Tofacitnib Citrate

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Tofacitinib citrate, eo hape e tsejoang e le CP-690550 citrate, ke inhibitor e matla ea janus kinase 3 (JAK3), tyrosine kinase e thibelang lisele tsa hematopoetic e kenyang phetisetso ea matšoao e laolang bophelo ba lymphocyte, ho ata, ho arohana, le apoptosis.Thibelo ke JAK3 e khethehileng e nang le selectivity 1000-fold ho feta tse ling tse seng tsa JAK family kinases.Ntle le ho thibela JAKS (IC50 = 1 nM), tofacitinib citrate e boetse e thibela janus kinase 2 (JAK2) le janus kinase 1 (JAK1) e nang le 20- le 100-fold ka potency ka ho latellana.Leha ho le joalo, phuputsong ea morao tjena, li-affinities tse tlamang (Ki) tsa tofacitinib citrate ho JAK1, JAK2, le JAK3 li tlalehiloe e le 1.6 nM, 21.7 nM, le 6.5 nM ka ho latellana.

Tshupiso

Lalitha Vijayakrishnan, R. Venkataramanan le Palak Gulati.Ho phekola ho ruruha ka janus kinase inhibitor CP-690,550.Mekhoa ea Lisaense tsa Pharmacological 2011: 32 (1);25-34

Tlhahiso ea Sehlahisoa

  • 1. Panagi I, Jennings E, et al."Salmonella Effector SteE E Fetola Mammalian Serine/Threonine Kinase GSK3 ho ba Tyrosine Kinase ho Direct Macrophage Polarization."Microbe Host Host.2020;27(1):41–53.e6.PMID:31862381
  • 2. McInnes IB, Byers NL, le ba bang."Papiso ea baricitinib, upadacitinib, le tofacitinib mediated regulation of cytokine signing in human leukocyte subpopulations."Ramatiki e Res Ther.2019 Aug 2;21(1):183.PMID:31375130
  • 3. Liu S, Verma M, le ba bang."Steroid resistance of airway type 2 innate lymphoid cells from bakuli ba nang le asma e matla: Karolo ea thymic stromal lymphopoietin." J Allergy Clin Immunol.2018 Jan; 141 (1): 257-268.e6.PMID: 28433687
  • 4. Zheng, Lufeng, le ba bang."3' UTR ea CYP4Z2P ea pseudogene e khothalletsa tumor angiogenesis ka kankere ea matsoele ka ho sebetsa e le ceRNA bakeng sa CYP4Z1."Patlisiso le kalafo ea mofetše oa matsoele (2015): 1-14.PMID:25701119

Tlhaloso

Tofacitinib citrate ke JAK1/2/3 inhibitor e fumanehang ka molomo e nang le IC50s ea 1, 20, le 112 nM, ka ho latellana.Tofacitinib citrate e na le mesebetsi ea antibacterial, antifungal le antiviral.

Polokelo

4°C, sireletsa kganya

*Ka solvent : -80°C, likhoeli tse 6;-20°C, khoeli e le 1 (sireletsa leseli)

 

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