Aviptadilyog ib hom tshuaj uas muaj npe tshuaj N-[2-(aminoethyl)-1-methylethyl]-N-(2-chloroethyl) urea acetate. Nws yog ib hom vasodilator thiab yog dawb huv los yog yuav luag dawb hmoov. Molecular formula C147H238N44O42S CAS 40077-57-4. Nws muaj tsawg solubility hauv dej, tab sis tuaj yeem yaj zoo hauv cov kuab tshuaj organic xws li methanol thiab ethanol. Tsis tas li ntawd, nws solubility hauv dej kub yog siab dua li hauv dej txias. Nws muaj qee qhov kev ua tau zoo vim muaj cov ionizable pawg hauv nws cov qauv molecular. Nws tsis muaj ntxhiab tsw tshwj xeeb, tab sis nws cov tshuaj yuav muaj cov ntxhiab tsw tshwj xeeb vim muaj cov khoom siv ntxiv lossis lwm yam khoom siv. Feem ntau hais lus, vim muaj ntau pawg polar hauv cov qauv ntawm atepidil acetate, nws yuav raug hloov mus rau theem lossis sublimation ntawm qee qhov kub thiab txias. Nws yog tsuas yog siv rau hauv cov tshuaj pleev ib ce, xab npum, naj hoom thiab lwm yam khoom kom coj cov ntxhiab tsw qab ntxiag rau cov khoom.
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Customized Bottle Caps Thiab Corks:
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Tshuaj Formula |
C147H238N44O42S |
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Exact Mass |
3324 |
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Molecular Luj |
3326 |
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m/z |
3325 (100.0%), 3324 (62.9%), 3326 (52.1%), 3327 (41.3%), 3326 (26.9%), 3326 (15.1%), 3325 (9.5%), 3328 (9.4%), 3327 (8.6%), 3327 (7.9%), 3328 (6.7%), 3326 (5.4%), 3328 (5.4%), 3327 (4.7%), 3327 (4.5%), 3328 (4.5%), 3329 (3.6%), 3329 (3.1%), 3326 (2.8%), 3326 (2.7%), 3328 (2.4%), 3328 (2.3%), 3327 (2.2%), 3329 (1.9%), 3325 (1.7%), 3326 (1.6%), 3329 (1.5%), 3329 (1.5%), 3328 (1.3%), 3328 (1.3%), 3328 (1.2%), 3329 (1.1%), 3327 (1.1%), 3326 (1.1%), 3325 (1.0%) |
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Elemental Analysis |
C, 53.09; H, 7.21; N, 18.53; O, 20.20; S, 0.96 |
Aviptadilmuaj ntau lwm yam kev siv dua li siv los ua ib feem ntawm txuj lom thiab essence.
1. Kev kho mob teb
(1) Vasodilator: Nws yog ib hom vasodilator uas tuaj yeem ua rau cov leeg nqaij du thiab txo cov ntshav siab. Hauv kev kho mob ntshav siab thiab kab mob plawv, nws feem ntau yog siv los ua cov tshuaj ntxiv nrog rau lwm cov tshuaj tiv thaiv hypertensive los txhim kho cov nyhuv antihypertensive.
(2) Lub plab hnyuv secretion enhancer: tuaj yeem txhawb nqa cov kua hauv plab, pab txhim kho cem quav thiab plab hnyuv ua haujlwm. Hauv qee qhov kev kho cem quav, nws yog siv los ua ib qho tshuaj ntxiv los txhawb txoj hnyuv peristalsis thiab defecation.
(3) Gastrointestinal smooth muscle contraction inhibitor: Nws muaj cov nyhuv inhibitory ntawm kev cog qoob loo ntawm cov nqaij ntshiv plab thiab pab txo cov plab hnyuv thiab mob. Hauv kev kho mob ntawm qee yam kab mob hauv plab, nws yog siv los ua cov tshuaj adjuvant kom txo qhov mob thiab tsis xis nyob.
(4) Neuroendocrine modulators: Lawv muaj qee yam cuam tshuam rau cov kab mob neuroendocrine thiab tuaj yeem ua rau lub caj pas pituitary tso tawm cov tshuaj hormones xws li prolactin, kev loj hlob hormone, adrenocorticotropic hormone (ACTH), thiab luteinizing hormone (LH). Cov tshuaj hormones no muaj ntau yam physiological cuam tshuam rau tib neeg lub cev, yog li ntawd lawv muaj qee yam kev siv nyiaj hauv kev kho cov kab mob neuroendocrine.
(1) Kev tshawb fawb txog vascular biology: Nws muaj nuj nqis tseem ceeb hauv kev tshawb fawb vascular biology. Raws li vasodilator, nws tuaj yeem siv los kawm txog lub cev thiab cov tshuaj pharmacological ntawm cov leeg nqaij leeg, nrog rau tshawb nrhiav cov kab mob thiab cov tswv yim kho mob ntawm cov kab mob plawv.
(2) Kev tshawb fawb txog Neuroendocrine: Qhov cuam tshuam ntawm cov kab mob neuroendocrine ua rau nws muaj txiaj ntsig rau kev siv hauv kev tshawb fawb neuroendocrine. Kawm txog kev tswj hwm ntawm acetaminophen ntawm kev tso tawm cov tshuaj hormones tuaj yeem pab kom nkag siab tob txog cov kab mob thiab kev kho mob ntawm cov kab mob neuroendocrine.
(3) Pharmacological tshawb fawb: Raws li cov khoom muaj nyob hauv cov tshuaj, nws muaj txiaj ntsig tseem ceeb hauv kev tshawb fawb tshuaj. Kawm txog cov tshuaj pharmacological thiab cov yam ntxwv ntawm pharmacokinetic ntawm atepidil acetate tuaj yeem pab tshawb pom cov hom phiaj tshuaj tshiab thiab cov tswv yim kho mob.
(1) Kev tsim tshuaj pleev ib ce thiab naj hoom: Nrog cov ntxhiab tsw qab ntxiag, nws yog siv los ua txuj lom thiab cov khoom xyaw hauv cov tshuaj pleev ib ce thiab tshuaj tsw qab. Nws tuaj yeem muab ntxiv rau cov khoom siv tu tus kheej xws li cov khoom tu tawv nqaij, tshuaj zawv plaub hau, da dej gel, thiab lwm yam, muab cov ntxhiab tsw qab ntxiag thiab tsw qab.
(2) Khoom noj khoom haus additives: Lawv cov aroma thiab saj cov yam ntxwv ua rau lawv muaj qee yam kev siv tus nqi hauv kev lag luam khoom noj.Aviptadiltuaj yeem muab ntxiv ua zaub mov ntxiv rau dej haus, khoom qab zib, pastries, thiab lwm yam khoom noj los txhim kho lawv saj thiab tsw.
(3) Pharmaceutical kev lag luam: Raws li cov khoom muaj nyob hauv cov tshuaj, nws muaj txiaj ntsig tseem ceeb hauv kev lag luam kws tshuaj. Nws tuaj yeem siv los npaj cov tshuaj rau kev kho cov kab mob plawv, kab mob hauv plab, thiab kab mob neuroendocrine, muab cov neeg mob nrog cov phiaj xwm kho mob zoo dua.
Mechanism ntawm kev nqis tes ua thiab kev cai ntawm kev taw qhia txoj hauv kev
1. Mechanism ntawm kev tiv thaiv- qog ua haujlwm
Cov txheej txheem ntawm kev ua ntawm acetic acid dipeptidyl hauv kev kho mob qog noj ntshav yog feem ntau cuam tshuam nrog nws cov nyhuv inhibitory ntawm phosphatidylinositol 3-kinase (PI3K). PI3K yog ib qho tseem ceeb enzyme koom nrog hauv cellular signaling, thiab nws txoj kev ua kom txawv txav yog ze ze rau qhov tshwm sim thiab kev loj hlob ntawm ntau yam qog. Adipidil acetate, raws li ib tug me me molecule inhibitor ntawm PI3K, nthuav qhia siab xaiv thiab affinity ntawm alpha subtype ntawm PI3K.
Los ntawm inhibiting qhov kev ua ntawm PI3K, acetic acid dipeptidyl tuaj yeem thaiv qhov kev sib kis ntawm cov dej ntws hauv qab, yog li inhibiting kev loj hlob, tsiv teb tsaws, thiab ntxeem tau ntawm cov qog hlwb. Cov txheej txheem ntawm kev txiav txim no ua rau nws muaj peev xwm qhia tau tias muaj peev xwm kho tau tus nqi hauv kev mob qog noj ntshav mis, mob qog noj ntshav hauv lub taub hau thiab caj dab, mob qog nqaij hlav endometrial thiab lwm yam qog nqaij hlav.
Tshwj xeeb tshaj yog, acetic acid dipeptidyl txo qhov kev ua ntawm PI3K / Akt / mTOR teeb liab txoj hauv kev los ntawm inhibiting cov haujlwm ntawm PI3K. Txoj kev taw qhia no ua lub luag haujlwm tseem ceeb hauv kev loj hlob, ciaj sia taus, thiab ntxeem tau ntawm cov qog hlwb. Los ntawm inhibiting txoj kev taw qhia no, acetic acid dipeptidyl tuaj yeem cuam tshuam qhov kev loj hlob thiab kev cuam tshuam ntawm cov qog hlwb, yog li ua kom qeeb ntawm kev loj hlob thiab kev sib kis ntawm cov qog.
2. Vasodilation thiab kho cov txheej txheem ntawm cov kab mob pulmonary
Ntxiv nrog rau nws cov tshuaj tiv thaiv -cov nyhuv qog, acetic acid dipeptidyl kuj muaj cov nyhuv vasodilation thiab tuaj yeem siv los kho ntau yam kab mob ntsws. Nws cov nyhuv vasodilatory feem ntau yog ua tiav los ntawm inducing pulmonary vasodilation, inhibiting proliferation ntawm vascular du leeg hlwb (SMCs), thiab txo platelet aggregation.
Adipidil acetate tuaj yeem simulate vasodilation nyhuv ntawm VIP los ntawm activating VIP receptors ntawm vascular du leeg hlwb, txhawb cov efflux ntawm intracellular calcium ions, yog li txo qhov nro ntawm vascular du nqaij thiab ua tiav vasodilation. Cov txheej txheem ntawm kev ua haujlwm no tau qhia txog qhov muaj txiaj ntsig zoo hauv kev kho mob xws li pulmonary fibrosis, pulmonary arterial hypertension (PAH), thiab ua pa tsis ua haujlwm los ntawm SARS-CoV-2 nrog acetic acid dipeptidyl.
Hauv kev kho mob pulmonary fibrosis, acetic acid dipeptidyl tuaj yeem txhim kho cov hemodynamics ntawm cov hlab ntsha hauv cov hlab ntsha, txo qis qhov caws pliav thiab fibrosis ntawm lub ntsws cov ntaub so ntswg, thiab txo cov tsos mob ntawm cov neeg mob los ntawm nws cov vasodilatory nyhuv. Nyob rau hauv kev kho mob ntawm PAH, acetic acid dipeptidyl dilates pulmonary hlab ntsha, txo pulmonary artery siab, thiab txhim kho cov neeg mob txoj kev ua pa ua pa thiab ua hauj lwm kam rau ua. Hauv kev kho mob ua pa tsis ua haujlwm tshwm sim los ntawm SARS-CoV-2, acetanilide tuaj yeem txo qhov mob ntsws thiab kev puas tsuaj, thiab txhim kho cov neeg mob ua pa ua pa los ntawm nws cov tshuaj tiv thaiv kab mob thiab antioxidant.
Synergistic teebmeem nrog rau lwm yam tshuaj
Adipidil acetate tsis tsuas yog muaj txiaj ntsig ntawm kev siv ib leeg hauv kev kho mob qog noj ntshav, tab sis kuj tuaj yeem ua ke nrog lwm cov tshuaj tiv thaiv qog nqaij hlav los tsim cov teebmeem kev sib koom ua ke thiab txhim kho kev kho mob. Cov tswv yim kho mob ua ke no muab cov tswv yim tshiab thiab cov hau kev kho mob qog noj ntshav.
1. Synergistic nyhuv nrog tshuaj kho mob
Adipidil acetate tuaj yeem siv ua ke nrog cov tshuaj kws khomob ib txwm siv los txhim kho kev ua haujlwm ntawm cov tshuaj khomob los ntawm inhibiting kev loj hlob thiab kev cuam tshuam ntawm cov qog hlwb. Piv txwv li, hauv kev kho mob qog noj ntshav ntawm lub mis, opipidil acetate tuaj yeem siv ua ke nrog cov tshuaj khomob xws li fluoxetine txhawm rau txhawm rau txuas ntxiv kev vam meej tsis muaj sia nyob (PFS) ntawm cov neeg mob. Qhov kev sib koom ua ke no tuaj yeem ua tiav los ntawm inhibiting PI3K / Akt / mTOR txoj kev taw qhia thiab txo cov tshuaj tua kab mob.
2. Synergistic effect nrog cov tshuaj tsom
Adipidil acetate kuj tseem siv tau ua ke nrog cov tshuaj tsom mus ua kom muaj kev sib koom ua ke los ntawm kev ua haujlwm ntawm kev taw qhia sib txawv thiab lub hom phiaj. Piv txwv li, hauv kev kho mob cancer ntawm lub taub hau thiab caj dab, acetic acid dipeptidyl tuaj yeem siv ua ke nrog cov tshuaj tiv thaiv xws li EGFR inhibitors los txhim kho kev kho mob los ntawm inhibiting kev loj hlob thiab kev muaj peev xwm ntawm cov qog hlwb. Qhov kev sib koom ua ke no tuaj yeem ua tiav los ntawm inhibiting tus ntoo khaub lig- tham ntawm PI3K/Akt/mTOR signaling pathway thiab EGFR signaling pathway.
3. Synergistic nyhuv nrog immunotherapy
Nyob rau hauv xyoo tas los no, immunotherapy tau ua kom muaj kev vam meej hauv kev kho mob qog. Adipidil acetate kuj tseem siv tau ua ke nrog cov tshuaj tiv thaiv kab mob txhawm rau txhim kho kev kho mob los ntawm kev tswj cov qog microenvironment thiab txhim kho cov haujlwm ntawm lub cev tiv thaiv kab mob. Piv txwv li, hauv kev kho mob qog noj ntshav endometrial, acetate dipeptidyl tuaj yeem siv ua ke nrog cov tshuaj tiv thaiv kab mob xws li PD-1 inhibitors los txhim kho kev kho mob los ntawm inhibiting qog cell tiv thaiv kev khiav tawm thiab txhim kho lub cev tiv thaiv kab mob. Qhov kev sib koom ua ke no tuaj yeem ua tiav los ntawm inhibiting PI3K / Akt / mTOR kev taw qhia txoj hauv kev thiab tswj kev ua haujlwm thiab kev ua haujlwm ntawm lub cev tiv thaiv kab mob.
Cov txheej txheem ntawm kev siv cov tshuaj tiv thaiv acylation los ua cov tshuaj salicylic acid nrog acetic anhydride kom tau txais atepidil acetate tuaj yeem muab faib ua cov kauj ruam hauv qab no:
Salicylic acid dhau acylation cov tshuaj tiv thaiv nrog acetic anhydride los tsim atepidil acetate. Cov kev sib npaug tshuaj lom neeg tshwj xeeb yog:
C7H4O3+C4H6O2 → C11H12O5
Ua ntej, xyuas kom meej tias tag nrho cov khoom siv raw, cov tshuaj reagents, thiab cov cuab yeej rau cov tshuaj tiv thaiv yog npaj txhij. Qhov xav tau salicylic acid, acetic anhydride, catalyst, thiab hnyav yuav tsum ua tau raws li cov qauv tshuaj purity. Npaj cov tshuaj tiv thaiv kom tsim nyog kom lawv huv si thiab qhuav.
Dissolve salicylic acid thiab acetic anhydride hauv cov kuab tshuaj tsim nyog. Feem ntau, anhydrous ethanol lossis ether tuaj yeem xaiv los ua cov kuab tshuaj, uas pab txhawb kev nce qib ntawm cov tshuaj tiv thaiv. Sib tov cov kua qaub salicylic acid thiab acetic anhydride tov ua ke, kom ntseeg tau tias ob txoj kev daws tau zoo sib xyaw.
Ntxiv qhov tsim nyog tus nqi ntawm cov catalyst rau cov tshuaj tov los txhawb cov tshuaj tiv thaiv acylation. Cov catalysts muaj xws li concentrated sulfuric acid, phosphoric acid, los yog hydrogen chloride. Xaiv tus nqi tsim nyog ntawm cov catalyst ntxiv rau cov tshuaj raws li cov xwm txheej tshwj xeeb.
Nyob rau hauv qhov kev txiav txim ntawm lub catalyst, salicylic acid thiab acetic anhydride pib mus rau acylation cov tshuaj tiv thaiv. Thaum cov txheej txheem tshuaj tiv thaiv,aviptadil uaNws yog ib qho tsim nyog los tswj qhov kub thiab txias lub sij hawm cov tshuaj tiv thaiv los xyuas kom meej qhov kev vam meej ntawm cov tshuaj tiv thaiv. Acylation cov tshuaj tiv thaiv yog cov tshuaj tiv thaiv rov qab, thiab txhawm rau txhawb cov tshuaj tiv thaiv rau pem hauv ntej, cov dej tsim tawm hauv cov tshuaj tiv thaiv tuaj yeem raug tshem tawm raws sijhawm. Cov txheej txheem feem ntau suav nrog kev siv desiccants lossis ua haujlwm fractionation.
Tom qab cov tshuaj tiv thaiv tiav lawm, nws yog ib qho tsim nyog yuav tsum ua tom qab- kev kho thiab kev ua kom huv huv ntawm cov khoom tsim tawm. Feem ntau, extraction yog siv los rho tawm cov khoom los ntawm cov tshuaj tiv thaiv. Cov kuab tshuaj organic tsim nyog tuaj yeem siv rau kev rho tawm, thiab tom qab ntawd cov kuab tshuaj tuaj yeem rov qab los ntawm distillation lossis lwm txoj hauv kev kom tau txais cov khoom nyoos. Tsis tas li ntawd, cov khoom nyoos tuaj yeem raug ntxuav los ntawm txoj kev xws li recrystallization lossis kem chromatography kom tau txais siab -purity atepidil acetate.
Cov lus nug nquag
Aviptadil kho dab tsi?
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Aviptadil, ib daim ntawv hluavtaws ntawm vasoactive plab hnyuv peptide (VIP), tau txais kev tso cai US Food and Drug Administration (FDA) Fast Track Designation rau kev kho mob tseem ceeb ntawm COVID-19 nrog ua pa tsis ua haujlwm.
Puas yog aveptadil siv rau ARDS?
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304 stainless hlau ua tau raws li cov kev cai thoob ntiaj teb ntawm qib zaub mov, 316 stainless hlau tsis yog qib zaub mov lossis qib kho mob nkaus xwb. Txawm li cas los xij, kev siv qib kev kho mob no ua lub khob ntim khoom yuav tsis coj cov txiaj ntsig ntxiv rau txhua tus. Vim li cas thiaj hu 304 lossis 316? Qhov no feem ntau txhais raws li cov khoom muaj pes tsawg leeg. 316 stainless hlau tsis zoo ib yam li cov ntaub ntawv ntxhia, tom qab siv tau tuaj yeem tso qee yam khoom los txhawb kev nqus ntawm tib neeg.
Puas yog aviptadil yog ib qho tshuaj tiv thaiv - mob?
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Lub presumed therapeutic mechanism ntawm kev txiav txim ntawm inhaled aviptadil yog ib tug ua ke ntawm anti- inflammatory zog thiab induction ntawm tolerogenic tiv thaiv kab mob ntawm lub cev tiv thaiv kab mob nyob rau hauv lub ntsws.
Cim npe nrov: Aviptadil CAS 40077-57-4, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom