheej txheem tsis. Piv txwv li, nws lub siab melting point yuav tsum tau kub thiab siab tswj thaum lub sij hawm compression txheej txheem kom tsis txhob siv lead ua transformation. Lub flowability ntawm nws cov hmoov yuav tsum tau txhim kho los ntawm kev ntxiv cov kev pab cuam txaus (xws li microcrystalline cellulose) kom ntseeg tau tias qhov sib txawv qhov hnyav ntawm cov ntsiav tshuaj raws li cov qauv tshuaj pharmacopoeia. Tsis tas li ntawd, cov kev tshawb fawb txog kev sib raug zoo ntawm Afurana nrog excipients tau qhia tias nws tsis cuam tshuam nrog cov khoom siv nquag xws li cov hmoov txhuv nplej siab thiab lactose, tab sis yuav tsum tsis txhob sib cuag nrog cov hlau ions los tiv thaiv catalytic degradation.
Kev sib raug zoo ntawm lub cev thiab cov tshuaj pharmacological:
Lub cev lub cev ntawm afoxolaner yog ze ze rau nws cov tshuaj pharmacological. Piv txwv li, nws cov dej solubility tsawg yuav ua rau qeeb tso tawm hauv lub plab zom mov, ua rau lub sijhawm ntev ntawm kev siv tshuaj (xws li kev ua tau zoo txhua hli ntawm Nissin). Nws cov morphology siv lead ua cuam tshuam rau qhov kev sib cais, uas ua rau muaj kev cuam tshuam rau lub sijhawm siab tshaj plaws ntawm cov tshuaj ntshav siab (Tmax=2-4 teev). Tsis tas li ntawd, nws txoj kev sib raug zoo nrog GABA receptors thiab glutamate gated chloride ion channels yuav cuam tshuam los ntawm molecular conformation, thiab conformational stability muaj feem xyuam rau nws lub cev lub cev.
Cov lus nug nquag
Yam tshuaj twg yog afoxolaner?
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Afoxolaner belongs rau cov chav kawm tshuaj isoxazoline, uas yog ib pawg ntawm cov tshuaj tua kab mob thiab tshuaj tua kab uas siv hauv cov tshuaj kho tsiaj.
Nws ua los ntawm inhibiting GABA-gated chloride channels hauv lub paj hlwb ntawm kab thiab arachnids, ua rau overexcitation thiab tuag ntawm cov cab. Afoxolaner feem ntau yog siv los tiv thaiv thiab kho cov kab mob yoov thiab zuam hauv dev.
Puas yog afoxolaner tib yam li ivermectin?
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The efficacy of afoxolaner was >96%, qhov kev ua tau zoo ntawm ivermectin tau qis dua piv nrog afoxolaner (p < . 05) thiab yeej tsis tau ua tiav 90% kev ua tau zoo uas tau thov los ntawm cov koom haum sau npe.
Vim li cas NexGard tsis zoo rau dev?
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Siv NexGard PLUS nrog ceev faj hauv cov dev uas muaj keeb kwm ntawm qaug dab peg los yog mob hlwb. Yog xav paub ntxiv, nyem qhov no rau cov ntaub ntawv sau tshuaj tag nrho. Tom qab siv HEARTGARD Plus (ivermectin / pyrantel) hauv cov dev, kev zom zaub mov thiab cov kab mob neurologic thiab khaus tau raug tshaj tawm.
Cim npe nrov: afoxolaner hmoov, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom