Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm acridine cas 260-94-6 hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo acridine cas 260-94-6 muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Acridineyog ib qho organic compound teej tug mus rau chav kawm ntawm aromatic amines. Akridin muaj cov tshuaj formula C13H9N thiab qhov hnyav molecular yog 179.22. Nws muaj lub hauv paus pyridine nplhaib thiab ob lub nplhaib benzene, tsim ib daim duab peb sab. Cov qauv no muab akridin tshwj xeeb lub cev thiab tshuaj. Akridin feem ntau yog daj mus rau daj- xim av crystalline hmoov nrog lub melting point ntawm li 106 ~ 109℃thiab lub boiling point ntawm 346℃. Nws muaj zoo solubility nyob rau hauv cov organic solvents xws li dioxane. Akridin muaj ib qho℃ntawm alkalinity, thiab nws tuaj yeem hnov mob nrog cov kua qaub los tsim cov ntsev. Nws tuaj yeem ua rau tshuaj lom neeg nrog qee cov reagents los ntawm kev hloov pauv, ntxiv thiab oxidation.
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Akridin nws tus kheej yuav tsis raug siv ncaj qha raws li cov khoom lag luam, tab sis nws yuav raug siv los ua cov khoom siv raw lossis nruab nrab hauv qee qhov tshwj xeeb lossis cov khoom lag luam. Hauv chav kuaj, akridin tuaj yeem siv ntau yam kev tshawb fawb thiab kev sim tshuaj, suav nrog cov organic synthesis, photophysical thiab photochemical kev tshawb fawb.
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Tshuaj Formula |
C13H9N |
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Molecular Luj |
179.22 |
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Exact Mass |
179.07 |
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m/z |
179.07 (100.0%), 180.08 (14.1%) |
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Elemental Analysis |
C, 87.12; H, 5.06; N, 7.82 |
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Melting point |
106-109 degree |
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Boiling point |
346℃(lit.) |
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Qhov ntom |
1,005 g / cm3 |
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Cia tej yam kev mob |
Lub tub yees |
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Solubility |
Dioxane: 0.1 g / ml, ntshiab |
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Flash Point |
346 degree |
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Index Ntawm Refracction |
1.7270 (kwv yees) |
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Acidity Coefficient (pKa) |
5.58 (ntawm 20 degree) |
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Daim ntawv |
Crystalline hmoov |
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Xim |
Yellow rau yellow-xim av |
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Dej Solubility |
57.35 mg / L (24 ºC) |
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Kev ruaj ntseg |
ruaj khov. Hluav taws kub. Incompatible nrog muaj zog oxidizing neeg sawv cev. |
Acridineyog ib hom kab mob uas muaj ntxhiab heterocyclic tsim los ntawm kev sib xyaw ntawm ob lub benzene rings thiab nitrogen -muaj pyridine nplhaib. Nws tuaj yeem muab rho tawm los ntawm cov thee tar, feem ntau yog concentrated nyob rau hauv cov roj anthracene, nrog rau cov ntsiab lus ntawm 0.6%, thiab kuj tuaj yeem tau los ntawm cov tshuaj synthesis. Qhov no zoo li yooj yim organic molecule, vim nws qhov tshwj xeeb rigid planar qauv, loj π - conjugated system, zoo heev fluorescence kev ua tau zoo, thiab nplua nuj tshuaj reactivity, tau qhia zoo kawg li daim ntawv thov nqi nyob rau hauv ntau yam xws li dyeing kev lag luam, tshuaj, optoelectronic cov ntaub ntawv, tshuaj ntsuam xyuas, ib puag ncig tswj, thiab lwm yam.
1. Dyes thiab pigments kev lag luam - feem ntau classic theem ntawm akridin
Daim ntawv thov qub tshaj plaws thiab paub tab tshaj plaws hauv kev lag luam yog qhov tsis ntseeg ntawm kev tsim cov dyes thiab cov pigments siab heev. Akridin muaj cov tshuaj ruaj khov thiab tuaj yeem siv tau los ua cov xim (xws li Yin Dan Shilin) thiab cov xim zoo nkauj (xws li quinacridone). Tom qab cov hydrogen ntawm lub nplhaib benzene ntawm akridin hloov los ntawm ib pawg amino, nws dhau los ua ib qho tseem ceeb nruab nrab ntawm akridin dye. Nws cov derivatives tuaj yeem siv los tsim ntau yam xim ci ntsa iab thiab siab - cov khoom siv dyeing, uas tau siv dav hauv kev lag luam textile thiab dyeing.
Tsis tas li ntawd, kev ua thiab hloov khoom siv kuj muaj cov ntawv thov zoo. Piv txwv li, oxyfluorenyl-2,3-acid tuaj yeem siv rau kev tsim cov dyes; 3-aminoalkyloxyfluorene tuaj yeem siv rau hauv cov tshuaj; Fluorine oxychloride tuaj yeem siv los ua ib qho ntxiv rau cov khoom siv hluav taws xob rwb thaiv tsev; Sulfonated condensates tuaj yeem siv los ua textile auxiliaries thiab wetting agents. Cov khoom lag luam hauv qab no txuas ntxiv nthuav dav kev lag luam ntawm akridin.
Nyob rau hauv daim teb ntawm cov plaub hau dyeing, akridin tebchaw kuj nyob ib qho chaw. Vim nws cov xim muaj zog muaj peev xwm thiab cov xim zoo nrawm, akridin derivatives yog siv rau hauv cov plaub hau xim formulations, muab cov neeg siv khoom nrog ntau hom plaub hau xaiv.
2. Kev kho mob teb - lub zog tseem ceeb uas cawm neeg txoj sia
Daim ntawv thov hauv kev kho mob tuaj yeem suav tias yog nws qhov kev siv tseem ceeb tshaj plaws, suav nrog ntau cov lus qhia xws li tshuaj tiv thaiv - qog, tshuaj tua kab mob thiab tshuaj tiv thaiv - mob, kho kab mob paj hlwb, kab mob metabolic, thiab lwm yam.
2.1. Cov tshuaj tiv thaiv qog
Acridinecov tebchaw yog ib chav kawm tseem ceeb ntawm cov tebchaw uas muaj peev xwm tiv thaiv - qog nqaij hlav, thiab kev kawm txog lawv cov txheej txheem tau dhau los ua cov ntsiab lus kub thiab tsom mus rau kev tshawb fawb tshuaj chemistry.
(1) Cov tshuaj cytotoxic ncaj qha: Lawv muaj cov teebmeem cytotoxic ncaj qha thiab feem ntau ua rau ntawm S theem ntawm lub voj voog ntawm tes, inhibiting synthesis ntawm purines, RNA, thiab cov proteins, nrog rau kev cuam tshuam DNA synthesis . 30 feeb tom qab ib qho kev txhaj tshuaj intravenously, cov concentration hauv cov ntshav nce mus txog nws qhov siab tshaj plaws, thiab cov tshuaj metabolic yog 45%. tso tawm los ntawm cov zis hauv 0-6 teev, tab sis tsis tuaj yeem dhau los ntawm cov hlab ntsha hauv hlwb. Clinically, nws yog tsuas yog siv rau kev kho mob ntawm Hodgkin tus kab mob, melanoma, thiab cov nqaij mos sarcoma. Cov koob tshuaj txhaj yog 200-400mg / m ² ib hnub, siv tsis tu ncua rau 5-10 hnub, nrog rau lub sijhawm ntawm 4-8 lub lis piam ua ntej kev kho thib ob.
(2) Amsacrine, tseem hu ua aminophenylacridine, muaj cov txheej txheem ntawm kev ua haujlwm zoo ib yam li cov tshuaj anthracycline. Nws tuaj yeem cuam tshuam nrog adenine thymidine puag khub, tiv thaiv DNA los ntawm kev ua tus qauv rau kev rov ua dua thiab kev sib txuas, thiab cuam tshuam nrog cov qauv ntawm cov cell membrane proteins los tsim kev tiv thaiv- qog nqaij hlav. Feem ntau yog siv rau cov neeg laus mob uas tsis yog lymphocytic leukemia, cov koob txhaj tshuaj yog 90-120mg / m ², ib zaug txhua 3-4 lub lis piam, thiab ib chav kho mob yog 500-750mg / m ².
(3) Mitoxantrone: ib qho khoom qab zib tsis muaj anthracycline anticancer tshuaj nrog cov qauv zoo ib yam li doxorubicin. Nws muaj dav dav los tiv thaiv- qog spectrum thiab siv rau mob qog noj ntshav mis, mob leukemia, malignant lymphoma thiab mob qog noj ntshav.
(4) Tacrine, tseem hu ua 9-amino-1,2,3,4-tetrahydroacridine lossis Cognex, yog acetylcholine ester inhibitor pom zoo los ntawm US FDA hauv 1993 rau kev kho mob Alzheimer's. Nws ua lub luag haujlwm tseem ceeb hauv thaj chaw ntawm neurology.
(5) Kev sib koom ua ke los tiv thaiv- qog cov nyhuv ntawm akridin daj thiab leflunomide: Kev tshawb fawb tau pom tias kev sib xyaw ua ke ntawmacridinedaj thiab classical bifunctional alkylated melphalan tuaj yeem txhim kho DNA kev puas tsuaj tshwm sim los ntawm yav tas los, txhawb cov qog cell apoptosis, thiab yog li kev sib koom ua ke los tiv thaiv - qog cov teebmeem hauv vitro thiab hauv vivo, muab kev tshawb fawb hauv paus rau kev kho mob tshuaj.
(6) Kev tshawb fawb txog kev tiv thaiv - qog cov teebmeem ntawm cov tshiab akridin derivatives: Qu Xiaona li al.
kawm tib neeg leukemia hlwb thiab doxorubicin resistant leukemia hlwb thiab pom tias tshiab akridin derivatives muaj ib tug tseem ceeb inhibitory nyhuv ntawm kev loj hlob ntawm doxorubicin resistant leukemia hlwb. Lawv tuaj yeem ua rau apoptosis thiab autophagy los ntawm inhibiting kev ua haujlwm thiab kev qhia ntawm P-glycoprotein, thiab ua rau muaj kev cuam tshuam rov qab rau ntau yam tshuaj tiv thaiv. Lub akridin polyamine derivatives tsim thiab tsim los ntawm Li Xiaoliu li al. pom kev ua haujlwm siab tiv thaiv tib neeg cov kab mob leukemia, cov qog nqaij hlav cancer hauv lub ntsws, thiab cov kab mob qog noj ntshav hauv tsev menyuam. Cov akridin amide thiourea derivatives kawm los ntawm Li Junwei thiab lwm tus muaj kev tiv thaiv - qog ua haujlwm hauv vitro tiv thaiv kab mob qog noj ntshav, mob qog noj ntshav, mob qog noj ntshav, neuroblastoma, mob qog noj ntshav nasopharyngeal thiab mob ntsws cancer.
2.2. Anti-inflammatory, antibacterial, antimalarial, thiab anticancer zog
Akridin tebchaw muaj cov haujlwm tseem ceeb ntawm cov tshuaj lom neeg lom neeg thiab tshuaj tshuaj hauv kev tiv thaiv - mob, tshuaj tua kab mob, tshuaj tiv thaiv kab mob, thiab tshuaj tiv thaiv kab mob. Nws cov haujlwm yog los ntawm kev siv dav dav ntawm hydrogen bonding thiab π - π kev sib cuam tshuam hauv supramolecular tes hauj lwm. Akridin dilute daws tuaj yeem siv los ua cov tshuaj tua kab mob thiab ua lub luag haujlwm pabcuam hauv kev tswj xyuas kab mob. Cov kev tshawb fawb ntsig txog kuj qhia tau tias cov tshuaj akridin tuaj yeem ua lub luag haujlwm tseem ceeb hauv cov tsos mob tshwm sim thaum cev xeeb tub hauv cov poj niam.
Kev tshawb fawb los ntawm Gao Sujuan et al. pom tias uterine artery embolization ua ke nrog methotrexate thiab ethacridine lactate tuaj yeem txo cov ntshav ntau, ua kom luv nyob hauv tsev kho mob, thiab txo qis tus nqi ntawm kev phais thiab hysterectomy hauv cov poj niam uas raug rho menyuam tawm nrog cov placenta previa hauv nruab nrab cev xeeb tub.
3. Kev tiv thaiv hom 2 mob ntshav qab zib mellitus - qhov kev tawm tshiab tshiab
Cov txiaj ntsig tshawb fawb tshiab tshaj tawm hauv lub Tsib Hlis 2026 qhia tias pab pawg coj los ntawm Shen Xin los ntawm Air Force Medical University tau tshawb pom ib hom tshiab ntawm acridone ketone GPR40 agonist ADD-16.
EC ₅₀ tus nqi ntawm cov tshuaj no rau GPR40 yog 12.33 μ mol / L, uas muaj zog insulin secretion txhawb nqa thiab txo qis hauv vitro siab toxicity dua TAK875. ADD-16 tuaj yeem txo cov ntshav qabzib tom qab hauv T2DM cov qauv nas, txhim kho cov piam thaj thiab insulin tsis kam, txo cov piam thaj tsis muaj roj, txhim kho cov metabolism hauv lipid, thiab txo cov rog hauv siab. Nws cov khoom pharmacokinetic yog qhov zoo, nrog rau ib nrab-lub neej ntawm 30.2 teev, thiab nws muaj cov yam ntxwv ntawm pancreatic hom phiaj. LD ₅₀ tus nqi ntawm kev kuaj mob toxicity hauv vivo yog 1168mg / kg, thiab tsis muaj toxicity tseem ceeb ntawm kev kho mob concentration. Kev ntsuas kev nyab xeeb yog qhov zoo.
Txoj kev tshawb no tau tsim lub hauv paus rau kev txhim kho GPR40 agonist tshuaj thiab muab txoj hauv kev tshiab rau kev kho T2DM.
2. 4. Kev kho mob ntawm cov kab mob hauv lub cev xeeb tub
Acridinone acetic acid (nws sodium ntsev yog dej{0}}soluble) tau tso cai los ntawm SDFS hauv Russia thiab lwm lub tebchaws. Nws cov ntsev thiab cov lipids tuaj yeem cuam tshuam rau androgens hauv tib neeg lub cev los ntawm kev kho cov tshuaj hormones, thiab tuaj yeem siv los kho thiab tiv thaiv cov qog nqaij hlav ntawm poj niam cev xeeb tub, xws li mob cancer mis, uterinecancer, cancer ntawm zes qe menyuam, thiab tseem tuaj yeem siv los kho txiv neej plaub hau poob, prostate adenoma, prostate cancer, prostate cancer recurrence thiab lwm yam kab mob. Cov nyhuv kho mob yog qhov zoo.
3. Chemiluminescence immunoassay - lub hnub qub reagent hauv kev kuaj mob
Acridinium ester yog chemiluminescent marker nrog ib qhoacridinenplhaib raws li nws cov qauv tseem ceeb. Nws yog ib qho zoo tshaj plaws luminescent reagents nyob rau hauv niaj hnub chemiluminescent immunoassay (CLIA), thiab nws daim ntawv thov tau nkag mus rau txhua yam ntawm kev kuaj mob.
3.1. Luminescence mechanism
Akridin ester dhau chemiluminescence cov tshuaj tiv thaiv hauv alkaline hydrogen peroxide tov: Thaum akridin ester raug hydrogen peroxide.
Cov pab pawg nquag hauv cov molecule yog oxidized, thiab C-9 hloov pauv nrog H ₂ O ₂ los ua kom muaj qhov tsis ruaj khov ethylene oxide nruab nrab. Qhov no intermediate sai decomposes rau hauv CO ₂ thiab lub electron zoo siab lub xeev ntawm N-methylacridone. Thaum nws rov qab los rau hauv av, nws tso tawm photons nrog lub siab tshaj plaws emission wavelength ntawm 430nm. Nws cov luminescence yog ntawm "flash type", ncav cuag nws qhov siab tshaj plaws hauv 0.4 vib nas this tom qab ntxiv cov oob khab reagent, nrog ib nrab-lub neej ntawm 0.9 vib nas this.
3.2. Core zoo
Akridin ester, raws li daim ntawv lo, muaj cov txiaj ntsig zoo xws li qis tom qab luminescence, siab teeb liab - rau- suab nrov piv, cuam tshuam tsawg kawg hauv cov tshuaj tiv thaiv luminescence, ceev thiab concentrated lub teeb tso tawm, siab luminescence efficiency, yooj yim khi nrog cov proteins tsis txo cov photon yield, thiab ruaj khov daim ntawv lo (tuaj yeem khaws cia rau ob peb lub hlis). Piv nrog rau cov cim cim, akridin ester luminescence immunoassay tshuab muaj qhov tseeb dua thiab ua haujlwm sai thiab yooj yim dua.
3.3. Daim ntawv thov kho mob
Los ntawm kev siv akridin ester chemiluminescence immunoassay technology ua ke nrog biotin avidin sib nqus particle sib cais tshuab, ib txoj kev tshawb nrhiav kom muaj nuj nqis rau carcinoembryonic antigen (CEA) cov ntsiab lus hauv cov ntshav tuaj yeem tsim, ua rau kev kho mob txiav txim siab ntawm cov ntshav CEA cov ntsiab lus sai thiab yooj yim dua. Cov thev naus laus zis no tseem tuaj yeem siv los txheeb xyuas cytokines xws li tib neeg interleukin-1 alpha, interleukin-1 beta, thiab interferon gamma, nrog rau cov pa phem xws li bisphenol A.
Tam sim no, akridin esters tau tsim ntau yam khoom, suav nrog AE-NHS, DMAE-NHS, Me-DMAE-NHS, NSP-DMAE-NHS, NSP-SA, NSP-SA{{8}{9}NHS, Ntawm lawv, akridin sulfonamides (xws li NSP-SA-NHS) muaj zog tiv thaiv hydrolysis vim C-N daim ntawv cog lus tau siab dua C-O daim ntawv cog lus, thiab kev qhia txog propane sulfonate sab hauv cov ntsev pawg ua kom dej solubility. Lub quantum tooj lwj ntawm chemiluminescence ntawm 37℃rau 4 lub lis piam yog tsawg dua 10%, qhia tau hais tias superior kev kawm. Pab pawg Kang Chuanqing ntawm Changchun Yinghua lub koom haum tau ua tiav kev tsim khoom loj ntawm cov khoom siv tshuaj tiv thaiv kab mob chemiluminescence immunoassay raws li hom tshiab ntawm akridin sulfonamide.
Acridinefeem ntau yog synthesized nyob rau hauv ntau txoj kev.
Txoj Kev 1: Los ntawm Acridone
Acridone yog tau los ntawm diphenylamine-2-carboxylic acid los ntawm cycling nrog sulfuric acid, thiab ces oxidising akridin los ntawm kev txo mus rau 9,10-dioxoacridine nrog pentanol thiab sodium.
Kev npaj hauv chav kuaj kuj tseem tuaj yeem ua los ntawm kev sib xyaw acridone Chemicalbook nrog zinc hmoov thiab cua sov.
Akridin sublimation generated los ntawm cov tshuaj tiv thaiv yog yaj nyob rau hauv hydrochloric acid, thiab ces alkalised nrog sodium hydroxide tov, precipitate, lim kom tau cov khoom crude.
Recrystallisation nrog methanol muab cov khoom zoo nrog lub melting point ntawm 110 degree.
Txoj Kev 2: Raws li cov tshuaj tiv thaiv condensation ntawm aniline thiab aldehyde lossis ketone
ua ntej, aniline yog condensed nrog formaldehyde nyob rau hauv acidic tej yam kev mob los tsim N-methylaniline.
C6H5NH2 + CH2O → C6H5NHCH3 (N-methylaniline)
Tom ntej no, N-methylaniline reacts nrog bromine nyob rau hauv cov kev mob tsim nyog muab N-methyl-N-bromoaniline.
C6H5NHCH3 + Br2 → C6H5N(CH3)Br (N-}methyl-N-bromoaniline)
Thaum kawg, ob lub N-methyl-N-bromoaniline molecules teb los ntawm kev sib txuas los ua akridin.
2C6H5N(CH3)Br → C13H9N + 2 HBr + 2 CH3Br
Cov lus nug nquag
Acridine ua dab tsi?
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Acridine yog polycyclic aromatic dye nrogantineoplastic, antimicrobial thiab imaging kev ua ub no. Acridine thiab nws cov derivatives intercalate nyob rau hauv DNA thiab RNA los ntawm kev tsim hydrogen- bonds thiab stacking ntawm lub hauv paus khub uas ua rau DNA crosslinks thiab strand so.
Dab tsi yog qhov kev hloov pauv los ntawm acridine dyes?
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Qhov no hu ua aframeshift kev hloov. Proflavin yog ib qho acridine dye uas intercalates nws tus kheej ntawm lub hauv paus khub ntawm DNA saw thiaj li ua rau poob los yog nce ntawm ib tug nucleotide. Cov noob hloov pauv hloov lub hauv paus ua ntu zus ntawm tag nrho cov kab mob caj ces los ntawm qhov kev hloov pauv hu ua frameshift mutation.
Puas yog acridine txiv kab ntxwv carcinogenic?
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Toxicity thiab carcinogenicity ntawm AO. Txij li AO yog mutagenic hauv cov kab mob (24, 25),Nws kuj tseem yuav ua tau carcinogenic hauv tib neeg.
Cim npe nrov: Acridine CAS 260-94-6, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom