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

Jẹmọ Biological Data

Jẹmọ Biological Data

Jẹmọ Biological Data

Jẹmọ Biological Data

Jẹmọ Biological Data