Background

Tofacitinib citrate, inozivikanwawo seCP-690550 citrate, inhibitor ine simba yejanus kinase 3 (JAK3), hematopoetic cell-inodzorwa tyrosine kinase inobatanidzwa mukufambiswa kwechiratidzo inodzora kupona kwelymphocyte, kupararira, kusiyanisa, uye apoptosis.Iyo inhibition ndeye JAK3 chaiyo ine selectivity 1000-yakapetwa kupfuura mamwe asiri eJAK mhuri kinases.Kunze kwekudzivisa JAKS (IC50 = 1 nM), tofacitinib citrate inodzivisawo janus kinase 2 (JAK2) uye janus kinase 1 (JAK1) ine 20- uye 100-fold zvishoma mu potency maererano.Nekudaro, muongororo ichangoburwa, iyo inosunga affinities (Ki) ye tofacitinib citrate yakanangana neJAK1, JAK2, uye JAK3 yakanzi 1.6 nM, 21.7 nM, uye 6.5 nM zvakateerana.

Reference

Lalitha Vijayakrishnan, R. Venkataramanan and Palak Gulati.Kurapa kuzvimba nejanus kinase inhibitor CP-690,550.Maitiro muPharmacological Sayenzi 2011: 32 (1);25-34

Product Citation

• 1. Panagi I, Jennings E, et al."Salmonella Effector SteE Inoshandura iyo Mammalian Serine/Threonine Kinase GSK3 kuita Tyrosine Kinase kuDirect Macrophage Polarization."Cell Host Microbe.2020;27(1):41–53.e6.PMID:31862381
• 2. McInnes IB, Byers NL, nevamwe."Kuenzanisa kwe baricitinib, upadacitinib, uye tofacitinib yakapindirana mutemo we cytokine kuisa chiratidzo muvanhu leukocyte subpopulations."Arthritis Res Ther.2019 Aug 2;21(1):183.PMID:31375130
• 3. Liu S, Verma M, nevamwe."Steroid resistance ye airway type 2 innate lymphoid masero kubva kuvarwere vane asthma yakaoma: Basa re thymic stromal lymphopoietin." J Allergy Clin Immunol.2018 Jan;141(1):257-268.e6.PMID:28433687
• 4. Zheng, Lufeng, nevamwe."Iyo 3' UTR yepseudogene CYP4Z2P inokurudzira tumor angiogenesis mukenza yemazamu nekuita se ceRNA yeCYP4Z1."Tsvakurudzo yekenza yemazamu uye kurapwa (2015): 1-14.PMID:25701119

Tsanangudzo

Tofacitinib citrate inowanika nemuromo JAK1/2/3 inhibitor ine IC50s ye1, 20, uye 112 nM, zvichiteerana.Tofacitinib citrate ine antibacterial, antifungal uye antiviral mabasa.

Storage

4°C, chengetedza kubva kuchiedza

*In solvent : -80°C, 6 mwedzi;-20°C, 1 mwedzi (dzivirira kubva kuchiedza)

Chimiro chemakemikari

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