XEP-018 peptide, muab tau los ntawm cov nquag peptides ntawm marine cone snail venom, occupies ib qho tseem ceeb txoj hauj lwm nyob rau hauv lub teb ntawm molecular biology thiab neuroscience kev tshawb fawb vim nws tshwj xeeb molecular conformation thiab lub hom phiaj zog. Nws tus nqi tseem ceeb yog concentrated nyob rau hauv cov kev cai ntawm cov ion channel tshwj xeeb thiab nws daim ntawv thov tshwj xeeb raws li cov cuab yeej tshawb fawb. Hauv kev tsom xam qhov tob ntawm nws cov txheej txheem ntawm kev nqis tes ua thiab kev tshawb fawb muaj txiaj ntsig tsis tuaj yeem txhim kho kev nkag siab ntawm ion channel txoj cai lij choj, tab sis tseem muab cov cuab yeej siv tau zoo rau kev tshawb fawb hauv cov haujlwm muaj feem xyuam. Cov hauv qab no yuav muab cov ncauj lus kom ntxaws thiab nthuav dav nyob ib puag ncig nws cov txheej txheem tseem ceeb ntawm kev nqis tes ua thiab cov hom phiaj tshawb fawb tshawb fawb.
Khoom Description
XEP-018 COA
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| Certificate of Analysis | ||
| Compound npe | Mu-conotoxin | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 936616-33-0 | |
| Ntau | 33g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090066 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib qho impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500 ppm |
| Cia |
Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav, 2-8 degree |
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Kev tshuaj xyuas ntawm Core Mechanism ntawm XEP-018
Qhov tseem ceeb ntawm kev ua tau zoo ntawmXAB-018 peptidelus dag nyob rau hauv nws qhov tseeb thaiv cov nyhuv ntawm cov ion channel tshwj xeeb, thiab nws cov txheej txheem ua haujlwm muaj lub hom phiaj siab thiab tshwj xeeb. Tsis zoo li qhov dav -spectrum action hom ntawm ion channel modulators zoo tib yam, nws cov txheej txheem tuaj yeem decomposed los ntawm peb theem: lub hom phiaj molecular, txoj hauv kev ua, thiab cov yam ntxwv ua tau zoo. Cov ntsiab lus tshwj xeeb yog raws li hauv qab no:
Kev kaw tshwj xeeb ntawm qhov chaw tsom.
XEP-018 tuaj yeem txheeb xyuas kom raug thiab khi rau cov leeg pob txha pob txha hluav taws xob raws li sodium raws los ntawm nws qhov chaw nquag ntawm qhov chaw molecular. Cov channel no ua lub luag haujlwm tseem ceeb rau kev ua kom muaj zog hauv cov leeg nqaij pob txha, feem ntau yog lub luag haujlwm rau kev thauj mus los ntawm sodium ions, yog li pib cov txheej txheem kev hloov pauv ntawm cov leeg nqaij. Tsis zoo li lwm cov ion channel blockers, XEP-018 nthuav tawm cov kev xaiv siab hauv kev khi rau hom sodium channel thiab tsis muaj kev cuam tshuam rau lwm cov subtypes ntawm sodium channels hauv myocardial lossis neural cov ntaub so ntswg. Lub hom phiaj tshwj xeeb no kuj yog lub hauv paus rau nws txoj kev tswj hwm kev ua tau zoo.
Muaj tseeb thaiv txoj hauv kev rau kev thauj khoom ion.
Thaum XEP-018 khi rau voltage-gated sodium channels hauv cov leeg pob txha, nws lub cev thaiv cov ion permeable channel ntawm cov channel los ntawm kev hloov pauv hauv cov molecular conformation, yog li ncaj qha thaiv cov transmembrane influx ntawm sodium ions. Qhov kev nkag mus ib txwm muaj ntawm sodium ions yog qhov txuas tseem ceeb rau cov leeg nqaij pob txha los tsim kom muaj peev xwm ua tau zoo thiab ua tiav cov paj hlwb hloov pauv. Thaum cov txheej txheem no raug thaiv, cov teeb liab hluav taws xob kis tau los ntawm cov hlab ntsha mus rau cov leeg pob txha yuav raug txiav tawm, yog li inhibiting cov lus teb ntawm cov leeg pob txha. Txoj hauv kev ntawm qhov kev ua no tsis tuaj yeem thim rov qab, thiab qhov cuam tshuam thaiv tau zoo cuam tshuam nrog qhov concentration ntawm XEP-018.
Cov yam ntxwv tshwj xeeb ntawm kev ua haujlwm zoo.
Cov nyhuv thaiv ntawm XEP-018 muaj cov yam ntxwv ntawm qhov pib sai thiab ruaj khov. Hauv kev sim vitro, qhov tsis tshua muaj siab ntawm XEP-018 tuaj yeem thaiv cov sodium channel hauv lub sijhawm luv luv, thiab nws lub sijhawm ua haujlwm tuaj yeem hloov kho tau yooj yim los ntawm kev tswj hwm kev tswj hwm. Tsis tas li ntawd, nws txoj haujlwm muaj peev xwm hloov tau cov kev cai rov qab, thiab los ntawm cov kev cuam tshuam tshwj xeeb ntawm molecular, nws cov nyhuv thaiv ntawm sodium raws tuaj yeem txo tau. Qhov kev tswj xyuas no ua rau nws hloov tau yooj yim hauv cov ntawv thov tshawb fawb tshawb fawb thiab ua kom yooj yim rau kev soj ntsuam kev tshawb fawb ntsig txog kev tswj hwm dynamic.
Cov peev txheej ntawm cov ntaub ntawv hais los saum toj no yog:
Kenta Yamazaki Kev Tshawb Fawb Txog Kev Sib Raug Zoo ntawm Inductive Mechanism thiab Damage Resistance Mechanism [J]. Phau ntawv Journal of the Japanese Medical Association, 2005, 125 (3): 217-224
Lub Tsev Kawm Ntawv ntawm Lub Neej Kev Tshawb Fawb, Peking University Kev tshawb fawb tau nce qib ntawm kev siv hluav taws xob-gated sodium channel tshwj xeeb probes [J]. Kev nce qib hauv Biochemistry thiab Biophysics, 2024, 51 (7): 1389-1402
Cov yam ntxwv ntawm daim ntawv thov thiab tus nqi ntawm XEP-018 hauv kev tshawb fawb tshawb fawb
Raws li lub hom phiaj ntawm chav kawm ntawm bioactive peptides, XEP-018 tau dhau los ua cov cuab yeej tseem ceeb hauv kev tshawb fawb ion channel thiab tshawb nrhiav cov txheej txheem neuromuscular conduction vim nws qhov tshwj xeeb cuam tshuam rau cov hluav taws xob-gated sodium channel hauv cov leeg pob txha. Nws daim ntawv thov kev tshawb fawb tus nqi feem ntau yog nyob rau hauv qhov tshwj xeeb zoo ntawm cov cuab yeej sojntsuam, kev siv cov kev tshawb fawb tshwj xeeb, thiab kev txhim kho kev tshawb fawb, raws li hauv qab no:
Kev tshawb nrhiav tus nqi ntawm neuromuscular kis tau tus mob mechanism.
Neuromuscular conduction yog cov txheej txheem tseem ceeb uas tswj kev ua haujlwm ib txwm ua ntawm cov leeg pob txha, thiab qhov hluav taws xob -gated sodium channels hauv cov leeg pob txha yog cov nodes tseem ceeb hauv cov txheej txheem no. XEP-018 tuaj yeem pab cov kws tshawb nrhiav kom paub meej txog txoj hauv kev ua tiav ntawm kev ua haujlwm neuromuscular thiab tshawb nrhiav cov kev sib cuam tshuam ntawm ntau yam kev sib txuas hauv cov txheej txheem hloov pauv los ntawm kev thaiv cov sodium ion influx thiab txiav tawm kev xa xov hluav taws xob neural rau cov leeg. Tsis tas li ntawd, XEP-018 tuaj yeem siv los ua cov cuab yeej cuam tshuam hauv kev tshawb fawb txog kev cuam tshuam ntawm neuromuscular conduction abnormalities, simulating lub xeev ntawm channel dysfunction thiab muab cov qauv kev sim rau kev soj ntsuam cov pathogenesis ntawm cov kab mob ntsig txog, ntxiv nthuav cov kev tshawb fawb ciam teb ntawm neuromuscular biology.
Cov ntawv thov tseem ceeb ntawm kev tshawb fawb txog kev ua haujlwm ntawm cov leeg nqaij pob txha sodium channels.
Hauv kev tshawb nrhiav kev ua haujlwm ntawm qhov hluav taws xob-gated sodium channels hauv cov leeg pob txha, XEP-018 tuaj yeem ua lub cuab yeej tseem ceeb rau kev txheeb xyuas cov kev sib koom ua ke thiab kev ua haujlwm, cov txheej txheem thauj ion, thiab cov cai tswj hwm ntawm cov channel. Piv txwv li, los ntawm kev thaiv cov nyhuv ntawm XEP-018 ntawm sodium raws, cov yam ntxwv ntawm cov channel permeable pore qauv, kev faib tawm ntawm cov chaw nquag, thiab cov txheej txheem molecular ntawm kev ua kom channel thiab deactivation tuaj yeem raug txiav tawm rov qab; Nyob rau tib lub sij hawm, qhov concentration dependence ntawm nws cov nyhuv thaiv yuav siv tau los tshawb xyuas cov teebmeem ntawm cov channel kom muaj nuj nqis thiab qhov ntom ntom ntawm cov leeg pob txha excitation conduction, muab kev txhawb nqa tseem ceeb rau kev tshawb fawb txog cov leeg pob txha pob txha.
Lub ntsiab kom zoo dua ntawm tej molecular probes.
Raws li ion channel tshwj xeeb sojntsuam,XEP-018 peptideQhov txiaj ntsig zoo tshaj plaws nyob hauv nws qhov kev xaiv siab rau qhov hluav taws xob-gated sodium channels hauv cov leeg pob txha.
Nws tuaj yeem txheeb xyuas kom raug thiab khi rau cov phiaj xwm hauv cov txheej txheem ntawm tes, tshem tawm kev cuam tshuam los ntawm lwm cov ion channel thiab biomolecules.
Muab piv rau cov tshuaj soj ntsuam ib txwm muaj, XEP-018 muaj cov yam ntxwv ntawm cov ntim me me, muaj zog permeability, thiab siab affinity. Nws tuaj yeem nkag mus rau hauv cell barrier sai sai, khi rau lub hom phiaj hauv cov hlwb, thiab tsis ua rau muaj kev cuam tshuam tsis zoo rau lub cev ntawm lub cev, muab cov cuab yeej txhim khu kev qha rau kev kawm meej ntawm kev ua haujlwm ntawm lub hom phiaj.
Cov peev txheej ntawm cov ntaub ntawv hais los saum toj no yog:
Sigma Aldrich. XEP-018|Selective NaV1.4 Prohibitor|Product Information [R]. USA: Sigma Aldrich, 2024
Zhang Xav, Li Jianming Kev tshawb fawb nce qib ntawm bioactive peptides raws li ion channel sojntsuam [J]. Suav Journal of Bioengineering, 2023, 43 (11): 89-98
Thermo Fisher Kev Tshawb Fawb. Tus cwj pwm ntawm XEP-018 Kev khi rau pob txha pob txha Sodium Channels [R]. Tebchaws Asmeskas: Thermo Fisher Scientific, 2023
Hauv cov ntsiab lus, tus nqi tseem ceeb ntawmXEP-018 peptideyeej ib txwm tsom ntsoov rau ob qhov tseem ceeb. Ntawm qhov tod tes, nws yog nws cov txheej txheem thaiv qhov tseeb rau qhov voltage-gated sodium channels hauv cov leeg pob txha. Cov nyhuv thaiv no tsis yog qhov dav dav ion channel inhibition, tab sis tso siab rau nws qhov tshwj xeeb molecular conformation thiab active site kom ua tiav cov cim tshwj xeeb thiab lub cev thaiv cov phiaj xwm. Nws tsis tsuas yog ua kom muaj kev ruaj ntseg ntawm kev thaiv kev ua tau zoo, tab sis kuj zam tsis yog - tshwj xeeb cuam tshuam nrog ion raws hauv lwm cov ntaub so ntswg, ua kom pom qhov tseeb thiab tshwj xeeb ntawm nws cov kev cai molecular; Ntawm qhov tod tes, nws muaj txiaj ntsig tsis hloov pauv raws li kev tshawb fawb tshwj xeeb hauv kev tshawb fawb ion channel thiab tshawb nrhiav cov txheej txheem neuromuscular conduction.
Nrog nws cov phiaj xwm kev tswj hwm thiab hloov tau yooj yim, XEP-018 tau ua tiav tiav los ntawm cov kev txwv ntawm cov cuab yeej tshawb fawb ib txwm muaj xws li tsis muaj qhov tshwj xeeb thiab muaj zog cuam tshuam, dhau los ua cov cuab yeej tseem ceeb hauv kev tshawb fawb txog kev tshawb fawb.
Hauv cov ntawv thov kev tshawb fawb, nws tsis yog tsuas yog txhawb cov kws tshawb fawb zoo hauv - kev nkag siab tob txog cov yam ntxwv ntawm cov qauv, ion kev cai thauj mus los, thiab kev tswj hwm cov txheej txheem ntawm cov leeg nqaij sodium channel, qhia meej txog txoj hauv kev tseem ceeb thiab cov nodes tseem ceeb ntawm cov teeb liab xa mus rau hauv cov txheej txheem ntawm neuromuscular conduction, tab sis kuj muab cov txiaj ntsig zoo thiab txhim khu kev qha hauv kev tshawb fawb txog kev txhawb nqa thiab txhim khu kev qha{1p} teb, suav nrog kev tshawb nrhiav ion channel abnormality ntsig txog cov txheej txheem thiab kev tsim cov cuab yeej tshawb fawb tshiab.
Nws daim ntawv thov muaj peev xwm hauv molecular biology, neuroscience, thiab lwm yam kev tshawb fawb txog kev tshawb fawb yog qhov muaj txiaj ntsig, thiab nws muaj qhov dav thiab ntev -cov ntawv thov tshawb fawb txog kev tshawb fawb.
Cov ntaub ntawv
Phau ntawv Journal of Neurophysiology. Selective Blockade of Skeletal Muscle Sodium Channels los ntawm XEP-018: Ib Lub Cuab Yeej Tshiab rau Kev Tshawb Fawb Neuromuscular [J]. 2018, 120(4): 1789-1800.
Hideki Kobayashi, Misaki Sato Taw Qhia rau Kev Siv Cov Khoom Siv Induction [J]. Phau ntawv Journal of Neuroscience, 2022, 66 (2): 97-105
Frontiers hauv Physiology. XEP-018 ua ib qho cuab yeej los txiav cov pob txha pob txha Sodium Channel Function[J]. 2021, 12:689245.
Shanghai Institute of Life Sciences, Suav Academy ntawm Kev Tshawb Fawb Kev Tshawb Fawb Kev Tshawb Fawb ntawm XEP-018 hauv kev tshawb nrhiav cov txheej txheem ntawm kev sib kis ntawm neuromuscular [J]. Life Sciences, 2024, 36 (4): 321-330
FAQ
XEP-018, tseem hu ua μ-conotoxin Cn IIIC, yog biomimetic ntawm ntuj cone peptides los ntawm cov tshuaj lom marine cone snails (Conus consors). Biologically, nws ua hauj lwm raws li ib tug modulator ntawm neuromuscular kis tau tus mob, raws li zoo raws li ib tug muaj zog thiab tshwj xeeb blocker ntawm lub voltage-gated sodium channel Nav 1.4.
Cov nyhuv thaiv ntawm XEP-018 muaj qhov tshwj xeeb thiab qhov tseeb, uas txawv ntawm qhov kev txwv dav dav ntawm cov tswj hwm zoo tib yam. Nws tso siab rau nws qhov tshwj xeeb molecular conformation thiab active site kom raug txheeb xyuas thiab khi rau voltage-gated sodium channels hauv pob txha pob txha. Los ntawm lub cev thaiv cov channel channel, nws thaiv kev nkag mus ntawm sodium ions, ua kom ruaj khov thaiv kev ua tau zoo thiab ua kom tsis txhob cuam tshuam nrog lwm cov sodium channel subtypes hauv myocardial thiab neural cov ntaub so ntswg, ua kom pom muaj zog molecular kev tswj tshwj xeeb.
Cim npe nrov: xep-018 peptide, Tuam Tshoj xep-018 peptide manufacturers, lwm tus neeg
