| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
| ln Vitro |
Similar to aripiprazole (Emax=50% of dopamine), nuciferine is a partial agonist at the DD2 receptor with action (Emax=67% of dopamine). Nuciferine is as effective as clozapine (Nuciferine KB=62 nM; Clozapine KB=20 nM) at blocking Gi activation of dopamine inducers, which is consistent with its partial agonist action, according to Schild regression analysis [1]. Nuciferine, a naturally occurring substance, effectively inhibits the movement of insects. Schistosoma adenalis's basal motility and 5-HT-induced motility can both be successfully inhibited by nuciferine. Nuciferine inhibits Schistosoma at 0.62±0.22 μM and Sm.5HTRL at 0.24±0.04 μM, respectively [2].
|
|---|---|
| ln Vivo |
In dental animal models related to the effects of antipsychotic drugs, nuciferine expands the apical response and prestimulatory effects of 5-HT2A agonists, replaces the precise stimulation of clozapine, enhances amphetamine-induced locomotor activity, and inhibits phencyclidine Piperidine (PCP)-induced locomotor activity and relieves PCP-induced prepulse inhibition but does not induce catalepsy. In the presence of 1 or 3 mg/kg Nuciferine, cumulative PCP dosages resulted in equivalent replacement to PCP alone. In clozapine-trained animals, a dose-dependent substitution of 1.25 mg/kg Clozapine was observed with 10 mg/kg Nuciferine (80.63% drug lever response), with an ED50 value of 5.42 mg/kg (95% CI 3.09-9.48 mg )/kg), whereas the lower doses tested (0.1 mg/kg-3 mg/kg) failed to produce discriminative cues for clozapine. In addition to eliciting a high number of responses to clozapine suitable levers, 10 mg/kg Nuciferine generated considerable gradient suppression (p<0.001) compared to vehicle control points [1].
|
| References |
[1]. Farrell MS, et al. In Vitro and In Vivo Characterization of the Alkaloid Nuciferine. PLoS One. 2016 Mar 10;11(3):e0150602.
[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 |
| Additional Infomation |
Nuciferine has been reported in Ziziphus jujuba, Paliurus hemsleyanus, and other organisms with data available.
|
| Molecular Formula |
C19H21NO2
|
|---|---|
| Molecular Weight |
295.3755
|
| Exact Mass |
295.157
|
| CAS # |
475-83-2
|
| PubChem CID |
10146
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
430.7±45.0 °C at 760 mmHg
|
| Melting Point |
165.5°C
|
| Flash Point |
151.9±17.3 °C
|
| Vapour Pressure |
0.0±1.0 mmHg at 25°C
|
| Index of Refraction |
1.597
|
| LogP |
4.12
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
401
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C([H])([H])C([H])([H])N(C([H])([H])[H])[C@]3([H])C([H])([H])C4=C([H])C([H])=C([H])C([H])=C4C1=C32)OC([H])([H])[H]
|
| InChi Key |
ORJVQPIHKOARKV-OAHLLOKOSA-N
|
| InChi Code |
InChI=1S/C19H21NO2/c1-20-9-8-13-11-16(21-2)19(22-3)18-14-7-5-4-6-12(14)10-15(20)17(13)18/h4-7,11,15H,8-10H2,1-3H3/t15-/m1/s1
|
| Chemical Name |
(6aR)-1,2-dimethoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline
|
| 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 |
| 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 : ~5 mg/mL (~16.93 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.11 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.11 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04148677 | Unknown status | Dietary Supplement: Protoves M1® | Bladder Cancer LUTS Pain |
Cardarelli Hospital | 2019-12-01 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
