Olamkicept

Names

[ CAS No. ]:
1702282-14-1

[ Name ]:
Olamkicept

Biological Activity

[Description]:

Olamkicept (FE 999301) is a selective inhibitor of the soluble interleukin 6 (sIL-6R)/IL-6 complex. Olamkicept is a soluble gp130-Fc-fusion-protein and anti-inflammatory agent[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related
Research Areas >> Inflammation/Immunology

[Target]

sIL-6R/IL-6 Complex[1]


[In Vitro]

Olamkicept (10 µg/mL，60 分钟) 抑制 HREC 中 IL-6 转信号介导的 STAT3 激活[5]。 Olamkicept (10 µg/mL，60 分钟) 抑制 IL-6 转导信号诱导的 HREC 中 H2O2 水平的增加[5]. Olamkicept (10 µg/mL，60 分钟) 抑制 IL-6 转导诱导的 HREC 细胞凋亡[5]。 Olamkicept (0-1 µg/mL) 抑制 IL-11/重组 sIL-11R 诱导的 Ba/F3-gp130 细胞增殖[6]。 Western Blot Analysis[5] Cell Line: Human retinal endothelial cells (HRECs) Concentration: 10 µg/mL Incubation Time: 60 min Result: Inhibited IL-6/sIL-6R induced increase in STAT3 phosphorylation.

[In Vivo]

Olamkicept (sgp130Fc) (0.01-10 mg/kg，皮下注射) 提高盲肠结扎穿孔 (CLP) 败血症小鼠模型的存活率[3]。 Olamkicept (0.5 mg/kg，腹腔注射) 抑制盲肠结扎穿孔 (CLP) 诱导的败血症小鼠的炎症并提高存活率[4]。 Animal Model: Cecal ligation and puncture (CLP) sepsis mice model[3] Dosage: 0.01, 0.1, 1, 10 mg/kg Administration: s.c. Result: Improved survival rate and physical activity.

[References]

[1]. Schreiber S, et al. Therapeutic Interleukin-6 Trans-signaling Inhibition by Olamkicept (sgp130Fc) in Patients With Active Inflammatory Bowel Disease. Gastroenterology. 2021 Jun;160(7):2354-2366.e11.  

[2]. Zhang S, et al. Effect of Induction Therapy With Olamkicept vs Placebo on Clinical Response in Patients With Active Ulcerative Colitis: A Randomized Clinical Trial. JAMA. 2023 Mar 7;329(9):725-734.  

[3]. Barkhausen T, et al. Selective blockade of interleukin-6 trans-signaling improves survival in a murine polymicrobial sepsis model. Crit Care Med. 2011 Jun;39(6):1407-13.  

[4]. SHI Dan-dan, et al. IL-6 trans-signaling inhibitor sgp130Fc suppresses inflammation and regulates immune cells in mice with sepsis. Basic & Clinical Medicine. 2022, 42 (12): 1895-1899.

[5]. Valle ML, et al. Inhibition of interleukin-6 trans-signaling prevents inflammation and endothelial barrier disruption in retinal endothelial cells. Exp Eye Res. 2019 Jan;178:27-36.  

[6]. Lokau J, et al. Proteolytic Cleavage Governs Interleukin-11 Trans-signaling. Cell Rep. 2016 Feb 23;14(7):1761-1773.  

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds