Mob neuralgia, mob visceral, ntxhov siab vim, thiab kev quav yeeb tshuaj tau ntev tsis muaj kev cuam tshuam zoo thiab muaj txiaj ntsig. Ib txwm siv μ-opioids yog nquag rau kev quav tshuaj thiab muaj kev pheej hmoo siab ntawm kev kam rau siab, thaum lub κ-opioid receptor pathway tau dhau los ua cov kev tshawb fawb tseem ceeb rau tom ntej - tiam analgesia thiab mus ob peb vas kev cai.Dynorphin A (1-13) Acetate, nrog ib tug purity Ntau dua los yog sib npaug rau 99.0%✨, yog ib qho endogenous 13-peptide κ-opioid receptor heev xaiv agonist acetate polypeptide raw khoom. Kev vam khom rau nws lub hom phiaj siab κ receptor, tsis muaj zog μ receptor kev ua, tsis muaj kev quav yeeb quav tshuaj, thiab ua ke cov tshuaj tua kab mob thiab tiv thaiv kev ntxhov siab, nws tau siv dav hauv kev tshawb fawb thiab kev loj hlob ntawm neuropharmacology, mob mechanisms, mob hlwb, thiab kev cuam tshuam kev quav yeeb quav tshuaj.
🧩 Basic linear 13-peptide acetate backbone
Dynorphin A (1-13) Acetatemuaj cov amino acid sequence Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys mole CH, C₇₄H₁₃₀N₂₃O₁₆, molecular hnyav 1603.06, thiab tshwm li cov hmoov dawb lyophilized. Nws purity ntau dua los yog sib npaug rau 99.0%, nrog ib qho impurities Tsawg dua lossis sib npaug li 0.15%, noo noo tsawg dua lossis sib npaug rau 4.0%, thiab endotoxin<0.1 EU/mg. It meets USP peptide raw material, EP pharmacopoeia, and cGMP research-grade peptide standards. The molecule consists of an N-terminal receptor core binding region, a middle arginine-rich basic region, a C-terminal flexible regulatory peptide segment, and an acetate salt-forming group. As a natural endogenous dynorphin active fragment, it exhibits higher stability and stronger κ-receptor selectivity compared to the full-length dynorphin, making it a benchmark molecule for research-grade opioid peptides.
The N-terminal Tyr-Gly-Gly-Phe-Leu pentapeptide sequence is the core functional region for activating the κ-opioid receptor. This conserved sequence is homologous to other endogenous opioid peptides. The phenolic hydroxyl group of tyrosine residues and the hydrophobic side chain of phenylalanine can precisely embed into the extracellular domain of the κ receptor, forming a stable network of hydrophobic interactions and hydrogen bonds. The 99.0% high-purity raw material is strictly controlled with amino acid deletions, oxidation, and deamination impurities ≤0.1%, and sequence integrity >99.5%. Hauv vitro receptor binding tests qhia tau hais tias nws txoj kev sib raug zoo rau tib neeg κ-opioid receptors ntau dua li qhov ntawd rau μ thiab δ receptors, nthuav tawm lub hom phiaj zoo tshaj plaws thiab zam qhov kev pheej hmoo ntawm kev quav yeeb quav tshuaj cuam tshuam nrog kev tawm ntawm - cov txiaj ntsig ntawm cov tshuaj opioid peptides. Khoom-theem peptide synthesis siv Fmoc lub tswv yim, ua kom muaj kev sib xyaw ua ke thiab acetate ntsev tsim, ua rau muaj kev sib txuam zoo heev - rau -batch stability.
Kev nruam arginine- cheeb tsam nplua nuj nyob rau hauv nruab nrab muab lub zog zoo, txhim kho peptide cov dej solubility thiab txhim kho nws cov electrostatic adsorption rau cell membranes, txhawb cov molecular tsub zuj zuj nyob rau hauv nruab nrab thiab peripheral mob neurons. High- ceev ceev yooj yim amino acids tiv thaiv sai hydrolysis los ntawm aminopeptidases thiab carboxypeptidases, ho ncua lub ib nrab -lub neej piv rau luv luv - saw opioid peptides. Qhov no tso cai rau lub sijhawm ntev ntawm kev ua haujlwm hauv cerebrospinal kua thiab cov ntaub so ntswg, ua rau nws tsim nyog rau kev sim hauv vitro cell thiab hauv vivo tsiaj kev tshawb fawb txog tshuaj.
C-terminal saj zawg zog tswj peptide tuaj yeem ua tau zoo- kho qhov kev ua kom lub cev ua kom zoo, txo qis kev ua haujlwm tsis muaj zog ntawm μ-opioid receptors thiab ntxiv dag zog rau κ receptor tshwj xeeb. Nws kuj tseem koom nrog hauv kev tswj hwm tus nqi qis G protein qhia txoj hauv kev tsis ncaj ncees, nyiam ua rau Gi/O protein inhibitory txoj hauv kev, txo kev kam rau siab thiab cov kev mob tshwm sim los ntawm -arrestin txoj hauv kev, muab cov qauv tsim rau qis -kev quav tshuaj quav cawv. Cov qauv hloov pauv no tseem tso cai rau cov molecule hloov mus rau ntau txoj hauv kev tswj hwm, tswj kev ua haujlwm ruaj khov nrog kev siv tshuaj intraventricular, intrathecal, thiab kev tswj hwm subcutaneous.
Cov pab pawg acetate salting optimizes peptide cov khoom-lub xeev stability thiab dej solubility, neutralizes peptide tus nqi pib, tiv thaiv kev sib sau thiab degradation thaum khaws cia, thiab txo cov hygroscopicity ntawm lyophilized hmoov. Tom qab 6 lub hlis ntawm kev ntsuas kev ruaj ntseg ntawm 40℃/ 75% RH, purity txo yog<0.2%, allowing for long-term storage. The acetate form can also improve the dissolution rate of peptides in physiological buffer solutions, making it suitable for scientific research experiments such as cell incubation and animal drug administration.
🔧Targeting κ-opioid receptors kom ua tiav ntau-txoj kev tswj lub cev
Dynorphin A (1-13) Acetatemuaj cov txheej txheem sib txawv kiag li ntawm μ-receptor agonists xws li morphine thiab fentanyl. Nws cov txheej txheem tseem ceeb suav nrog kev xaiv ua kom muaj zog ntawm lub hauv paus thiab cov khoom siv peripheral κ-opioid receptors, inhibiting mob teeb liab kis, tswj dopamine thiab norepinephrine tso, thiab exerting analgesic, tiv thaiv- ntxhov siab vim, tiv thaiv- kev ntxhov siab, thiab nqi zog-inhibiting Nws tsis muaj qhov tseem ceeb ua pa nyuaj siab lossis muaj zog ntxiv. Nws 99.0% ultra- siab purity ua kom muaj kev ncaj ncees thiab kev ruaj ntseg ntsev, tso cai rau kev txiav txim siab meej thiab tswj tau raws li txoj hauv kev, ua rau nws tsim nyog rau hauv - qhov tob ntawm kev tshawb fawb neuropharmacological mechanism.
Tom qab kev tswj hwm, cov peptide nyiam tshaj plaws hauv qhov mob - thiab kev xav- tswj lub paj hlwb xws li lub dorsal horn ntawm tus txha caj qaum, periaqueductal grey teeb meem ntawm midbrain, amygdala, thiab hypothalamus. Nws tshwj xeeb khi rau κ-opioid receptors, ua kom lub Gi/O protein signaling pathway, inhibiting adenylate cyclase kev ua, kaw voltage-gated calcium channels, thiab qhib cov poov tshuaj. Qhov no ua rau hyperpolarization ntawm mob neurons, ncaj qha thaiv kev tso tawm ntawm qhov mob-inducing neurotransmitters xws li tshuaj P thiab CGRP, thiab zoo inhibiting qhov uptake ntawm neuropathic mob thiab visceral mob signals.
Ntawm qhov nruab nrab nqi zog theem, peptide no tuaj yeem cuam tshuam qhov txawv txav ntawm dopamine tso tawm hauv cov kab ke mesolimbic thiab txo qis cov nqi zog hauv Circuit Court. Tsis zoo li dopamine - nce mechanism ntawm μ- receptor agonists, nws tsis tsim euphoria, yog li zam kev quav yeeb tshuaj, kam rau ua, thiab kev vam khom ntawm lub hauv paus. Nws kuj tseem tuaj yeem txo cov tshuaj - nrhiav tus cwj pwm rau yeeb tshuaj yeeb thiab tshuaj opioids, ua rau muaj peev xwm tiv thaiv kev quav yeeb quav tshuaj.
Los ntawm kev tswj cov hypothalamus-pituitary-adrenal axis, nws inhibits qhov tso tawm ntawm corticotropin- tso cov tshuaj hormones, txo cov qib cortisol, thiab tawm dag zog los tiv thaiv- ntxhov siab vim, tshuaj tiv thaiv kev nyuaj siab, thiab kev ntxhov siab ntev - txo cov teebmeem. Nws muaj kev tswj xyuas cov txiaj ntsig ntawm kev tshaj tawm -kev nyuaj siab ntxhov plawv thiab kev ntxhov siab ntev ntev- cuam tshuam txog kev puas siab puas ntsws, thiab tuaj yeem txhim kho cov teeb meem kev xav uas cuam tshuam nrog qhov mob.
Hauv cov ntaub so ntswg peripheral, nws tuaj yeem qhib κ-receptors ntawm dorsal cag ganglia, pob qij txha, thiab plab hnyuv mucosa, inhibiting qhov tso tawm ntawm cov kab mob hauv zos thiab txo cov mob visceral. Tib lub sijhawm, nws tsis cuam tshuam rau lub plab zom mov, thiab cov kev mob tshwm sim peripheral xws li cem quav thiab xeev siab yog qis dua li cov tshuaj opioids.
Ntev- siv sijhawm ntev tsis ua rau muaj kev cuam tshuam sai ntawm κ- receptors. Cov tshuaj tiv thaiv kab mob ruaj khov thiab mus ob peb vas- tswj kev cuam tshuam txawm tias tom qab kev tswj hwm tas mus li, tsis muaj qhov ua siab ntev. Nws yuav luag tsis muaj kev cuam tshuam rau cov hlab plawv thiab cov chaw ua pa, thiab nws txoj kev nyab xeeb yog qhov zoo tshaj rau cov tshuaj opioid analgesics, muab cov qauv zoo tagnrho rau kev txhim kho cov tshuaj kho mob tshiab.
💊 Cov cuab yeej tshawb fawb rau kev tshawb fawb txog kev quav tshuaj thiab kev tiv thaiv kab mob
Qhov tseem ceeb siv ntawmDynorphin A (1-13) AcetateHauv kev tshawb fawb tshawb fawb yog ib qho kev xaiv agonist ntawm κ opioid receptor thiab cov cuab yeej rau kev kawm txog kev quav tshuaj. Hauv kev tshawb fawb txog tshuaj dependence, no peptide yog dav siv los simulate lub siab lub ntsws tsis zoo thaum tshem tawm. Hauv morphine-cov nas nyob ntawm, kev txhaj tshuaj intraventricular ntawm Dynorphin A (1-13) ua rau muaj cov tsos mob zoo li tshem tawm thiab txhim kho kev mob siab rau. Cov teebmeem no tuaj yeem thim rov qab los ntawm κ antagonists, tawm tswv yim tias overactivation ntawm κ receptors koom nrog hauv kev cuam tshuam ntawm kev tshem tawm opioid. Qhov kev tshawb pom no muab lub hom phiaj tshiab rau kev tsim tshuaj los kho cov tshuaj dependence.
Hauv kev tshuaj ntsuam pharmacological rau cov tshuaj tiv thaiv kev ntxhov siab thiab kev ntxhov siab, Dynorphin A (1-13) tau siv dav los ua kev tswj hwm zoo. Nyob rau hauv qhov kev ntsuam xyuas tus Tsov tus tw los yog yuam ua luam dej, intraventricular los yog lateral ventricle txhaj ntawm no peptide koob - nyob ntawm tsub kom lub sij hawm immobility, ua raws li kev nyuaj siab - zoo li phenotype. Qhov kev nyuaj siab no tuaj yeem thaiv los ntawm κ-receptor antagonists; Yog li ntawd, ntau cov tshuaj tiv thaiv kev nyuaj siab tsom rau κ receptors siv cov nyhuv ntawm dynorphin A (1-13) ua tus qauv rau kev ntsuas kev ntseeg siab ntawm kev tshuaj ntsuam xyuas. Hauv kev ntxhov siab neurobiology, dynorphins yog tus neeg nruab nrab tseem ceeb ntawm kev ntxhov siab. Kev ntxhov siab txog kev ntxhov siab ntev tuaj yeem txhim kho dynorphin Ib qho kev qhia hauv hippocampus, tsav kev zam kev sib raug zoo thiab anhedonia. Cov peptide no yog siv rau hauv microdialysis lossis microinjection rau hauv ib cheeb tsam ntawm lub hlwb los kawm txog kev sib raug zoo ntawm kev ntxhov siab hauv cov cheeb tsam ntawm lub hlwb.
Hauv thaj tsam ntawm kev tiv thaiv neuroprotection, lub luag haujlwm ntawm Dynorphin A (1-13) Acetate yog qhov tsis txaus ntseeg. Qee cov ntaub ntawv tshaj tawm tias thaiv κ receptors hauv cerebral ischemia qauv tuaj yeem txo qhov ntim ntawm infarct, qhia tias kev tso tawm ntawm endogenous dynorphins exacerbates ischemic puas; Txawm li cas los xij, lwm cov kev tshawb fawb tau pom tias qis - koob tshuaj dynorphin A (1-13) tiv thaiv cov neurons los ntawm kev puas tsuaj los ntawm hypoxic los ntawm inhibiting calcium influx thiab scavenging dawb radicals. Qhov kev cuam tshuam dual no ua rau peptide no yog "ob-edged ntaj" hauv kev kawm txog cov txheej txheem ntawm kev mob stroke. Hauv cov qauv kev raug mob neurological, Dynorphin A (1-13) Acetate koom nrog cov txheej txheem pathological ntawm kev raug mob thib ob. Dynorphin qhia yog upregulated tom qab tus txha caj qaum raug mob, thiab κ antagonists tuaj yeem txhim kho lub cev muaj zog rov ua haujlwm. Yog li, cov peptide no tau siv los kawm txog lub luag haujlwm pathophysiological ntawm endogenous opioid system tom qab raug mob qaum qaum.
Hauv kev tshawb fawb tsis ntev los no hauv 2026, cov kws tshawb fawb tau siv optogenetics ua ke nrog microinjection ntawm dynorphin A (1-13) los piav qhia seb cov neurons qhia dynorphin hauv cov nucleus accumbens koom ua ke aversion signals. Cov kev tshawb pom no muab cov pov thawj tseem ceeb rau kev nkag siab txog kev quav tshuaj thiab khoom plig circuits, qhia tias daim ntawv thov tus nqi ntawm cov peptide hauv neuroscience txuas ntxiv mus.
🔭 Kev txhim kho kev ruaj ntseg thiab kev xa khoom hauv nruab nrab
Cov teeb meem tseem ceeb hauv kev tshawb fawb daim ntawv thov ntawm Lynorphin A (1-13) Acetate dag nyob rau hauv peptide's nyob rau hauv vivo instability (tsis tshua muaj luv luv ib nrab-lub neej) thiab nws cov khoom xa mus rau hauv nruab nrab paj hlwb. Hloov cov glycine ntawm qhov thib ob lossis thib peb txoj haujlwm nrog D-amino acid yog ib lub tswv yim zoo rau kev txhim kho peptide metabolic stability. Tocris Biosciences 'D-Arg- hloov pauv cov analogues ntawm Lynorphin A (1-13) nthuav tawm lub sijhawm ntev ib nrab-lub neej hauv ntshav plasma thaum khaws cov receptor zoo affinity. Cov analogs no nquag siv hauv kev sim xav tau ntev-acting κ receptor blockade.
Hauv kev tshawb nrhiav cov tshuaj cyclization thiab conformational locking, cyclizing linear Lynorphin A (1-13) Acetate ntawm disulfide los yog amide bonds yog ib qho kev tshawb fawb tawm tshiab rau kev txhim kho nws cov khoom lom. Txawm hais tias cyclization tuaj yeem hloov kho nws cov receptor selectivity, nws cov txheej txheem biology muab cov qauv tseem ceeb rau kev daws cov qauv siv lead ua ntawm κ receptor-ligand kev sib cuam tshuam complex, paving txoj kev rau kev loj hlob ntawm tsis yog -peptide κ agonists / antagonists. Hais txog kev xa khoom siv thev naus laus zis, vim nws qhov muaj zog hydrophilicity thiab tus nqi zoo, Denorphin A (1-13) tsis tuaj yeem nkag mus rau cov hlab ntsha-hlwb tsis zoo. Hauv cov kev tshawb fawb, kev tswj hwm tus kab mob los ntawm kev txhaj tshuaj intraventricular lossis intrathecal feem ntau xav tau, txwv nws txoj kev loj hlob raws li tus neeg sib tw tshuaj. Tam sim no, kev tswj xyuas qhov ntswg tau raug tshawb nrhiav rau kev xa tawm κ peptides, tab sis nws txoj kev xa khoom tseem qis dua li kev tswj hwm hauv nruab nrab.
Hais txog kev siv thev naus laus zis, derivatives ntawm Denorphin A (1-13) Acetate tau tsim los ua κ receptor tracers rau positron emission tomography (PET). Los ntawm chelating radionuclides ntawm cov chaw tshwj xeeb ntawm peptide, tsis yog -kev saib xyuas ntawm κ receptor faib thiab nyob hauv cov tsiaj muaj sia tuaj yeem ua tiav, uas yog qhov tseem ceeb rau kev ua kom ceev cov kev kho mob txhais cov tshuaj κ-targeted tshuaj.
Raws li lub siab -purity reagent, Denorphin A (1-}13) Acetate yog ib qho khoom sawv cev ntawm cov khoom sib txuas ntawm cov khoom sib txuas hauv qib peptide. Nws cov kab ke ntev thiab ntau qhov txiaj ntsig zoo ntawm cov amino acids tso siab rau kev ua kom zoo thiab ua kom huv thaum lub sijhawm ua ke. Rov qab-theem siab-kev ua haujlwm ua kua chromatography (RP-HPLC) yog ib kauj ruam tseem ceeb hauv kev ua kom huv huv, yuav tsum muaj kev tswj hwm nruj ntawm cov tshuaj endotoxin kom tau raws li kev sim ntawm cov kab lis kev cai ntawm tes thiab hauv vivo txhaj. Cov tuam txhab lag luam thoob ntiaj teb muab cov khoom lag luam tau lees paub los ntawm HPLC thiab huab hwm coj spectrometry, nrog cov ntaub ntawv qhia meej txog bioactivity.
🧬 Xaus
Dynorphin A (1-13) Acetate, raws li kev xaiv agonist ntawm lub ntuj endogenous κ-opioid receptor, muaj cov tshuaj sib txawv ntawm cov tshuaj muaj zog, tiv thaiv- ntxhov siab, tiv thaiv -kev quav yeeb quav tshuaj, thiab muaj kev nyab xeeb qis- ua rau nws muaj txiaj ntsig zoo {{7} 13-peptide linear conserved sequence, yooj yim enrichment qauv, acetate-stabilized hloov kho, thiab meej lub hom phiaj ntawm κ-receptors. Nws muaj txiaj ntsig zoo heev hauv kev tshawb fawb hauv paus thiab kev tsim tshuaj tshiab rau kev cuam tshuam hauv kev mob neuropathic, kev nyuaj siab, thiab kev quav tshuaj.
Raws li tus neeg muag khoom ntawmDynorphin A (1-13) Acetate, peb nkag siab txog qhov tseem ceeb ntawm cov saw hlau ruaj khov hauv kev sib tw ua lag luam. Peb cov txheej txheem kev tsim khoom thiab cov khoom lag luam tswj xyuas kom cov khoom siv tas mus li txawm tias cov khoom muag sib txawv. Thov mus saib peb cov khoom lag luam nthuav dav thiab sib tham txog koj qhov kev xav tau nrog peb cov kws tshaj lij ntawmallen@faithfulbio.com.
Cov ntaub ntawv
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