Latar mburi

Tofacitinib citrate, uga dikenal minangka CP-690550 citrate, minangka inhibitor kuat saka janus kinase 3 (JAK3), sawijining kinase tyrosine sing diwatesi sel hematopoetik sing melu transduksi sinyal sing ngatur kaslametan, proliferasi, diferensiasi, lan apoptosis limfosit.Inhibisi kasebut spesifik JAK3 kanthi selektivitas 1000 kali luwih akeh tinimbang kinase kulawarga non-JAK liyane.Kejabi nyandhet JAKS (IC50 = 1 nM), tofacitinib sitrat uga nyandhet janus kinase 2 (JAK2) lan janus kinase 1 (JAK1) kanthi potensi 20- lan 100 kali luwih sithik.Nanging, ing panaliten anyar, afinitas ikatan (Ki) saka tofacitinib sitrat menyang JAK1, JAK2, lan JAK3 dilaporake masing-masing 1.6 nM, 21.7 nM, lan 6.5 nM.

Referensi

Lalitha Vijayakrishnan, R. Venkataramanan lan Palak Gulati.Nambani inflamasi kanthi inhibitor janus kinase CP-690,550.Tren ing Ilmu Farmakologi 2011: 32 (1);25-34

Kutipan produk

• 1. Panagi I, Jennings E, et al.Salmonella Effector SteE Ngonversi Mamalia Serine/Threonine Kinase GSK3 dadi Tyrosine Kinase kanggo Langsung Polarisasi Makrofag.Mikroba Inang Sel.2020;27(1):41–53.e6.PMID: 31862381
• 2. McInnes IB, Byers NL, et al."Perbandingan baricitinib, upadacitinib, lan tofacitinib mediated regulasi sinyal sitokin ing subpopulasi leukosit manungsa."Artritis Res Ther.2 Agustus 2019; 21 (1): 183.PMID: 31375130
• 3. Liu S, Verma M, et al."Resistensi steroid saka saluran napas jinis 2 sel limfoid bawaan saka pasien kanthi asma abot: Peran limfopoietin stromal timus." J Alergi Clin Immunol.2018 Jan;141(1):257-268.e6.PMID: 28433687
• 4. Zheng, Lufeng, et al."3' UTR saka pseudogene CYP4Z2P ningkatake angiogenesis tumor ing kanker payudara kanthi tumindak minangka ceRNA kanggo CYP4Z1."Riset lan perawatan kanker payudara (2015): 1-14.PMID: 25701119

Katrangan

Tofacitinib citrate minangka inhibitor JAK1/2/3 sing kasedhiya kanthi lisan kanthi IC50s masing-masing 1, 20, lan 112 nM.Tofacitinib citrate nduweni aktivitas antibakteri, antijamur lan antivirus.

Lumbung

4 ° C, nglindhungi saka cahya

* Ing solvent: -80 ° C, 6 sasi;-20°C, 1 sasi (lindhungi saka cahya)

Struktur kimia

Data Biologi sing Gegandhengan

Data Biologi sing Gegandhengan

Data Biologi sing Gegandhengan

Data Biologi sing Gegandhengan

Data Biologi sing Gegandhengan