Baricitinib yog dab tsi?
Baricitinib hmoovyog dawb-zoo li los yog dawb crystalline hmoov, tsw thiab saj, me ntsis soluble nyob rau hauv dej, soluble nyob rau hauv dej kub, kuj ruaj khov nyob rau hauv ib txwm kub, insoluble nyob rau hauv ethanol los yog acetone, thiab soluble nyob rau hauv sodium hydroxide xeem tshuaj.
Baricitinib yog Janus kinase (JAK) inhibitor. JAKs yog ib qho enzyme intracellular, uas tuaj yeem xa cov teeb liab tsim los ntawm kev sib cuam tshuam ntawm cytokines lossis kev loj hlob zoo receptors ntawm cov cell membrane, uas tuaj yeem cuam tshuam cov txheej txheem cellular ntawm hematopoietic muaj nuj nqi thiab lub cev tiv thaiv kab mob.
| Khoom npe | Baricitinib |
| CAS | 1187594-09-7 |
| Cov mis mos molecular | C16H17N7O2S |
| Molecular hnyav | 371.42 |
| EINECS Number | 691-421-4 |
| Kev cia khoom | -20 degree |
| Melting point | 212-215 degree |
| Solubility | Soluble hauv DMSO (txog 30mg / ml) lossis DMF (txog 50mg / ml). |
| Qhov tshwm sim | Dawb hmoov |
| Boiling point | 7 07.2 ± 70.0 degree ntawm 760 mmHg |
| Qhov ntom | 1.56 |
Lub mechanism ntawm Baricitinib yog dab tsi?
Baricitinib yog ib qho kev xaiv inhibitor ntawm JAK2 thiab JAK1, thiab muaj kev cuam tshuam me ntsis ntawm JanusKinase thiab jak3orTYK2. Qhov kinase no thiab nws cov teeb liab cuam tshuam txog kev hloov pauv thiab kev hloov pauv hloov pauv (JAK-STAT) yog txoj hauv kev tseem ceeb hauv lub cev los tswj lub amplitude thiab lub sijhawm ntawm cov teeb liab hloov ntawm cytokines thiab hom I thiab hom II cytokine receptors. Cov receptors no tsis muaj qhov ua haujlwm ntawm lub cev enzyme teeb liab hloov pauv uas tuaj yeem kho tau; Janus Kinase \ Cov teeb liab thiab kev hloov pauv cov activators yog phosphorylated los ntawm JAK enzyme, uas ua rau kev ua kom STAT. Ntau yam inflammatory yam cuam tshuam rau hauv lub pathogenesis ntawm RA, suav nrog IL-6, granulocyte-macrophage colony stimulating factor thiab (GM-CSF) factor. Interferon teeb liab hla dhau JAK-STAT teeb liab txoj hauv kev. Yog li, JAK1 thiab JAK2 inhibitors tuaj yeem tsom ntau yam RA-txog cytokine txoj hauv kev, yog li txo qis kev ua kom muaj zog thiab loj hlob ntawm lub cev tiv thaiv kab mob tseem ceeb ntawm cov kab mob inflammatory.Baricitinib hmoovtsis muaj kev cuam tshuam rau JAK3. JAK3 tej zaum yuav muaj feem xyuam nrog cov saw hlau receptor. Feem ntau cov cytokines ntawm cov saw muaj xws li IL-15 thiab IL-21, uas feem ntau tswj cov lymphocyte activation, muaj nuj nqi thiab kev loj hlob.
Khoom Specification
| Yam khoom | Specification | Cov txiaj ntsig |
| Qhov tshwm sim | Dawb los yog dawb dawb hmoov hmoov | Ua raws |
| Kev txheeb xyuas | Los ntawm IR | Ua raws |
| Los ntawm HPLC | Ua raws | |
| Solubility | Soluble nyob rau hauv DMF, sparingly soluble nyob rau hauv THF, me ntsis soluble nyob rau hauv methanol thiab acetonitrile, heev sightly soluble nyob rau hauv ethanol thiab dichloromethane, insoluble nyob rau hauv dej | Ua raws |
| Polymorphic Form | Polymorphic daim ntawv 1 | Ua raws |
| Melting Point | 211ºC~216ºC | 212.8ºC~214.9ºC |
| Cov ntsiab lus dej | Tsawg dua los yog sib npaug rau 0.50% | 0.10% |
| Hnyav Hlau | Tsawg dua lossis sib npaug li 20ppm | Ua raws |
| Residue ntawm Ignition | Tsawg dua lossis sib npaug rau 0.20% | 0.09% |
| Yam khoom | Ib qho impurity: Tsawg dua lossis sib npaug rau 0.10% | 0.06% |
| Tag nrho cov impurities: Tsawg dua lossis sib npaug rau 1.00% | 0.16% | |
| Assay (ntawm lub hauv paus anhydrous) | 98.0%~102.0% | 99.94% |
| Particle Loj | D90: Tsawg dua lossis sib npaug rau 100µm | Ua raws |
| Xaus: | Ua raws li kev lag luam specification. | |
Baricitinib siv rau qhov twg?
1.Baricitinib hmoovyog siv los kho mob nruab nrab mus rau hnyav rheumatoid mob caj dab (RA) rau cov neeg laus. Cov neeg mob uas tsis haum rau ib lossis ntau dua cov tshuaj tiv thaiv kab mob tuaj yeem kho nrog cov khoom no, uas tuaj yeem kho nrog ib qho tshuaj lossis ua ke nrog methotrexate.
2. Siv rau hauv kev tshawb fawb tshawb fawb thiab tshuaj reagents.
HTML5 atlas of Baricitinib
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Kev ua haujlwm lom ntawm Baricitinib:
| Piav | Baricitinib yog ib qho kev xaiv thiab qhov ncauj inhibitor ntawm JAK1 thiab JAK2 nrog IC50 ntawm 5.9 nM thiab 5.7 nM, feem. |
| Lub hom phiaj |
JAK 2:5.7 nM (IC50) JAK 1:5.9 nM (IC50) Tyk 2:53 nM (IC50) JAK3:560 nM (IC50) |
| Kev tshawb fawb hauv vitro | Baricitinib (INCB028050) tau raug pov thawj tias yog ib qho zoo inhibitor ntawm JAK teeb liab transduction thiab muaj nuj nqi hauv kev soj ntsuam ntawm tes. Hauv PBMC, Baricitinib inhibited phosphorylation ntawm STAT3 (pSTAT3) txhawb nqa los ntawm IL-6 thiab tom qab tsim tawm ntawm MCP-1, nrog IC50 qhov tseem ceeb ntawm 44nM thiab 40nM, feem. Hauv cov kab mob uas tsis muaj kev sib cais, INCB028050 kuj inhibit PSTAT 3 txhawb nqa los ntawm IL{11}} (IC50=20} nm). Qhov tseem ceeb, qhov inhibition no tiv thaiv Th17 hlwb los ntawm kev tsim ob kab mob cytokines (IL-17 thiab IL{15}})- tus pab T cell subtype nrog pom tseeb inflammatory thiab pathogenic yam ntxwv-nrog IC50 tus nqi ntawm 50nM. Hauv qhov sib txawv ntse, JAK1/2 inhibitors INCB027753 thiab INCB029843, uas zoo sib xws hauv cov qauv tab sis tsis muaj txiaj ntsig, tsis muaj kev cuam tshuam loj hauv ib qho ntawm cov kev txiav txim siab no thaum kuaj ntawm qhov siab li 10 μ m. |
| Hauv vivo kawm | Piv nrog rau tus neeg nqa khoom, lub paw ntim tau nce 50% tom qab kho nrog INCB028050 rau 2 lub lis piam. Cov koob tshuaj yog 1 mg / kg,> 95%, thiab cov koob tshuaj yog 3 lossis 10 mg / kg. Vim hais tias lub hauv paus paw ntim tau ntsuas nyob rau 0 hnub ntawm kev kho tsiaj ntawm cov tsiaj uas muaj cov cim tseem ceeb ntawm cov kab mob, nws yuav muaj > 100% inhibitory nyhuv ntawm o, qhia tau hais tias ib tug tseem ceeb kev txhim kho ntawm o. Baricitinib (0.7mg / hnub) kho cov nas, raws li kev soj ntsuam los ntawm H&E staining, pom tau tias txo qhov mob, txo CD8 infiltration thiab txo MHC chav kawm I thiab II qhia. Piv nrog rau cov nas uas tau kho nrog vector tswj, CD8+NKG2D + cov cell hauv nas kho nrog Baricitinib yog cov txiaj ntsig tseem ceeb ntawm cov kab mob hauv nas thiab tib neeg alopecia (AA), uas txo qis heev. |
| Kinase kev sim | Homogeneous lub sij hawm daws teeb meem fluorometry (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) los yog tag nrho-ntev enzyme (cMET). Thiab Chk2) thiab peptide substrate. Txhua qhov tshuaj tiv thaiv enzyme tau ua nrog lossis tsis muaj qhov sib xyaw ua ke (11- taw tes dilution), JAK, cMET lossis Chk2 enzyme, 500 nm (100nM rau CHK2) peptide, ATP (Km lossis 1mM tshwj xeeb rau txhua kinase), thiab 2.0％DMSO tau ntxiv rau qhov kev xeem tsis. Qhov ntsuas IC 50 tus nqi yog qhov sib xyaw ua ke uas yuav tsum tau ua kom txo qis 50% fluorescence teeb liab. Kev soj ntsuam kinase ntxiv tau ua nyob rau ntawm Cerep siv cov txheej txheem ntawm 200nM. Enzymes kuaj muaj xws li: Abl, Akt1, AurA, AUB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKK, IKK, JNK1, Lck , MEK1. |
| Kev sim ntawm tes | Tib neeg PBMC raug cais los ntawm leukocyte sib cais, thiab tom qab ntawd Ficoll-Hypaque centrifugation tau ua. Txhawm rau txiav txim siab MCP-1 ntau lawm induced los ntawm IL-6, PBMC tau inoculated rau hauv RPMI 1640+10% FCS nrog 3.3 ×10 5 cell per well nyob rau hauv lub xub ntiag los yog tsis muaj. INCB028050 (1 nM, 10 nM, 100 nM). 1μM thiab 10μM). Tom qab ua ntej incubation nrog cov compound nyob rau hauv chav tsev kub rau 10 feeb, hlwb tau stimulated los ntawm kev ntxiv 10ng / mL ntawm tib neeg recombinant IL -6 rau txhua qhov dej. Cov hlwb raug incubated ntawm 37 degree thiab 5% CO 2 rau 48 teev. Tus supernatant tau sau thiab qib ntawm tib neeg MCP-1 tau txheeb xyuas los ntawm ELISA. Lub peev xwm ntawm INCB028050 los inhibit IL-6-induced MCP-1 secretion tau tshaj tawm raws li qhov xav tau concentration (IC50) rau 50% inhibition. Cell-Titer Glo [1] tau siv los proliferate Ba/F3-TEL-JAK3 hlwb hauv 3 hnub. |
| Tsiaj sim | nas: Poj niam nas (n {{0}}} nyob rau hauv txhua pab pawg) tau muab ib koob ntawm 10mg/kg Baricitinib, thiab tau muab 10mL/kg los ntawm qhov ncauj yuam pub. Thawj peb nas tau los ntshav ntawm 0 (ua ntej kev tswj hwm), 2 teev, 8 teev thiab 24 teev, thiab peb nas thib ob tau los ntshav ntawm 1,4 thiab 12 teev tom qab tswj hwm. EDTA yog siv los ua anticoagulant, thiab cov qauv yog centrifuged kom tau plasma. Cov txheej txheem analytical rau quantifying INCB028050 tau tsim thiab siv los soj ntsuam cov qauv los ntawm kev tshawb fawb toxicological. Cov txheej txheem sib xyaw ua ke cov kua dej nag los nrog 10% methanol hauv acetonitrile thiab nqa tawm LC / MS / MS tsom xam. Txoj kev no siv 0.1mL cov qauv tshawb fawb los ua pov thawj tias qhov kev txiav txim siab linear yog 1-5000nM. Siv Analyst 1.3.1 los ua cov ntaub ntawv. Siv qhov hnyav linear regression (1/x2) los txiav txim tus qauv nkhaus ntawm qhov chaw siab tshaj qhov sib piv concentration. C3H/HeJ hloov pauv tus neeg txais tus nas qauv ntawm nas AA tau siv rau hauv cov kev sim no. Hauv luv luv, daim tawv nqaij alopecia los ntawm C3H/HeJ nas nrog spontaneous alopecia tau hloov mus rau C3H/HeJ nas hnub nyoog 8-10 lub lis piam tsis muaj kab mob. Thaum lub sijhawm hloov pauv, lub twj tso kua mis osmotic tau cog, uas tau tswj hwm txog 0.7mg / hnub ntawm Baricitinib lossis placebo. Lub twj tso kua mis osmotic yuav tsum tau hloov ib hlis ib zaug. Lub sij hawm-qhov xwm txheej muaj sia nyob tsom xam ntawm lub sijhawm censored cov ntaub ntawv yog nqa tawm. Cov pob ntawv ciaj sia taus thiab ncua sij hawm nyob rau hauv r yog siv los ua qhov ntsuas ntsuas ntsuas. Qhov kev xav tias kev muaj sia nyob sib npaug sib npaug hauv (n=10) Baricitinib-kho nas thiab (n=10) cov nas uas siv cov placebo raug tsis lees paub ntawm qib 5%, thiab tus nqi P yog 0.0035 los ntawm kev siv Sun tus qhab nia rau qhov tseeb log-qib ob-tus qauv xeem. |
| Cov ntaub ntawv |
[1]. Fridman JS, et al. Kev xaiv inhibition ntawm JAK1 thiab JAK2 yog qhov ua tau zoo hauv cov qauv nas ntawm kev mob caj dab: preclinical characterization ntawm INCB028050. J Immunol. 2010 May 1; 184(9):5298-307. [2]. Jabbari A, et al. Kev thim rov qab ntawm Alopecia Areata tom qab kho nrog JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5. [3]. Khan IM, et al. Intermuscular thiab perimuscular rog nthuav dav hauv kev rog rog cuam tshuam nrog cov leeg pob txha T cell thiab macrophage infiltration thiab insulin tsis kam. Int J Obes (Lond). 2015 Nov; 39(11):1607-18. |
Qhov txawv ntawm Baricitinib thiab Tofacitinib yog dab tsi?
Ua ntej, ob qho tib siBaricitinib hmoovthiab Tofacitinib hmoov yog xaiv JAK inhibitors. JAK (Janus kinase) yog ib qho ntawm cov enzymes tseem ceeb uas tswj ntau yam cytokine signaling txoj hauv kev thiab raug suav tias ua lub luag haujlwm tseem ceeb hauv kev tsim cov kab mob autoimmune. Ob yam khoom no tuaj yeem thaiv cov teeb liab hloov pauv ntawm cytokines los ntawm inhibiting cov haujlwm ntawm JAK kinase, yog li txo qis kev ua haujlwm ntawm cov hlwb ntsig txog mob thiab tshwm sim ntawm cov tshuaj tiv thaiv inflammatory.
Txawm li cas los xij, muaj qee qhov sib txawv hauv kev xaiv thiab qhov tshwj xeeb ntawm Baricitinib thiab Tofacitinib. Baricitinib nyiam inhibit JAK1 thiab JAK2, thaum Tofacitinib muaj kev xaiv siab rau plaub JAK kinases (JAK1, JAK2, JAK3 thiab TYK2). Qhov sib txawv no ua rau Baricitinib muaj qee qhov tshwj xeeb zoo hauv kev kho mob tshwj xeeb.
Hais txog cov kev mob tshwm sim, cov kev mob tshwm sim ntawm Baricitinib thiab Tofacitinib yog qhov zoo sib xws, tab sis muaj qee qhov sib txawv me me. Nws yog ib qho tseem ceeb heev uas yuav tsum nco ntsoov tias vim tias ob qho tib si cov khoom lag luam inhibit qhov kev ua haujlwm ntawm lub cev tiv thaiv kab mob, lawv tuaj yeem ua rau muaj kev pheej hmoo kis mob thaum siv.
Kev ceev faj ntawm Baricitinib hmoov yog dab tsi?
1. Xyuas kom tus neeg mob tsis raug mob los ntawm tuberculosis lossis lwm yam kab mob ua ntej siv.
2. Koj yuav tsum tsis txhob siv cov khoom no yog tias koj ua xuaBaricitinib hmoovlos yog muaj tej yam kab mob.
3. "Cov tshuaj tiv thaiv nyob" tsis tuaj yeem txhaj tshuaj thaum siv; Cov tshuaj tiv thaiv inoculated nyob rau lub sijhawm no yuav tsis muaj qhov xav tau, thiab tsis tuaj yeem tiv thaiv cov neeg mob los ntawm kev puas tsuaj ntawm tus kab mob.
4. Baricitinib yuav cuam tshuam rau lub cev tiv thaiv kab mob thiab tej zaum yuav kis tau tus kab mob ntau dua, txawm tias mob hnyav lossis tuag taus.
Yuav ua li cas thiab qhov twg yuav Baricitinib hmoov lag luam wholesale?
Koj tuaj yeem tso siab rau peb qhov kev txiav txim vim tias peb muaj cov ntaub ntawv zoo ntawm kev muag tshuaj qhia kev cai lij choj.
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
|
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, |
|
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: baricitinib hmoov cas 1187594-09-7, Suav teb, 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