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Neferine NF-κB inhibitor

Name: Neferine
Brand: Selleck Chemicals
SKU: S5144
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S5144

Neferine ((R)-1,2-Dimethoxyaporphine), a natural component of Nelumbo nucifera, has antitumor efficiency. It induces apoptosis in renal cancer cells. This compound prevents autophagy through activation of Akt/mTOR pathway and Nrf2 in muscle cells. It strongly inhibits NF-κB activation. It possesses a number of therapeutic effects such as anti-diabetic, anti-aging, anti-microbial, anti-thrombotic, anti-arrhythmic, anti-inflammatory and even anti-HIV.

Chemical Structure

Molecular Weight: 624.77

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other NF-κB Products	Omaveloxolone (RTA-408) DCZ0415 BAY 11-7082 (BAY 11-7821) JSH-23 QNZ (EVP4593) SC75741 Caffeic Acid Phenethyl Ester DHA (Dihydroartemisinin) Andrographolide Evodiamine

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (160.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5mg/ml (8.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.71mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	624.77	Formula	C₃₈H₄₄N₂O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2292-16-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	(R)-1,2-Dimethoxyaporphine			Smiles	CN1CCC2=CC(=C(C=C2C1CC3=CC=C(C=C3)OC)OC4=C(C=CC(=C4)CC5C6=CC(=C(C=C6CCN5C)OC)OC)O)OC

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB
In vitro	Neferine induces reactive oxygen species mediated caspase-dependent apoptosis in liver and lung cancer cells, reverses the multidrug resistance in human breast cancer cells (MCF-7/ADM), human hepatocarcinoma (HepG2/ADR) and human gastric carcinoma cells (SGC7901/VCR). This compound enhances the cytotoxic potential of cisplatin in A549 cells and augments cisplatin inducecd Sub-G1 accumulation. It inhibits the migration and invasion of human lung cancer cells and lowers the antioxidant enzyme activities. This chemical sensitizes the lung cancer cells to cisplatin and induces apoptosis through G1 cell cycle arrest, upstream ROS production, depletion of cellular antioxidant pool, reduction of mitochondrial membrane potential (ΔΨm) with increased expression of Bax, Bad, Bak, down regulates the expression of Bcl2, release of cytochrome c, cleaved caspase-9, cleaved caspase-3 and PARP.
In vivo	Neferine has an antifibrosis effect on CCl4-induced hepatic fibrosis in mice, possibly partly due to the decreased expression of TGF-β1 in the liver. The plasma concentration-time curves of this compound (10, 20 and 50 mg/kg, i.g.) shows double absorption peaks with the first peak at 10 min and the second peak at 1 h. The t^β_1/2 are 15.6 h, 22.9 h and 35.5 h, for each of these doses, respectively. This compound distributes rapidly into different organ systems, with the highest concentrations found in the liver, followed by the lung, kidney and heart at doses of 10 or 20 mg/kg. At 50 mg/kg dose, concentrations of the kidney and lung are higher than those of others. Moreover, this compound is mainly metabolized in the liver and converted partially by CYP2D6 to liensinine, isoliensinine, desmethyl-liensinine and desmethyl-isoliensinine.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28214344/ [2] https://pubmed.ncbi.nlm.nih.gov/25800905/ [3] https://pubmed.ncbi.nlm.nih.gov/17654697/ [4] https://pubmed.ncbi.nlm.nih.gov/27041079/

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