Aprepitant yog dab tsi?
Aprepitant hmoovyog dawb los yog me ntsis dawb crystal hmoov, uas yog ib yam tshuaj thiab insoluble nyob rau hauv dej. Lub solubility ntawm aripipitan nyob rau hauv dej yog tsawg heev ntawm pH 2 ~ 1 0, nrog ib tug Log P ntawm 4.8 ntawm pH 7.0. Me ntsis soluble hauv acetonitrile, me ntsis soluble hauv ethanol thiab isopropyl acetate, soluble hauv ethanol.
Aprepitant yog Neurokinin-1(NK-1) receptor antagonist, uas yog cov tshuaj tiv thaiv kab mob qog noj ntshav thiab ntuav cov khoom kho mob. Aprepitant muaj kev xaiv zoo rau tib neeg, tab sis tsis tshua muaj affinity rau 5- hydroxytryptamine, dopamine thiab corticosteroid receptors. Tshuaj P yog ib hom tachykinin (neurokinin), uas yog nyob rau hauv nruab nrab thiab peripheral paj hlwb neurons. Nws muaj feem xyuam rau ntau yam dej num, xws li ntuav, kev nyuaj siab, inflammatory mob thiab o ntawm lwm yam kab mob. Qhov kev txiav txim ntawm cov tshuaj P yog kho los ntawm NK-1 receptor, uas yog G protein receptor thiab txuas nrog phosphoinositide teeb liab txoj hauv kev. Aprepitant khi rau NK-1 receptor nyob rau hauv lub hlwb thiab thaiv cov receptor, yog li kho cov kab mob kho los ntawm cov tshuaj P. Aprepitant tuaj yeem xaiv los tiv thaiv kev sib xyaw ntawm cov tshuaj P thiab NK-1 receptor nyob rau hauv lub hauv paus paj hlwb kom nres. ntuav, thiab tuaj yeem siv rau xeev siab thiab ntuav los ntawm cov tshuaj khomob nruab nrab thiab siab emetic.
| Khoom npe | Aprepitant |
| CAS | 170729-80-3 |
| Cov mis mos molecular | C23H21F7N4O3 |
| Molecular hnyav | 534.43 |
| EINECS Number | 677-636-6 |
| Kev cia khoom | Muab kaw rau hauv qhuav, 2-8 degree |
| Melting point | 244-246 degree |
| Solubility | Soluble in DMSO(>25 mg/ml) |
| Qhov tshwm sim | Dawb rau beige hmoov |
| Kev sib hloov tshwj xeeb | D25 +69 degree (c=1 00 hauv methanol) |
| Qhov ntom | 1.51 ± 0.1 g / cm3 (Tshaj tawm) |
Dab tsi yog pharmacological kev txiav txim ntawm Aprepitant?
Nws thaiv qhov kev txiav txim ntawm cov tshuaj P los ntawm kev khi rau NK-1 receptor, uas feem ntau muaj nyob rau hauv lub hauv paus paj hlwb thiab nws periphery.Aprepitant hmoovtuaj yeem tuav NK-l receptors nyob rau hauv lub hlwb los ntawm cov ntshav-hlwb barrier, nrog siab xaiv thiab affinity, tab sis tsis tshua muaj affinity rau NK-2 thiab NK-3 receptors. Nyob rau tib lub sijhawm, kev sib raug zoo ntawm Aprepitant rau lub hom phiaj ntawm lwm cov tshuaj (xws li dopamine receptor thiab 5-HT3 receptor) siv los kho xeev siab thiab ntuav vim los ntawm kws khomob kuj tsawg heev, thiab nws cov txiaj ntsig ntawm kev txo qis xeev siab thiab ntuav yog zoo dua li lwm yam tshuaj. Cov khoom no tuaj yeem txhim kho qhov ua tiav cov lus teb ntawm qhov mob hnyav thiab qeeb xeev siab thiab ntuav vim los ntawm kev siv tshuaj khomob hauv cov qauv kev kho mob ntuav hnyav tshwm sim los ntawm kws khomob nrog 5- tryptamine 3(5-HT3) receptor blocker thiab dexamethasone . Aprepitant tuaj yeem cuam tshuam qhov ntuav ntuav thiab ntuav uas tshwm sim los ntawm Cisplatin hauv cov qauv tsiaj pub dawb. Ib koob tshuaj ua ntej lossis tib lub sijhawm nrog cisplatin. Aprepitant tuaj yeem txo cov tsos mob ntuav hauv 72 teev tom ntej; Tib lub sijhawm, Aprepitant tuaj yeem txhim kho nws cov nyhuv antiemetic los ntawm kev sib txuas nrog dexamethasone lossis 5-HT thiab receptor blocker ondansetron.
Khoom Specification
| Yam khoom | Specification | Cov txiaj ntsig |
| Qhov tshwm sim | Dawb los yog dawb crystalline hmoov | Dawb hmoov hmoov |
| Kev txheeb xyuas | Los ntawm IR | Ua raws |
| Los ntawm HPLC | Ua raws | |
| Solu bility | Dawb soluble nyob rau hauv dimethyl sulfoxide, insoluble hauv dej |
Ua raws |
| Kev sib hloov tshwj xeeb | {{0}} 0~+71.0 degree | {0}}.0 degree |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug rau 0.50% | 0.13% |
| Poob rau ziab | Tsawg dua lossis sib npaug rau 0.50% | 0.10% |
| Residue ntawm Ignition | Tsawg dua lossis sib npaug rau 0.10% | 0.06% |
| Organic impurities | Impurity AP {{0}}: Tsawg dua lossis sib npaug li 0.15% | ND |
| Impurity AP1: Tsawg dua lossis sib npaug rau 0.15% | ND | |
| Impurity AP2: Tsawg dua lossis sib npaug rau 0.15% | ND | |
| Desfluoro aprepitant: Tsawg dua lossis sib npaug rau 0.15% | ND | |
| Lwm tus neeg impurity: Tsawg dua lossis sib npaug rau 0.10% | 0.06% | |
| Tag nrho cov impurities: Tsawg dua lossis sib npaug rau 0.30% | 0.25% | |
| Assay | 98.0%~102.0% | 99.85% |
| Xaus: | Ua raws li kev lag luam specification. |
Lub luag haujlwm ntawm Aprepitant yog dab tsi?
Aprepitant hmoovyog ib qho tshuaj tiv thaiv qog noj ntshav nrog cov tshuaj tiv thaiv kab mob, tshuaj tiv thaiv kab mob, tshuaj tua kab mob, tshuaj tua kab mob antioxidant, thiab kev ua haujlwm hauv plab hnyuv txhim kho cov teebmeem thiab kev ua haujlwm.
1. Antiemetic:
Aprepitant tuaj yeem cuam tshuam qhov ntuav ntuav thiab ntuav los ntawm cisplatin, thiab txhim kho cov kev ua haujlwm antiemetic ntawm 5-HT3 receptor antagonist ondansetron thiab glucocorticoid dexamethasone ntawm ntuav los ntawm cisplatin. Yog li, Aprepitant tuaj yeem siv los txo cov tsos mob xeev siab thiab ntuav.
2. Anti-inflammatory:
Aprepitant muaj qee yam tshuaj tiv thaiv kab mob, uas tuaj yeem cuam tshuam kev loj hlob ntawm cov ntaub so ntswg granulation thiab tshem tawm cov lus teb inflammatory. Qhov no muaj qhov txo qis ntawm cov tsos mob inflammatory uas yuav tshwm sim hauv cov neeg mob qog thaum kho.
3. Anticoagulant:
Aprepitant muaj cov nyhuv anticoagulant thiab tuaj yeem txo cov ntshav viscosity. Cov viscosity siab tuaj yeem ua rau microcirculatory mob, thiab cov nyhuv anticoagulant ntawm aprepitant capsules pab txhim kho microcirculation.
4. Antioxidant:
Aprepitant muaj cov nyhuv ntawm kev tshem tawm cov dawb radicals, thiab tuaj yeem txo cov kev ntxhov siab oxidative los ntawm kev ntes cov dawb radicals.
5. Txhim kho plab hnyuv muaj nuj nqi: Aprepitant tuaj yeem ua rau cov ntshav plab zom mov, txo cov kua qaub hauv plab, thiab txhim kho plab hnyuv.
HTML5 atlas of Aprepitant
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Qhov txawv ntawm fosaprepitant thiab aprepitant yog dab tsi?
1. Cov khoom xyaw thiab cov teebmeem tseem ceeb
Fosaprepitant feem ntau yog siv los ua ib qho tshuaj antiemetic thiab muaj cov nyhuv tiv thaiv qog. Nws tuaj yeem siv los kho cov hlwb rov ua dua tshiab los ntawm kev txhim kho angiogenesis hauv cov qog nqaij hlav thiab ua kom cov tshuaj tiv thaiv qog nqaij hlav, yog li ua tiav cov nyhuv tiv thaiv qog.Aprepitant hmoovyog ib qho tshuaj tiv thaiv qog noj ntshav, feem ntau yog siv los tiv thaiv mob hnyav thiab qeeb xeev siab thiab ntuav thaum pib thiab rov kho cov tshuaj kho mob emetogenic heev los tiv thaiv qog.
2. Mechanism ntawm kev ua
Fosaprepitant ua rau cov qog nqaij hlav los ntawm nws cov txheej txheem tshwj xeeb ntawm kev ua, uas tuaj yeem cuam tshuam rau kev loj hlob thiab metastasis ntawm cov qog hlwb. Aprepitant feem ntau inhibits 5-hydroxytryptamine receptors nyob rau hauv neurons los inhibit lub excitability ntawm neurons rau kev kho mob qog nqaij hlav, thiab yog muab nyob rau hauv ua ke nrog rau lwm yam tshuaj antiemetic los tiv thaiv xeev siab thiab ntuav los ntawm kws khomob.
Kev Ua Haujlwm Biological ntawm Aprepitant:
| Piav | Aprepitant yog ib qho kev xaiv thiab muaj kev sib raug zoo neurokinin 1 receptor antagonist nrog Kd ntawm 86 pM. |
| Kev tshawb fawb hauv vitro | Aprepitant txo cov metabolic kev ua si nrog kwv yees li IC50 tus nqi ntawm 20μM. Aprepitant induces cell loj hlob inhibition thiab G1 cell voj voog ntes. Aprepitant ho induces apoptosis hauv Nalm-6 hlwb, uas yog kho los ntawm caspase-3 ua kom. Aprepitant (20μM) induces p53 tsub zuj zuj thiab kev qhia ntawm pro-apoptotic p53 hom phiaj noob. Aprepitant (1, 5, 10μM) inhibits tus kab mob HIV nyob rau hauv MDM los ntawm kev nyuaj siab thiab unsuppressed HIV-tsis zoo cov neeg ex vivo nyob rau hauv ib tug npaum li cas ntawm koob tshuaj. Tus nqi IC90 ntawm aprepitant yog sib npaug rau 10μM thiab IC50 tus nqi yog kwv yees li 5μM. |
| Hauv vivo kev tshawb fawb | Aprepitant tiv thaiv B. burgdorferi kab mob-induced nce hauv NK-1R qhia hauv NHPs hauv vivo. Kev kho mob Aprepitant tiv thaiv B. burgdorferi-induced nce hauv CCL2 protein ntau hauv cov kua cerebrospinal ntawm NHPs. Kev kho Aprepitant tiv thaiv B. burgdorferi-induced nce hauv CCL2 thiab CXCL13 mRNA qhia hauv dorsal cag ganglia ntawm NHPs thiab tiv thaiv B. burgdorferi-induced nce hauv CCL2, CXCL13, IL-17A, thiab IL-6 mRNA qhia nyob rau hauv tus txha caj qaum ntawm NHPs. Kev kho mob Aprepitant attenuates B. burgdorferi kab mob-vim txo qis hauv astrocyte kev ua si / tus lej. Aprepitant (10 mg / kg, ip) txo qis AMPH- thiab cocaine-induced CPP qhia thiab locomotor activation hauv nas. Nyob rau hauv sib piv, aprepitant ho txhim kho morphine-induced CPP qhia thaum tseem ceeb inhibiting morphine-mediated locomotor kev ua si nyob rau hauv nas. Aprepitant tsis induce CPP tseem ceeb los yog conditioned qhov chaw aversion los yog locomotor activation los yog inhibition. Aprepitant (125 mg / hnub, qhov ncauj) ua rau 1-cov ntaub ntawv txo qis hauv plasma qib ntawm tus kab mob RNA piv rau kev tswj tsis tau kho. |
| Kev sim ntawm tes | Cov nyhuv inhibitory ntawm aprepitant rau kev ua haujlwm metabolic ntawm Nalm{{0}} cov hlwb raug soj ntsuam los ntawm kev siv ntawm thiazolyl xiav tetrazolium bromide (MTT) los ntawm cov hlwb nyob. Cov noob tau cog rau hauv 96- cov phiaj zoo ntawm qhov ntom ntawm 5000 lub hlwb / qhov zoo. Tom qab kev kho mob nrog 5, 10, 15, 20, thiab 30 μM ntawm aprepitant rau 24, 36, thiab 48 h, cov hlwb tau txuas ntxiv nrog 100 μM MTT (0.5 mg / mL) ntawm 37 degree rau 3 h. Cov hlwb tsis kho tau txhais tias yog pawg tswj hwm. Tom qab solubilization ntawm precipitated formazan nrog 100 μL DMSO, qhov optical ntom tau ntsuas ntawm lub wavelength ntawm 578 nm siv ELISA nyeem ntawv. |
| Tsiaj sim | Kaum tsib rhesus liab tau tshuaj loog thiab inoculated intrathecally rau hauv cisterna magna nrog 1 × 108 siv tau spirochetes, whereas 5 rhesus liab tsis muaj kab mob thiab tau txais 1 mL ntawm RPMI 1640 nruab nrab tom qab tshem tawm ntawm qhov sib npaug ntawm CSF. Tsim kom muaj nyob rau hauv vivo B. burgdorferi tus kab mob tau lees paub los ntawm kab lis kev cai zoo los ntawm tsawg kawg ib qho kev kuaj mob ntawm cov nqaij mos. Thawj pab pawg tsiaj tau kawm rau 2 lub lis piam thiab suav nrog ob tus tsiaj tswj (ib qho uas tau kho nrog aprepitant), ob tug kab mob thiab cov tsiaj tsis kho, thiab ob tug tsiaj muaj kab mob kho nrog aprepitant. Cov tsiaj thib ob tau kawm rau 4 lub lis piam thiab suav nrog 3 tus tsiaj tswj (ib qho uas tau kho nrog aprepitant), 5 tus kab mob thiab cov tsiaj tsis kho, thiab 4 tus tsiaj muaj kab mob kho nrog aprepitant. Tsiaj txhu tau txais ib koob tshuaj txhua hnub ntawm aprepitant ntawm 28 ± 6 mg / kg ib hnub, thiab kev kho tshuaj tau pib 2 hnub ua ntej inoculation. Cov koob tshuaj no zoo ib yam nrog cov txheej txheem kws kho tsiaj rau cov tshuaj xaiv hauv NHPs, thiab lub sijhawm 4-lub lim tiam ntawm txoj kev tshawb no txwv tsis pub muaj kev txhim kho neuropathology uas tshwm sim 8 lub lis piam tom qab B. burgdorferi kab mob. |
| Cov ntaub ntawv |
[1]. Martinez AN, et al. Aprepitant txwv nyob rau hauv vivo cov lus teb neuroinflammatory hauv tus qauv rhesus ntawm Lyme neuroborreliosis. J Neuroinflamation. 2017 Peb 15; 14(1):37. [2]. Bayati S, et al. Inhibition ntawm tachykinin NK1 receptor siv aprepitant induces apoptotic cell tuag thiab G1 ntes los ntawm Akt / p53 axis hauv pre-B mob lymphoblastic leukemia hlwb. Eur J Pharmacol. 2016 Nov 15;791:274-283. [3]. Mannangatti P, et al. Cov teebmeem sib txawv ntawm aprepitant, ib qho chaw kho mob siv neurokinin -1 receptor antagonist ntawm qhov kev qhia ntawm kev mob siab rau lub hlwb tiv thaiv opioid nqi zog. Psychopharmacology (Berl). 2017 Feb; 234(4):695-705. [4]. Barrett JS, et al. Pharmacologic rationale rau NK1R antagonist, aprepitant li adjunctive therapy nyob rau hauv HIV. J Transl Med. Peb Hlis 26, 2016; 14(1): 148. |
Dab tsi yog kev ceev faj rau Aprepitant?
Aprepitant yog ib koob tshuaj CYP3A4 inhibitor thiab yuav tsum tau siv nrog ceev faj thaum siv nrog cov khoom uas feem ntau metabolized los ntawm CYP3A4; Qee cov tshuaj chemotherapy yog metabolized los ntawm CYP3A4.
Aprepitant tuaj yeem ua rau muaj qhov txo qis hauv kev sib piv thoob ntiaj teb normalized (INR) ntawm lub sijhawm prothrombin thaum siv nrog warfarin.
Kev ua tau zoo ntawm cov tshuaj tiv thaiv hormonal tuaj yeem txo qis thaum lub sijhawm thiab rau 28 hnub tom qab siv tshuaj aprepitant. Yog li ntawd, lwm txoj kev tiv thaiv kab mob los yog txoj kev cawm seej yuav tsum tau siv rau kev tiv thaiv kab mob thaum siv aprepitant thiab rau 1 lub hlis tom qab noj tshuaj aprepitant kawg.
Yuav ua li cas thiab qhov twg yuav Aprepitant Powder wholesale?
Koj tuaj yeem tso siab rau peb qhov kev txiav txim vim tias peb muaj cov ntaub ntawv zoo ntawm kev muag tshuaj raws cai.
Peb ua qhov kev kuaj xyuas ywj pheej ntawm txhua yam khoom thiab tom qab ntawd muag rau peb cov neeg siv khoom hwm.
Xa koj Cov Lus Nug kom paub meej ntxiv, Nyem email:allen@faithfulbio.comTam sim no.
Muaj ntau txoj kev xa khoom rau koj xaiv
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Tsheb thauj mus los |
Shipping txoj kev |
Cargo hnyav xav tau |
Qhov zoo |
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3-7 hnub |
DHL, Lub teb chaws Yelemees DHL, Lub teb chaws Yelemees DPD, |
Haum rau qis dua 50kg. |
Peb muaj warehouses nyob rau hauv lub teb chaws Yelemees thiab California, teb chaws USA, |
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7-15 hnub |
Los ntawm Cua |
Haum rau ntau tshaj 50kg. |
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15-60 hnub |
Los ntawm Hiav Txwv |
Haum rau ntau tshaj 500kg. |
Xa koj Cov Lus Nug kom paub meej ntxiv, Nyem email:allen@faithfulbio.comTam sim no.
Tsis lees paub: Cov ntawv luam tawm ntawm lub xaib no yog siv los txhawb kev sib pauv kev kawm thiab kev kawm, thiab tsis txhais hais tias lub vev xaib no pom zoo nrog nws cov kev xav lossis lees paub qhov tseeb ntawm nws cov ntsiab lus. Thov lim kom zoo. Yog tias koj ntseeg tias tsab xov xwm no ua txhaum, thov hu rau tus thawj tswj hwm. Peb tsis muaj lub luag haujlwm rau qhov tshwm sim ntawm kev siv cov ntaub ntawv thiab cov kev pabcuam hauv lub vev xaib no.
Nco tseg: Cov tshuaj no yuav tsum tau siv rau kev tshawb fawb nkaus xwb. Cov lus thov no tsis tau raug soj ntsuam los ntawm Food and Drug Administration. Thov nrog koj tus kws kho mob tham thiab kawm txog cov kev tshawb fawb muaj ua ntej siv lawv. Cov khoom no tsis yog tsim los kuaj xyuas, kho, kho, lossis tiv thaiv txhua yam kab mob.
Cim npe nrov: aprepitant hmoov cas 170729-80-3, Tuam Tshoj, lwm tus neeg, manufacturers, hoobkas, customized, lag luam wholesale, yuav, nqe, tej, ntshiab, tsim, luv nqi, muag, Tshuag, dawb qauv, raw hmoov, raw khoom, ua nyob rau hauv Tuam Tshoj