[CAS NO. 23599-69-1] Norisoboldine
PRODUCTS SPECIFICATIONS [23599-69-1]
DESCRIPTION [23599-69-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 313.35 |
| Molecular Formula | C18H19NO4 |
| SMILES | OC1=C(OC)C=C2CCN[C@@]3([H])CC4=CC(O)=C(OC)C=C4C1=C23 |
Summary
Norisoboldine is an orally active natural aryl hydrocarbon receptor ( AhR ) agonist. Norisoboldine, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis [1] [2] .
IC50 & Target
AhR [2]
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
[2]
.
Norisoboldine (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia
[2]
.
Norisoboldine (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia
[2]
.
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
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [2]
| Cell Line: | CD4+T cells |
| Concentration: | 1~30 μM |
| Incubation Time: | 24 hours |
| Result: | Activated AhR in cells under hypoxic microenvironment. |
RT-PCR [2]
| Cell Line: | CD4+T cells |
| Concentration: | 1~30 μM |
| Incubation Time: | 24 hours |
| Result: | Significantly downregulated mRNA expression of miR-31. |
Immunofluorescence [2]
| Cell Line: | CD4+T cells |
| Concentration: | 30 μM |
| Incubation Time: | 24 hours |
| Result: | Inhibited glycolysis in hypoxia. |
Cell Differentiation Assay [2]
| Cell Line: | Treg cells |
| Concentration: | 1~30 μM |
| Incubation Time: | 72 hours |
| Result: | Promoted Treg differentiation in hypoxia. |
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
[1]
.
Norisoboldine (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : ≥ 62.5 mg/mL ( 199.46 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.1913 mL | 15.9566 mL | 31.9132 mL |
| 5 mM | 0.6383 mL | 3.1913 mL | 6.3826 mL |
| 10 mM | 0.3191 mL | 1.5957 mL | 3.1913 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.64 mM); Clear solution
References
- [1] Luo Y, et al. Therapeutic effect of norisoboldine, an alkaloid isolated from Radix Linderae, on collagen-induced arthritis in mice. Phytomedicine. 2010;17(10):726-731.
- [2] Lv Q, et al. Norisoboldine, a natural AhR agonist, promotes Treg differentiation and attenuates colitis via targeting glycolysis and subsequent NAD+/SIRT1/SUV39H1/H3K9me3 signaling pathway. Cell Death Dis. 2018;9(3):258. Published 2018 Feb 15.
Synonyms