Qhov twg Fluralaner haum hauv Isoxazoline Class

Tshawb nrhiav qhov twg fluralaner haum nyob rau hauv chav kawm isoxazoline - nws cov txheej txheem tshwj xeeb, chloride channel phiaj, thiab yuav ua li cas nws sib nrug hauv kev tswj ectoparasite niaj hnub. Thaum cov kws tshawb fawb thiab cov kws tsim qauv tham txog tom ntej - tiam ectoparasiticides, chav kawm isoxazoline ua rau muaj kev mob siab rau. Nyob rau hauv cov chav kawm ntawd, fluralaner nyob ib qho chaw tshwj xeeb -txhais chaw - ib qho zoo li nws cov kev xaiv molecular, ntev - kev ua ub no, thiab kev loj hlob muaj feem cuam tshuam thoob plaws cov kws kho tsiaj thiab cov ntawv thov tshawb fawb. Tsab ntawv xov xwm no nthuav tawm yuav ua li cas fluralaner cuam tshuam nrog lwm cov isoxazolines, dab tsi ua rau nws cov txheej txheem sib txawv, thiab vim li cas kev nkag siab qhov sib txawv no tseem ceeb rau txhua tus neeg ua haujlwm hauv cov tshuaj nruab nrab lossis cov khoom siv tshuaj tshwj xeeb.

Fluralaner Drops

1. General Specification (hauv Tshuag)
(1) Kev daws teeb meem
(2) Tablet
(3) Txhaj tshuaj
(4) Txau
(5) Poob
2.Customization:
Peb yuav sib tham tus kheej, OEM / ODM, Tsis muaj hom, rau kev tshawb nrhiav kev ruaj ntseg nkaus xwb.
Internal Code: BM-9-007
Fluralaner CAS 864731-61-3
Lub khw tseem ceeb: Tebchaws Asmeskas, Australia, Brazil, Nyiv, Lub Tebchaws Yelemees, Indonesia, UK, New Zealand, Canada thiab lwm yam.
Chaw tsim tshuaj paus: BLOOM TECH Xi'an Hoobkas
Kev tshuaj xyuas: HPLC, LC-MS, HNMR
Kev them nyiaj yug Technology: R & D Dept.-4

Cov qauv sib txawv uas zoo li kev ua haujlwm

Ob peb lub tebchaw nquag sib koom nrog isoxazoline scaffold, tab sis cov tshuaj hloov pauv ntawm cov tshuaj no ua rau muaj kev coj cwj pwm tseem ceeb. Fluralaner muaj cov pab pawg tshwj xeeb trifluoromethyl sulfonyl thiab muaj cov qauv hloov pauv uas pab nws khi thiab nyob ruaj khov hauv lub cev metabolism. Cov cwj pwm no ua rau nws txawv ntawm lwm cov tshuaj isoxazoline raws li nws ua haujlwm tau zoo thiab ntev npaum li cas.

Fluralaner tau noj thoob plaws hauv lub cev thiab tau txais kab ectoparasites los ntawm cov ntshav noj. Qhov no txawv ntawm cov tshuaj pleev ib ce lossis tiv tauj - cov neeg ua haujlwm ua haujlwm. Ntau tus phooj ywg- tshuaj xyuas kev tshawb fawb, xws li Rohdich et al. (2014), uas tau lees paub 12-lub lim tiam flea thiab zuam tswj nyob rau hauv cov tsiaj phooj ywg, tau qhia tias cov khoom no ua hauj lwm rau lub sij hawm ntev vim hais tias nws yog faib thoob plaws hauv lub cev.

 

 

Duration thiab Selectivity piv rau cov qauv Analogues

Lwm cov tshuaj nyob rau hauv chav kawm isoxazoline ua haujlwm zoo ib yam los thaiv cov enzymes, tab sis lawv muaj ib nrab ntawm -lub neej, kev tswj hwm, thiab muaj peev xwm los tsom rau cov hom tshwj xeeb. Fluralaner muaj plasma ib nrab-lub neej ntawm 12-15 hnub hauv cov dev, yog vim li cas nws tuaj yeem muab tau ntev dua. Cov tshuaj pharmacokinetic no tsis yog ib txwm pom hauv tsev neeg isoxazoline. Qhov no ua rau fluralaner xaiv cov tshuaj zoo dua rau cov xwm txheej uas yuav tsum tau muaj kev cuam tshuam ntev -.

Lub luag haujlwm ntawm Ligand-Gated Chloride Channels hauv Invertebrate Physiology

Hauv arthropods, ligand-gated ion channels tswj kom txaus siab neurons tuaj yeem tau txais. GABA-gated thiab glutamate-gated chloride channels yog ob qho tseem ceeb tshaj plaws rau kev sib txuas lub hlwb thiab cov leeg nqaij.Fluralaneryog ib tug muaj zog blocker ntawm ob hom ntawm channel, txwv tsis pub cov chloride ntws thiab teeb tawm chaotic neuronal kev ua si nyob rau hauv parasites uas nws lub hom phiaj.

Qhov kev thaiv ntawm ob txoj kab no yog qhov zoo -paub qhov zoo ntawm fluralaner's pharmacodynamics. Kev kawm los ntawm Ozoe et al. (2010) hauv British Journal of Pharmacology xam pom tias isoxazoline ua haujlwm li cas ntawm qib molecular ntawm invertebrate chloride channels. Qhov no tau muab cov kws tshawb fawb ib txoj hauv kev los piav qhia vim li cas cov tshuaj xws li fluralaner tua hma, zuam, thiab mites sai thiab zoo.

Yog vim li cas Arthropod Selectivity Matters nyob rau hauv Tshuaj Sourcing

Vim hais tias cov qauv ntawm cov chloride channel subtypes txawv nyob rau hauv arthropods thiab vertebrates, fluralaner muaj ib tug siab selectivity sib txawv uas txhawb nws txoj kev ruaj ntseg profile nyob rau hauv cov tsiaj. Qhov tshwj xeeb biochemical no tsis yog ib qho kev sib tham hauv pharmacology xwb; nws muaj kev cuam tshuam ncaj qha rau cov neeg muag khoom thiab cov kws tshawb fawb tau faib cov fluralaner li cov tshuaj nruab nrab thiab vim li cas nws thiaj li xav tau ntau hauv kev lag luam tshuaj zoo.

Targeting Ligand-Gated Chloride Channels

Fluralaner thaiv ligand-gated chloride channel tsim nyog rau cov paj hlwb kom pom tseeb hauv cov kab mob rhiab heev. Los ntawm kev cuam tshuam cov channel no nws hloov qhov sib npaug ntawm cov hlab ntsha kev ua haujlwm thiab inhibits cov kab mob los ntawm kev tswj hwm kev txav mus los thiab ua haujlwm. Cov txheej txheem no yog tus yam ntxwv ntawm cov chav kawm isoxazoline thiab txhawb kev nkag siab txog kev ua haujlwm zoo ntawm fluralaner tiv thaiv cov phiaj xwm ectoparasites. Tsis zoo li cov tshuaj lom neeg dav dav, nws cov haujlwm yog txuas rau cov hom phiaj ntawm lub paj hlwb, muab cov qauv tsim thiab cov kws kho tsiaj uas muaj cov tshuaj muaj tseeb meej rau nws siv hauv kev tswj cov kab mob parasite.

Isoxazoline Structure thiab Selective Activity

Fluralaner belongs rau chav kawm isoxazoline ntawm molecules,

uas tau tsim los xaiv lub hom phiaj ntawm cov kab mob parasite neurological. Nws kev sib cuam tshuam nrog ligand gated chloride channels txawv ntawm cov tshuaj tiv thaiv kab mob coj mus rau lwm lub hom phiaj lom neeg. Lub hom phiaj no -oriented mechanism yog tshwj xeeb muaj feem xyuam rau qhov kev ntsuam xyuas ntawmfluralanernrog rau lwm yam tshuaj ntawm tib chav kawm. Nws kuj tseem pab cov neeg tsim khoom thiab cov kws tshawb fawb nkag siab txog qhov sib txuas ntawm nws cov qauv tshuaj thiab kev ua haujlwm receptor, nrog rau kev txiav txim siab tsim cov kev xav tau, kev ua haujlwm ntawm cov khoom, thiab lub luag haujlwm ntawm fluralaner hauv kev tswj hwm ectoparasite tam sim no.

Los ntawm Channel cuam tshuam rau Parasite Control

Fluralaner ua haujlwm ntawm qib ntawm cov receptor, tab sis qhov kawg tshwm sim yog kev puas tsuaj ntawm kev txav mus los thiab muaj sia nyob ntawm cov cab. Los ntawm kev thaiv cov cim qhia ntawm cov tshuaj chloride, cov kab mob hauv lub paj hlwb raug tiv thaiv los ntawm kev tswj hwm kev ua haujlwm kom raug.

Kev cuam tshuam ntawm neurological ua rau tuag tes tuag taw thiab tuag ntawm cov kab mob rhiab heev. Qhov kev sib raug zoo ntawm molecular kev txiav txim thiab cov lus teb lom neeg muaj txiaj ntsig zoo rau cov neeg tsim khoom vim nws nthuav tawm lub hauv paus ntawm fluralaner cov tshuaj tiv thaiv kab mob. Nws kuj tseem muaj cov ntsiab lus tseem ceeb rau kev sib piv fluralaner rau lwm cov tshuaj isoxazoline ua los ntawm cov hom phiaj zoo sib xws.

Lub hom phiaj txoj hauv kev rau Parasite Nerve Signaling

Fluralaner yog cov txheej txheem tshiab rau kev tswj hwm ectoparasite uas tsom rau ligand -gated chloride channels hauv cov kab mob cab. Cov channel no ua lub luag haujlwm tseem ceeb hauv kev tswj hwm kev ua haujlwm ntawm cov hlab ntsha, thiab kev puas tsuaj rau lawv cov kev ua haujlwm tsis tu ncua tuaj yeem ua rau kev ua haujlwm tsis zoo ntawm lub paj hlwb, tuag tes tuag taw thiab tuag ntawm cov cab. Cov txheej txheem no muaj ntau yam tshwj xeeb rau fluralaner los tua fleas, zuam thiab lwm yam ectoparasites yooj yim dua li cov txheej txheem dhau los uas yuav tsom mus rau ntau hom kab mob lom neeg. Nws qhov kev txiav txim ntawm lub paj hlwb yog txuas nrog rau cov tshuaj pharmacological uas ua rau cov chav kawm isoxazoline.

Yuav ua li cas GABA-Txog Kev Ua Haujlwm Pab Tswj Ectoparasites

GABA-gated chloride channels yog ib qho tseem ceeb inhibitory mechanism nyob rau hauv lub neural systems ntawm ntau invertebrates. Fluralaner cuam tshuam cov channel no thiab yog li cuam tshuam nrog kev sib npaug ntawm cov paj hlwb hauv cov kab mob tsis zoo. Thaum qhov inhibition no ploj lawm cov kab mob hauv lub paj hlwb mus haywire thiab thaum kawg poob tswj kev txav thiab lwm yam tseem ceeb. Ib qho laj thawj vim li cas cov tshuaj isoxazoline yog ib qho tseem ceeb ua ntej hauv kev tswj flea tam sim no thiab zuam yog lawv lub peev xwm los ua haujlwm ntawm cov kab mob no - cov hom phiaj tshwj xeeb neuronal.

Los ntawm Kev Tswj Dav mus rau Ntau Lub Hom Phiaj Ectoparasite Management

Fluralaner txoj kev loj hlob yog ib feem ntawm txoj kev loj dua hauv kev tsim cov tshuaj uas tsom rau cov hom phiaj molecular.

Kev tswj hwm ectoparasite niaj hnub no yog ntau thiab ntau dua los ntawm kev sib txawv ntawm tus tswv tsev thiab cov kab mob kab mob parasitic es tsis yog cov tshuaj lom neeg. Txoj kev no zoo ib yam nrog fluralaner, uas yog nyob rau hauv chav kawm isoxazoline thiab ua rau ligand-gated chloride channels. Cov ntaub ntawv no muaj txiaj ntsig zoo rau cov neeg tsim khoom lag luam thiab cov chaw muab tshuaj kho tsiaj thaum txiav txim siab txog qhov muaj peev xwm ntawm cov tshuaj tiv thaiv kab mob tshwm sim kom xa cov kev tswj hwm ectoparasite zoo nrog kev xaiv hom kev ua.

Sib koom Scaffold, Divergent Selectivity Profiles

Nws yog qhov tseeb tias tag nrho cov isoxazolines ua haujlwm ntawm invertebrate chloride channels, tab sis theem ntawm kev xaiv ntawm GABA- thiab glutamate-gated subtypes txawv hauv chav kawm.Fluralanerthaiv ob leeg nrog txog tib theem ntawm lub zog, uas ua rau nws txawv ntawm cov tshuaj zoo sib xws uas muaj zog tiv thaiv ib qho subtype dua li lwm tus. Nws qhov dav -spectrum kev ua tau zoo tiv thaiv yoov tshaj cum, ntau hom zuam, thiab mites yog ib feem ntawm qhov kev tiv thaiv ob.

Qhov cuam tshuam rau Pharmaceutical Intermediate Applications

Nws yog qhov muaj txiaj ntsig zoo rau cov kws tshawb fawb kom paub txog qhov sib txawv no thaum lawv ua cov isoxazoline derivatives lossis nrhiav fluralaner raws li cov qauv siv los yog nruab nrab.

 

 

Nws pab nrog kev txiav txim siab txog kev tsim cov derivatives, npaj kev sib piv bioassays, thiab sau cov ntaub ntawv tswj hwm. Ntau thiab ntau, cov tuam txhab uas ua haujlwm hauv kev tshawb fawb tshuaj thiab kev tsim kho lossis kev lag luam tshuaj tshwj xeeb pom cov fluralaner tsis yog tsuas yog cov khoom xyaw nquag xwb tab sis kuj yog cov qauv molecule hauv chav kawm isoxazoline.

Fluralaner muaj qhov chaw ntshiab hauv chav kawm isoxazoline. Nws muaj dual chloride channel inhibition, kev thauj mus los hauv lub cev, thiab cov tshuaj pharmacokinetic profile uas tso cai rau lub sijhawm ntev - koob tshuaj. Nws txawv ntawm cov laus ectoparasiticide cov chav kawm thiab nws cov isoxazoline analogs vim tias nws ua haujlwm li cas nrog cov qauv tshwj xeeb thiab cov receptors.Fluralaneryog cov tshuaj muaj zog thiab txhim khu kev qha uas tuaj yeem siv los ua qhov pib rau txhua tus neeg yuav khoom, kawm, lossis kev tsim kho hauv cheeb tsam no.

Bloomtechz npaj txhij los pab koj nrhiav kev ntseeg siabfluralaner suppler uas nws cov khoom yog GMP{0}} ntawv pov thawj thiab nws cov qauv zoo tau raug kuaj xyuas. Bloomtechz tau ua lag luam txij li xyoo 2008 thiab muaj 100,000 m² koom tes GMP cog uas tau pom zoo los ntawm US -FDA, EU-GMP, JP, thiab CFDA. Lawv coj ntau tshaj 12 xyoo ntawm kev paub hauv organic synthesis rau txhua qhov kev txiav txim. Peb txoj kev tswj xyuas qhov zoo muaj peb theem: hauv{10}}lub Hoobkas, hauv- tsev QA/QC, thiab thib peb-tsoomfwv pov thawj. Cov qib no ua kom paub tseeb tias txhua qhov kev xa khoom xa tuaj raws li cov nqe lus ntawm koj daim ntawv cog lus. Peb muag rau cov neeg yuav khoom tshwj xeeb tshuaj, tuam txhab tshuaj, thiab R & D labs thoob plaws ntiaj teb. Xa lus rau peb tam sim no, thiab peb yuav ua qhov zoo tshaj plaws kom phim koj cov kev xav tau nrog cov nqi raug thiab cov sij hawm ua tau zoo. Email rau peb ntawmSales@bloomtechz.com, thiab peb pab neeg yuav teb koj kom raug, tsis twv.

1. Rohdich, N., Roepke, RKA, & Zschiesche, E. (2014). Ib qho randomized, dig muag, tswj, thiab ntau- qhov chaw nyob rau hauv kev kawm piv rau kev ua tau zoo thiab kev nyab xeeb ntawm Bravecto (fluralaner) tawm tsam Frontline (fipronil) hauv flea- thiab zuam- dev kis. Parasites & Vectors, 7, 83.

2. Ozoe, Y., Asahi, M., Ozoe, F., Nakahira, K., & Mita, T. (2010). Antiparasitic isoxazoline A1H qhia antagonism ntawm GABA receptors txawv ntawm fipronil. Biochemical thiab Biophysical Research Communications, 391(1), 744–749.

3. Prichard, R., & Geary, T. (2008). Kev pom ntawm kev siv hluav taws xob ntawm moxidectin rau kev tswj cov kab mob parasitic nematodes nyob rau hauv lub ntsej muag ntawm kev txhim kho anthelmintic tsis kam. International Journal for Parasitology: Tshuaj thiab Tshuaj Tiv Thaiv, 1(1), 66–71.

4. Gassel, M., Wolf, C., Noack, S., Williams, H., & Ilg, T. (2014). Tus tshiab isoxazoline ectoparasiticide fluralaner: Xaiv inhibition ntawm arthropod -aminobutyric acid- thiab glutamate-gated chloride channels thiab insecticidal/acaricidal activation. Kab Biochemistry thiab Molecular Biology, 45, 111–124.

5. Casida, JE, & Durkin, KA (2013). Neuroactive insecticides: Lub hom phiaj, kev xaiv, kev ua haujlwm, thiab cov teebmeem thib ob. Kev Ntsuam Xyuas Txhua Xyoo ntawm Entomology, 58, 99–117.

6. Shoop, WL, Hartline, EJ, Gould, BR, Zakson-Aiken, M., & Olczyk, RG (2014). Kev tshawb nrhiav thiab hom kev ua ntawm afoxolaner, ib qho tshiab isoxazoline parasiticide rau dev. Veterinary Parasitology, 201(3–4), 179–189.