Ingemuva

I-Tofacitinib citrate, eyaziwa nangokuthi i-CP-690550 citrate, iyi-inhibitor enamandla ye-janus kinase 3 (JAK3), i-tyrosine kinase ekhawulelwe ngamaseli e-hematopoetic ehilelekile ekudlulisweni kwesignali elawula ukusinda kwe-lymphocyte, ukwanda, ukuhlukaniswa, kanye ne-apoptosis. Ukuvinjelwa kuqondile nge-JAK3 ngokukhetha okuphindwe ka-1000 ngaphezu kwamanye ama-kinase omndeni angewona ama-JAK. Ngaphandle kokuvimbela i-JAKS (IC50 = 1 nM), i-tofacitinib citrate iphinde ivimbele i-janus kinase 2 (JAK2) kanye ne-janus kinase 1 (JAK1) enamandla angu-20- kanye ne-100 ngokuphindaphindiwe ngokulandelana. Nokho, ocwaningweni lwakamuva, izibopho ezibophezelayo (Ki) ze-tofacitinib citrate eziya ku-JAK1, JAK2, ne-JAK3 kubikwe ukuthi ziyi-1.6 nM, 21.7 nM, kanye ne-6.5 nM ngokulandelanayo.

Ireferensi

Lalitha Vijayakrishnan, R. Venkataramanan kanye noPalak Gulati. Ukwelapha ukuvuvukala nge-janus kinase inhibitor CP-690,550. Amathrendi ku-Pharmacological Science 2011: 32 (1); 25-34

Ukucaphuna Komkhiqizo

• 1. Panagi I, Jennings E, et al. "I-Salmonella Effector SteE Iguqula i-Mammalian Serine/Threonine Kinase GSK3 ibe i-Tyrosine Kinase ukuze Iqondise I-Macrophage Polarization." I-Cell Host Microbe. 2020;27(1):41–53.e6. PMID:31862381
• 2. McInnes IB, Byers NL, et al. "Ukuqhathaniswa kwe-baricitinib, upadacitinib, kanye ne-tofacitinib mediated regulation of cytokine signing in human leukocyte subpopulations." I-Arthritis Res Ther. 2019 Aug 2;21(1):183. PMID:31375130
• 3. U-Liu S, u-Verma M, nabanye. "Ukumelana ne-Steroid yohlobo 2 lwamaseli e-lymphoid angaphakathi avela ezigulini ezine-asthma enzima: Indima ye-thymic stromal lymphopoietin." J Allergy Clin Immunol. 2018 Jan;141(1):257-268.e6. PMID:28433687
• 4. UZheng, uLufeng, nabanye. "I-3′ UTR ye-pseudogene CYP4Z2P ikhuthaza i-tumor angiogenesis kumdlavuza webele ngokusebenza njenge-ceRNA ye-CYP4Z1." Ucwaningo nokwelashwa komdlavuza webele (2015): 1-14. PMID:25701119

Incazelo

I-Tofacitinib citrate iyi-JAK1/2/3 inhibitor etholakala ngomlomo ene-IC50s engu-1, 20, kanye no-112 nM, ngokulandelanayo. I-Tofacitinib citrate ine-antibacterial, antifungal kanye nemisebenzi ye-antiviral.

Isitoreji

4°C, vikela ekukhanyeni

*Ku-solvent : -80°C, izinyanga ezingu-6; -20°C, inyanga engu-1 (vikela ekukhanyeni)

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