Norisoboldine

Research use only, not for human use.

Norisoboldine might be a potential therapeutic agent for rheumatoid arthritis, and it functions through protecting joint destruction as well as regulating the abnormal immune responses.

Norisoboldine might be a potential therapeutic agent for rheumatoid arthritis, and it functions through protecting joint destruction as well as regulating the abnormal immune responses. Norisoboldine inhibits the macrophage activation and the resultant production of pro-inflammatory cytokines via down-regulating the activation of MAPKs signaling pathways rather than NF-κB.(In Vitro):Norisoboldine (1~30 μM; 0~24 hours; CD4+T cells) activates AhR under hypoxic microenvironment and significantly downregulates mRNA expression of miR-31.Norisoboldine (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia.Norisoboldine (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia.Norisoboldine (10, 30 μM) facilitates the disassociation of HSP90/AhR complexes, the nuclear translocation of AhR, and the formation of AhR/ARNT complexes. Norisoboldine induces generation of Treg cells in hypoxia is independent of miR-31.(In Vivo):Norisoboldine (10~40 mg/kg; p.o.; 20 days) significantly reduces the severity of joint swelling and erythema during the course of the experiment.Norisoboldine (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons.

Norisoboldine (1~30 μM; 0~24 hours; CD4+T cells) activates AhR under hypoxic microenvironment and significantly downregulates mRNA expression of miR-31.Norisoboldine (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia.Norisoboldine (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia.Norisoboldine (10, 30 μM) facilitates the disassociation of HSP90/AhR complexes, the nuclear translocation of AhR, and the formation of AhR/ARNT complexes. Norisoboldine induces generation of Treg cells in hypoxia is independent of miR-31. Western Blot Analysis Cell Line:CD4+T cells Concentration:1~30 μM Incubation Time:24 hours Result:Activated AhR in cells under hypoxic microenvironment.RT-PCRCell Line:CD4+T cells Concentration:1~30 μM Incubation Time:24 hours Result:Significantly downregulated mRNA expression of miR-31.Immunofluorescence Cell Line:CD4+T cells Concentration:30 μM Incubation Time:24 hours Result:Inhibited glycolysis in hypoxia. Cell Differentiation Assay Cell Line:Treg cells Concentration:1~30 μM Incubation Time:72 hours Result:Promoted Treg differentiation in hypoxia.

Norisoboldine (10~40 mg/kg; p.o.; 20 days) significantly reduces the severity of joint swelling and erythema during the course of the experiment.Norisoboldine (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons. Animal Model:Male ICR mice (18–22 g)Dosage:10~40 mg/kg Administration:P.o.Result:Significantly reduced the severity of joint swelling and erythema during the course of the experiment.Animal Model:Female C57BL/6 mice (18–22 g)Dosage:40 mg/kg Administration:I.g.Result:Induced enhancement of CYP1A1 expression and suppressed expressions of Glut1 and HK2 in colons.

——

Others

Other Targets

MAPK

Inflammation/Immunology

——

23599-69-1

313.35

C18H19NO4

>98% (HPLC)

In Vitro:?DMSO : ≥ 62.5 mg/mL (199.46 m)

COC1=C(C2=C3C(CC4=CC(=C(C=C42)OC)O)NCCC3=C1)O

——

(-20℃)

With Ice Pack

≥ 2 years