2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Lupanine

Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM.

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Lupanine Chemical Structure

Lupanine Chemical Structure

CAS No. : 550-90-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Lupanine:

Lupanine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Lupanine (D-Lupanine) is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM[1].

IC50 & Target

Ki: 500 nM (Nicotinic receptor) and 11000 nM (Muscarinic receptor)[1]
In Vitro

Lupanine shows binding affinity for nicotinic receptor with a Ki value of 500 nM. While, Lupanine shows a very weak affinity for the muscarinic receptor with a Ki value of 11000 nM[1].
Lupanine (0-100 μM) is a weak agonist and desensitizer in SH-SY5Y cells, with EC50 and DC50 of 10.7 μM and 28.2 μM, respectively[2].

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

Lupanine Related Antibodies
In Vivo

Lupanine (100-300 mg/kg for i.p.; 175-700 mg/kg for p.o.) is much less toxic in one single injection in EOPS male Swiss mice (20-22 g) and Hartley guinea-pigs (400-500 g)[1].
Lupanine (1-7.5 mg/kg; i.v.) is more efficient than Sparteine for antagonizing secondary reflex hypertension in carotid occlusion and hypotension resulting from the stimulation of the pneumogastric nerve in both the cat and the dog[1].
Lupanine has an inhibitory action on nicotinic type hypertension produced by injection of Acetylcholine (500 p.g/kg i.v.) in the Atropine-treated dog[1].

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

248.36

Formula

C15H24N2O
CAS No.
Appearance

Liquid (Density: 0.9789 g/cm3)

Color

Colorless to light yellow

SMILES

O=C1N2[C@]([C@](C3)([H])CN(CCCC4)[C@]4([H])[C@]3([H])C2)([H])CCC1
Structure Classification
Initial Source
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
In Vitro: 

DMSO : ≥ 50 mg/mL (201.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0264 mL 20.1321 mL 40.2641 mL
5 mM 0.8053 mL 4.0264 mL 8.0528 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 1.25 mg/mL (5.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (5.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 (protect from light)

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

Purity: 98.04%

SDS (393 KB)

COA (252 KB) HNMR (269 KB) LCMS (217 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 4.0264 mL 20.1321 mL 40.2641 mL 100.6603 mL
5 mM 0.8053 mL 4.0264 mL 8.0528 mL 20.1321 mL
10 mM 0.4026 mL 2.0132 mL 4.0264 mL 10.0660 mL
15 mM 0.2684 mL 1.3421 mL 2.6843 mL 6.7107 mL
20 mM 0.2013 mL 1.0066 mL 2.0132 mL 5.0330 mL
25 mM 0.1611 mL 0.8053 mL 1.6106 mL 4.0264 mL
30 mM 0.1342 mL 0.6711 mL 1.3421 mL 3.3553 mL
40 mM 0.1007 mL 0.5033 mL 1.0066 mL 2.5165 mL
50 mM 0.0805 mL 0.4026 mL 0.8053 mL 2.0132 mL
60 mM 0.0671 mL 0.3355 mL 0.6711 mL 1.6777 mL
80 mM 0.0503 mL 0.2517 mL 0.5033 mL 1.2583 mL
100 mM 0.0403 mL 0.2013 mL 0.4026 mL 1.0066 mL
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Lupanine 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:

Lupanine550-90-3D-LupaninenAChRNicotinic acetylcholine receptorsSparteineketonic derivativeganglioplegic activitynicotinic receptorSH-SY5Y cellsInhibitorinhibitorinhibit

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