Nuciferine

Name: Nuciferine
Brand: MedChemExpress
SKU: HY-N0049
Rating: 5.0 (8 reviews)

Cat. No.: HY-N0049 Purity: 99.90%: Data Sheet
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Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

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

CAS No. : 475-83-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Nuciferine:

Nuciferine (Standard) Get quote

8 Publications Citing Use of MCE Nuciferine

Cell Proliferation/Viability Assay

Histological Imaging/Staining

ELISA

: Nuciferine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Aug 18:S2090-1232(25)00635-6. [Abstract]; Quantitative analysis of survival rates after treatment with different concentrations of Nuciferine (NF) (0.5, 1, 2, 5, 10, 20, 50, 100 μM) and Erastin in NRCMs.

: Nuciferine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Aug 18:S2090-1232(25)00635-6. [Abstract]; Representative Western blotting images and quantitative results of TFR1, ACSL4, PTGS2, NOX1, FTH1 and GPX4 expression in left ventricular tissues treated with Nuciferine (NF)

: Nuciferine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Aug 18:S2090-1232(25)00635-6. [Abstract]; Representative images of DCFH-DA and JC-1 staining, and quantification of ROS fluorescence and JC-1 ratio in NRCMs treated with Nuciferine (NF).

: Nuciferine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Aug 18:S2090-1232(25)00635-6. [Abstract]; Representative images of H&E staining, WGA staining and PSR staining in left ventricular sections treated with Nuciferine (NF) (30 mg/kg, p.o.).

: Nuciferine purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Aug 18:S2090-1232(25)00635-6. [Abstract]; Quantification of heart tissue levels of IL-6, IL-1b, and TNF-a treated with Nuciferine (NF) (30 mg/kg, p.o.).

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

5-HT_2C Receptor

131 nM (IC₅₀)

Schistosome

5-HT_1A Receptor

5-HT_2A Receptor

5-HT_2B Receptor

5-HT_2C Receptor

5-HT₇ Receptor

150 nM (IC₅₀)

5-HT_2A Receptor

478 nM (IC₅₀)

5-HT_2B Receptor

1 μM (IC₅₀)

5-HT₆ Receptor

700 nM (EC₅₀)

5-HT_1A Receptor

3.2 μM (EC₅₀)

D₂ Receptor

64 nM (EC₅₀)

D₄ Receptor

2 μM (EC₅₀)

D₅ Receptor

2.6 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
B16-4A5	IC₅₀	15.8 μM Compound: 2	Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry Inhibition of melanogenesis in mouse B16-4A5 cells after 72 hrs by spectrophotometry	[PMID: 23270663]

In Vitro

Nuciferine is a partial agonist at DD₂ receptor with an activity (E_max=67% of dopamine) similar to aripiprazole (E_max=50% of dopamine). In line with its partial agonist activity, Nuciferine inhibited dopamine-induced activation of G_i with a potency similar to clozapine (Nuciferine K_B=62 nM; Clozapine K_B=20 nM) as determined via Schild regression analysis^[1]. The natural product Nuciferine acts as an effective inhibitor of adult worm motility. Nuciferine is effective at inhibiting both basal and 5-HT evoked motility of adult schistosomes. Nuciferine inhibits Sm.5HTR_L and schistosomule with 0.24±0.04 and 0.62±0.22 μM, respectively^[2].

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

In Vivo

In rodent models relevant to antipsychotic drug action, Nuciferine blocks head-twitch responses and discriminative stimulus effects of a 5-HT_2A agonist, substituted for clozapine discriminative stimulus, enhanced amphetamine induced locomotor activity, inhibited phencyclidine (PCP)-induced locomotor activity, and rescued PCP-induced disruption of prepulse inhibition without induction of catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP doses produce similar substitution to PCP alone. In the clozapine-trained animals, a dose-dependent substitution for 1.25 mg/kg clozapine is seen at 10 mg/kg Nuciferine (80.63% drug lever responding), with an ED₅₀ value of 5.42 mg/kg (95% CI 3.09-9.48 mg/kg) while the lower doses tested (0.1 mg/kg-3 mg/kg) fails to produce substitution for clozapine’s discriminative cue. In addition to a high percentage of responding on the clozapine-appropriate lever, 10 mg/kg Nuciferine also produces significant rate suppression as compared to vehicle control points (p<0.001)^[1].

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

Molecular Weight

295.38

Formula

C₁₉H₂₁NO₂

CAS No.

475-83-2

Appearance

Solid

Color

White to off-white

SMILES

CN1CCC2=CC(OC)=C(OC)C3=C2[C@@]1([H])CC4=CC=CC=C34

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (16.93 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	3.3855 mL	16.9273 mL	33.8547 mL
5 mM	0.6771 mL	3.3855 mL	6.7709 mL
10 mM	0.3385 mL	1.6927 mL	3.3855 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 1.11 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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: ≥ 1.11 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.11 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 1.11 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.1 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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: 99.90%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (256 KB) HNMR (248 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Farrell MS, et al. In Vitro and In Vivo Characterization of the Alkaloid Nuciferine. PLoS One. 2016 Mar 10;11(3):e0150602. [Content Brief]

[2]. Chan JD, et al. Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist. Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):364-370. [Content Brief]

Kinase Assay ^[1]	For affinity determination, Nuciferine is subjected to primary radioligand binding assays tested at a single 10 μM concentration to displace 50% of the radioligand at a given receptor target. If a more than 50% of the radioligand is displaced, Nuciferine is selected for a secondary binding assay tested at 11 concentrations in triplicate in competition with the radioligand to generate an IC₅₀ and K_i. Binding assays are performed in 96-well plates with 125 μL per well in appropriate binding buffer using radioligand at or near the K_d. Plates are incubated at room temperature in the dark for 90 min. Reactions are stopped by vacuum filtrations onto 0.3% polyethyleneimine soaked 96-well filter mats using a 96-well Filtermate harvester, followed by at least three washes of cold wash buffer. Scintillation cocktail is melted onto dried filters and radioactivity is counted using a Wallac Trilux Microbeta^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are plated into 48-well plates one day before uptake is performed. Cells are washed with 0.5 mL uptake buffer (4 mM Tris, 6.25 mM HEPES, 120 mM NaCl, 5 mM KCl, 1.2 mM CaCl₂, 1.2 mM MgSO₄, 5.6 mM D-glucose, 1.7 mM ascorbic acid, and 1 μM pargyline, pH 7.4). Cells are incubated with 225 μL uptake buffer with or without the indicated concentration of Nuciferine for 15 minutes. After incubation, 25 μL uptake buffer containing ³H-DA and DA is added for a final concentration of 20 nM ³H-DA and 1 μM DA. Cells are incubated at 37°C for 20 minutes or for the time indicated. Nonspecific uptake is determined in the presence of 10 μM nomifensine. Uptake is terminated by aspirating uptake buffer and washing each well twice with 0.5 mL ice-cold uptake buffer. Cells are lysed in 0.1 N NaOH and transferred to vials containing 3 mL scintillation cocktail. Radioactivity is quantitated using a Beckman LS6500 counter. Data are analyzed in Graph Pad Prism 5.0^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Adult male NIH Swiss mice weighing approximately 25 g are used. Mice are injected with either Nuciferine (1, 3, or 10 mg/kg, i.p.) or vehicle, n=4 mice/condition. Fifteen minutes later, mice are injected with 1 mg/kg DOI (i.p.) and immediately placed in an observation chamber (new cage without bedding). Head-twitches (operationally defined as a rapid rotational jerk of the head that can be distinguished from species-appropriate grooming or scratching behaviors) are counted for 20 minutes in 5 minute bins. For the time-course study, mice are pretreated with 3.0 mg/kg Nuciferine (i.p.) at 60, 45, 30, 15, or 0 minutes (co-injection) prior to the 1.0 mg/kg DOI (i.p.) injection, and head-twitches are counted as described above. In one experiment, mice (n=4 per condition) are pretreated with an injection (s.c.) of 3.0 mg/kg Nuciferine or vehicle 15 minutes prior to 1.0 mg/kg DOI injection (i.p.) and head-twitches are counted as described above. All experiments are performed by 3 observers, with 2 observers blinded to the experimental conditions which are evenly distributed. Power analyses are performed with the resulting data. The two highest doses of Nuciferine tested (10 and 3 mg/kg), had 0.96 and 0.88 power to detect significance (α=0.05). As these experiments are performed blinded and in distinct mice, further replication is not performed. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Farrell MS, et al. In Vitro and In Vivo Characterization of the Alkaloid Nuciferine. PLoS One. 2016 Mar 10;11(3):e0150602. [Content Brief] [2]. Chan JD, et al. Pharmacological profiling an abundantly expressed schistosome serotonergic GPCR identifies nuciferine as a potent antagonist. Int J Parasitol Drugs Drug Resist. 2016 Dec;6(3):364-370. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3855 mL	16.9273 mL	33.8547 mL	84.6367 mL
	5 mM	0.6771 mL	3.3855 mL	6.7709 mL	16.9273 mL
	10 mM	0.3385 mL	1.6927 mL	3.3855 mL	8.4637 mL
	15 mM	0.2257 mL	1.1285 mL	2.2570 mL	5.6424 mL

Nuciferine Related Classifications

Neurological Disease

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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.

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Nuciferine

Customer Review

Other Forms of Nuciferine:

Nuciferine Related Antibodies

8 Publications Citing Use of MCE Nuciferine

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References

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Nuciferine Related Antibodies

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Complete Stock Solution Preparation Table

Nuciferine Related Classifications

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