2. GPCR/G Protein
  3. Adenosine Receptor
  4. Norisoboldine hydrochloride

Norisoboldine hydrochloride  (Synonyms: (+)-Laurelliptine hydrochloride)

Cat. No.: HY-N0586A
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Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.

For research use only. We do not sell to patients.

Norisoboldine hydrochloride Chemical Structure

Norisoboldine hydrochloride Chemical Structure

CAS No. : 5083-84-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Norisoboldine hydrochloride:

Norisoboldine hydrochloride Related Antibodies

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Description

Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, 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 hydrochloride (1~30 μM; 0~24 hours; CD4+T cells) activates AhR under hypoxic microenvironment and significantly downregulates mRNA expression of miR-31[2].
Norisoboldine hydrochloride (30 μM; 0~24 hours; CD4+T cells) inhibits glycolysis in hypoxia[2].
Norisoboldine hydrochloride (1~30 μM; 0~72 hours; Treg cells) promotes Treg differentiation in hypoxia[2].
Norisoboldine hydrochloride (10, 30 μM) facilitates the disassociation of HSP90/AhR complexes, the nuclear translocation of AhR, and the formation of AhR/ARNT complexes. Norisoboldine hydrochloride induces generation of Treg cells in hypoxia[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Norisoboldine hydrochloride Related Antibodies

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.

Immunofluorescence[2]

Cell Line: Treg cells
Concentration: 1~30 μM
Incubation Time: 72 hours
Result: Promoted Treg differentiation in hypoxia.
In Vivo

Norisoboldine hydrochloride (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 hydrochloride (40 mg/kg; i.g.; 10 days) induces enhancement of CYP1A1 expression and suppresses expressions of Glut1 and HK2 in colons[2].

MedChemExpress (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.
Molecular Weight

349.81

Formula

C18H20ClNO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.OC1=C(OC)C=C2CCN[C@@]3([H])CC4=CC(O)=C(OC)C=C4C1=C23
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (285.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8587 mL 14.2935 mL 28.5869 mL
5 mM 0.5717 mL 2.8587 mL 5.7174 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8587 mL 14.2935 mL 28.5869 mL 71.4674 mL
5 mM 0.5717 mL 2.8587 mL 5.7174 mL 14.2935 mL
10 mM 0.2859 mL 1.4293 mL 2.8587 mL 7.1467 mL
15 mM 0.1906 mL 0.9529 mL 1.9058 mL 4.7645 mL
20 mM 0.1429 mL 0.7147 mL 1.4293 mL 3.5734 mL
25 mM 0.1143 mL 0.5717 mL 1.1435 mL 2.8587 mL
30 mM 0.0953 mL 0.4764 mL 0.9529 mL 2.3822 mL
40 mM 0.0715 mL 0.3573 mL 0.7147 mL 1.7867 mL
50 mM 0.0572 mL 0.2859 mL 0.5717 mL 1.4293 mL
60 mM 0.0476 mL 0.2382 mL 0.4764 mL 1.1911 mL
80 mM 0.0357 mL 0.1787 mL 0.3573 mL 0.8933 mL
100 mM 0.0286 mL 0.1429 mL 0.2859 mL 0.7147 mL
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Norisoboldine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Norisoboldine5083-84-1(+)-LaurelliptineAdenosine ReceptorP1 receptororallynaturalisoquinolinealkaloidradixlinderaearthritisUCDSSInhibitorinhibitorinhibit

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