abẹlẹ

Tofacitinib citrate, ti a tun mọ ni CP-690550 citrate, jẹ oludena ti o lagbara ti janus kinase 3 (JAK3), tyrosine kinase ti o ni ihamọ ti ẹjẹ-ẹjẹ ti o ni ipa ninu iyipada ifihan agbara ti n ṣatunṣe iwalaaye lymphocyte, afikun, iyatọ, ati apoptosis.Idinamọ jẹ JAK3 pato pẹlu yiyan 1000-agbo diẹ sii ju awọn kinases idile ti kii ṣe JAK miiran.Yato si idinamọ JAKS (IC50 = 1 nM), tofacitinib citrate tun ṣe idiwọ janus kinase 2 (JAK2) ati janus kinase 1 (JAK1) pẹlu 20- ati 100-agbo kere si ni agbara lẹsẹsẹ.Sibẹsibẹ, ninu iwadi kan laipe, awọn abuda affinities (Ki) ti tofacitinib citrate si ọna JAK1, JAK2, ati JAK3 ni a royin lati jẹ 1.6 nM, 21.7 nM, ati 6.5 nM lẹsẹsẹ.

Itọkasi

Lalitha Vijayakrishnan, R. Venkataramanan ati Palak Gulati.Itoju igbona pẹlu janus kinase inhibitor CP-690,550.Awọn aṣa ni Awọn imọ-ẹrọ Pharmacological 2011: 32 (1);25-34

Itọkasi ọja

• 1. Panagi I, Jennings E, et al."Salmonella Effector SteE Yipada Serine Mammalian/Treonine Kinase GSK3 sinu Tyrosine Kinase lati Dari Polarization Macrophage."Cell Gbalejo Microbe.2020;27(1):41–53.e6.PMID: 31862381
• 2. McInnes IB, Byers NL, et al."Ifiwera ti baricitinib, upadacitinib, ati tofacitinib ilana iṣeduro ti iṣeduro cytokine ni awọn agbejade leukocyte eniyan."Arthritis Res Ther.Ọdun 2019 Oṣu Kẹjọ 2;21 (1): 183.PMID: 31375130
• 3. Liu S, Verma M, et al."Iduroṣinṣin sitẹriọdu ti ọna atẹgun iru 2 innate lymphoid ẹyin lati awọn alaisan ti o ni ikọ-fèé ti o lagbara: Ipa ti thymic stromal lymphopoietin."J Allergy Clin Immunol.2018 Jan; 141 (1): 257-268.e6.PMID: 28433687
• 4. Zheng, Lufeng, et al."3' UTR ti pseudogene CYP4Z2P ṣe igbega angiogenesis tumor ni akàn igbaya nipasẹ ṣiṣe bi ceRNA fun CYP4Z1."Iwadi ati itọju akàn igbaya (2015): 1-14.PMID: 25701119

Apejuwe

Tofacitinib citrate jẹ inhibitor JAK1/2/3 ti o wa ni ẹnu pẹlu IC50s ti 1, 20, ati 112 nM, lẹsẹsẹ.Tofacitinib citrate ni antibacterial, antifungal ati awọn iṣẹ antiviral.

Ibi ipamọ

4°C, aabo lati ina

* Ni epo: -80 ° C, 6 osu;-20°C, oṣu kan (dabobo lati ina)

Ilana kemikali

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Jẹmọ Biological Data