| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Plasmodium Dopamine Receptor serotonergic receptor
Asimilobine primarily targets the dopamine biosynthesis pathway and acts as a serotonergic receptor antagonist. It inhibits dopamine biosynthesis by reducing tyrosine hydroxylase (TH) activity and TH mRNA expression. It also targets Plasmodium, dopamine receptor, and 5-HT receptor. |
|---|---|
| ln Vitro |
Asimilobine (0.05-0.2 μM) exhibits a concentration-dependent, substantial suppression of intracellular dopamine levels over a 24-hour period, with an IC50 value of 0.13 μM[2]. At 24 hours, asimilobine (0.15 μM) suppresses the activities of both aromatic L-amino acid decarboxylase (AADC) and tyrosine hydroxylase (TH)[2]. Additionally, asimilobine reduces intracellular cyclic AMP levels and TH mRNA levels[2].
Asimilobine (0.05-0.2 μM; for 24 h) shows significant inhibition of intracellular dopamine levels in a concentration-dependent manner with an IC50 of 0.13 μM. Asimilobine (0.15 μM) inhibits tyrosine hydroxylase (TH) and aromatic L-amino acid decarboxylase (AADC) activities at 24 h. It also decreases TH mRNA levels and intracellular cyclic AMP levels. It displays weak inhibition against Streptococcus mutans with a MIC of 0.25 mg/mL. |
| ln Vivo |
In vivo activity data for asimilobine are limited. As a natural product with antimalarial and anticancer activities, it has been studied in various disease models. The compound shows effects on the central nervous system producing depression in rabbits. Further in vivo studies are needed to fully characterize its pharmacological effects.
|
| Enzyme Assay |
In vitro enzyme assays typically measure inhibition of tyrosine hydroxylase (TH) and aromatic L-amino acid decarboxylase (AADC) activities in cell lysates. Dopamine levels are quantified using HPLC or other analytical methods after treatment with asimilobine. Serotonergic receptor antagonism is assessed using receptor binding assays.
|
| Cell Assay |
Cell-based assays use PC12 cells treated with asimilobine (0.05-0.2 μM) for 24 hours. Intracellular dopamine levels are measured to determine the IC50 for dopamine biosynthesis inhibition. TH mRNA levels and intracellular cAMP levels are also quantified.
|
| Animal Protocol |
In vivo animal studies for asimilobine are limited. The compound has been reported to produce central nervous system depression in rabbits. Further studies in disease models such as malaria or cancer xenografts would be required to fully evaluate its in vivo efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for asimilobine are limited. As a natural isoquinoline alkaloid, its absorption, distribution, metabolism, and excretion properties have not been extensively characterized. Further pharmacokinetic studies are needed to determine its bioavailability and metabolic stability.
|
| Toxicity/Toxicokinetics |
Toxicological data for asimilobine are limited. As a natural product with multiple biological activities, its safety profile has not been fully established. Standard laboratory safety precautions should be followed when handling this compound. Further toxicity studies are needed for comprehensive safety assessment.
|
| References | |
| Additional Infomation |
R-(-)-Acimilobine is an apophene alkaloid that functions as a metabolite. It has been reported to be found in Magnolia officinalis, Longan arguta from Taiwan, and other organisms with relevant data.
Asimilobine is an aporphine isoquinoline alkaloid with diverse biological activities including dopamine biosynthesis inhibition, serotonergic receptor antagonism, antimalarial, anticancer, antioxidative, anti-AChE, anti-α-glucosidase, anti-leishmanial, and antifungal properties. It is a valuable natural product for research in neuroscience, infectious diseases, and cancer. |
| Molecular Formula |
C17H17NO2
|
|---|---|
| Molecular Weight |
267.32
|
| Exact Mass |
267.125
|
| CAS # |
6871-21-2
|
| PubChem CID |
160875
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
472.5±45.0 °C at 760 mmHg
|
| Melting Point |
177-179℃ (acetone )
|
| Flash Point |
239.6±28.7 °C
|
| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.638
|
| LogP |
2.46
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
361
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O(C([H])([H])[H])C1=C(C([H])=C2C([H])([H])C([H])([H])N([H])[C@]3([H])C([H])([H])C4=C([H])C([H])=C([H])C([H])=C4C1=C32)O[H]
|
| InChi Key |
NBDNEUOVIJYCGZ-CYBMUJFWSA-N
|
| InChi Code |
InChI=1S/C17H17NO2/c1-20-17-14(19)9-11-6-7-18-13-8-10-4-2-3-5-12(10)16(17)15(11)13/h2-5,9,13,18-19H,6-8H2,1H3/t13-/m1/s1
|
| Chemical Name |
(6aR)-1-methoxy-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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 3.7408 mL | 18.7042 mL | 37.4083 mL | |
| 5 mM | 0.7482 mL | 3.7408 mL | 7.4817 mL | |
| 10 mM | 0.3741 mL | 1.8704 mL | 3.7408 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.
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