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| 10mg |
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| 50mg |
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| ln Vitro |
In a hypoxic microenvironment, norisoboldine (1~30 μM; 0~24 hours; CD4+T cells) activates AhR and dramatically reduces the production of miR-31 mRNA [2]. In hypoxic settings, norisoboldine (30 μM; 0~24 hours; CD4+T cells) slows glycolysis [2]. In hypoxic environments, norisoboldine (1~30 μM; 0~72 hours; Treg cells) stimulates Treg differentiation [2]. The formation of the AhR/ARNT complex, nuclear translocation of AhR, and dissociation of the HSP90/AhR complex are all facilitated by norisoboldine (10, 30 μM). In the absence of miR-31, norisoboldine stimulates the production of Treg cells in hypoxic environments [2].
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| ln Vivo |
Norisoboldine (10~40 mg/kg; oral; 20 days) considerably reduced the severity of joint swelling and erythema during the experiment [1]. Norisoboldine (40 mg/kg; ig; 10 days) promotes elevated CYP1A1 expression and inhibits Glut1 and HK2 expression in the colon [2].
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| Cell Assay |
Western Blot analysis[2]
Cell Types: CD4+T cells Tested Concentrations: 1~30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Intracellular AhR was activated under hypoxic microenvironment. RT-PCR[2] Cell Types: CD4+T cells Tested Concentrations: 1~30 μM Incubation Duration: 24 hrs (hours) Experimental Results: miR-31 mRNA expression was Dramatically down-regulated. Immunofluorescence[2] Cell Types: CD4+T cells Tested Concentrations: 30 μM Incubation Duration: 24 hrs (hours) Experimental Results: Glycolysis is inhibited during hypoxia. Cell differentiation experiment [2] Cell Types: Treg cell Tested Concentrations: 1~30 μM Incubation Duration: 72 hrs (hours) Experimental Results: Treg cell differentiation was promoted under hypoxic conditions. |
| Animal Protocol |
Animal/Disease Models: Male ICR mice (18-22 grams)
Doses: 10~40 mg/kg Route of Administration: Oral Experimental Results:The severity of joint swelling and erythema was Dramatically diminished during the experiment. Animal/Disease Models: Female C57BL/6 mice (18–22 g) Doses: 40 mg/kg Route of Administration: Ig Experimental Results: Induced enhanced CYP1A1 expression and inhibited Glut1 and HK2 expression in the colon. |
| 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. |
| Molecular Formula |
C18H19NO4
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|---|---|
| Molecular Weight |
313.3478
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| CAS # |
23599-69-1
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| Related CAS # |
Norisoboldine hydrochloride;5083-84-1
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| SMILES |
O([H])C1=C(C([H])=C2C([H])([H])C([H])([H])N([H])[C@@]3([H])C([H])([H])C4=C([H])C(=C(C([H])=C4C1=C32)OC([H])([H])[H])O[H])OC([H])([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 62.5 mg/mL (~199.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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