| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
O-Nornuciferine targets the hERG (human Ether-à-go-go-Related Gene) potassium channel. It is a potent hERG channel inhibitor. By blocking the hERG channel, the compound modulates potassium ion flow, which is involved in cardiac action potential repolarization. This makes it a valuable tool for studying cardiac electrophysiology and for assessing the potential cardiotoxicity of other compounds.
|
|---|---|
| ln Vitro |
O-nornuciferine's in vitro hERG blockages in HEK293 cells had an IC50 of 7.91 μM[1]. In Xenopus oocytes, lotus alkaloids block the hERG channel 47% when O-nornuciferine (100 μM) is present[1].
In vitro, O-Nornuciferine reveals distinct hERG blockages measured in HEK293 cells with an IC50 value of 2.89 μM. In a screening study of herbal materials for hERG blockers, the alkaloid fraction of lotus leaf caused about 50% hERG current inhibition at 100 μg/mL. O-Nornuciferine was identified as one of the compounds responsible for this effect. Standard in vitro assays include electrophysiological recordings using automated two-microelectrode voltage clamp in Xenopus oocytes or patch-clamp in HEK293 cells. |
| ln Vivo |
In vivo, O-Nornuciferine has been studied for its antioxidant, anti-inflammatory, and neuroactive properties. As a hERG channel inhibitor, it may affect cardiac function in vivo. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool for studying hERG channel function and cardiotoxicity.
|
| Enzyme Assay |
For non-cell-based receptor binding assays, O-Nornuciferine can be evaluated using membrane preparations from cells expressing hERG channels. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-dofetilide. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration. Non-specific binding is determined in the presence of excess unlabeled dofetilide. IC50 values are calculated from displacement curves.
|
| Cell Assay |
For in vitro cellular assays, HEK293 cells expressing hERG channels are cultured in appropriate media. For functional assays, whole-cell patch-clamp electrophysiology is performed to record hERG currents. Cells are treated with various concentrations of O-Nornuciferine, and the reduction in hERG current amplitude is measured. IC50 values are calculated from concentration-response curves. Alternatively, automated two-microelectrode voltage clamp in Xenopus oocytes can be used.
|
| Animal Protocol |
For in vivo animal studies, O-Nornuciferine can be administered to rodents via intraperitoneal injection. In models of cardiac function, ECG parameters such as QT interval are monitored following compound administration to assess hERG-related cardiotoxicity. In models of inflammation or oxidative stress, the compound's protective effects are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels.
|
| ADME/Pharmacokinetics |
O-Nornuciferine has a molecular weight of 281.35 g/mol and a molecular formula of C18H19NO2. It has a predicted density of 1.216 g/cm3. The compound is soluble in DMSO at 50 mg/mL (177.71 mM). It should be stored as a powder at -20°C for up to 3 years or in solvent at -80°C for up to 1 year. It is for research use only and is not intended for human consumption.
|
| Toxicity/Toxicokinetics |
The toxicity profile of O-Nornuciferine is related to its hERG channel inhibitory activity. hERG channel blockade is associated with prolonged QT interval and increased risk of cardiac arrhythmias. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound.
|
| References | |
| Additional Infomation |
O-Nornuciferine has been reported in Stephania cephalantha, Ziziphus jujuba, and other organisms with available data.
See also: Floribundine (note moved to). O-Nornuciferine (CAS 3153-55-7) is a porphyrin alkaloid isolated from lotus leaf. It is a potent hERG channel inhibitor with an IC50 of 2.89 μM in HEK293 cells. The compound has been studied for its antioxidant, anti-inflammatory, and neuroactive properties. It is available for research purposes only. |
| Molecular Formula |
C18H19NO2
|
|---|---|
| Molecular Weight |
281.35
|
| Exact Mass |
281.141
|
| CAS # |
3153-55-7
|
| PubChem CID |
197017
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
451.4±45.0 °C at 760 mmHg
|
| Melting Point |
195-197℃ (ethyl acetate )
|
| Flash Point |
226.8±28.7 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.634
|
| LogP |
3.36
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
21
|
| Complexity |
387
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CN1CCC2=CC(=C(C3=C2[C@H]1CC4=CC=CC=C43)OC)O
|
| InChi Key |
AKXOIHNFHOEPHN-CQSZACIVSA-N
|
| InChi Code |
InChI=1S/C18H19NO2/c1-19-8-7-12-10-15(20)18(21-2)17-13-6-4-3-5-11(13)9-14(19)16(12)17/h3-6,10,14,20H,7-9H2,1-2H3/t14-/m1/s1
|
| Chemical Name |
(6aR)-1-methoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-2-ol
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 50 mg/mL (177.71 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5543 mL | 17.7715 mL | 35.5429 mL | |
| 5 mM | 0.7109 mL | 3.5543 mL | 7.1086 mL | |
| 10 mM | 0.3554 mL | 1.7771 mL | 3.5543 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
