| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Lirinidine targets multiple pathways. It has antioxidative activity, likely through its ability to chelate metal ions and scavenge free radicals. It inhibits the proliferation of melanoma cells, suggesting activity against cancer cell growth. It also shows potent inhibition of melanogenesis, indicating activity against melanin production. The compound inhibits platelet aggregation induced by collagen, arachidonic acid, and platelet-activating factor, suggesting anti-thrombotic activity. It is also a selective alpha-2 adrenergic receptor agonist used in the treatment of hypertension and has spasmolytic actions.
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| ln Vitro |
In vitro, Lirinidine exhibits antioxidative activity with moderate iron-reducing power and minor free radical scavenging ability. It significantly inhibits the proliferation of melanoma cells (A375). It also shows potent inhibition of melanogenesis. Additionally, Lirinidine significantly inhibits collagen, arachidonic acid, and platelet-activating factor-induced platelet aggregation. These in vitro activities confirm its multi-targeted pharmacological profile.
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| ln Vivo |
In vivo, Lirinidine relaxes smooth musculature and possesses hypotensive and spasmolytic actions. It has been reported to have an LD50 of 9.8 mg/kg (i.v.) and 21.3 mg/kg (s.c.) in mice. As a selective alpha-2 adrenergic receptor agonist, it is used in the treatment of hypertension. Detailed in vivo efficacy data from animal models are not extensively reported in the available literature. Its spasmolytic and hypotensive actions suggest potential therapeutic applications in cardiovascular and gastrointestinal disorders.
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| Enzyme Assay |
Non-cell-based assays for Lirinidine include antioxidant activity assays such as DPPH radical scavenging, ABTS radical scavenging, and ferric reducing power (FRAP) assays. The compound is incubated with the radical or reducing agent, and the change in absorbance is measured spectrophotometrically. Metal chelating activity may also be assessed. Platelet aggregation assays can be performed using platelet-rich plasma and aggregometry.
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| Cell Assay |
Cellular assays for Lirinidine utilize melanoma cells such as A375 to assess antiproliferative activity. Cells are treated with the compound at various concentrations, and cell proliferation is measured using standard viability assays (e.g., MTT, CCK-8). Melanogenesis inhibition is assessed in melanoma cells by measuring melanin content and tyrosinase activity. Platelet aggregation assays are performed using platelet-rich plasma from human or animal blood, with aggregation induced by collagen, arachidonic acid, or platelet-activating factor.
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| Animal Protocol |
In vivo animal models for Lirinidine include standard models for evaluating hypotensive and spasmolytic activity. For hypotensive effects, spontaneously hypertensive rats or normotensive animals are used. The compound is administered intravenously or orally, and blood pressure is measured. For spasmolytic effects, smooth muscle contraction assays in isolated tissue preparations (e.g., ileum, trachea) are used. Detailed protocols are not extensively reported in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Lirinidine include a molecular weight of 281.35 g/mol and molecular formula C18H19NO2. CAS number is 54383-28-7. The compound is soluble in DMSO at 55 mg/mL (195.49 mM). Purity is 98.76%. Storage conditions: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Detailed PK parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Lirinidine has an LD50 of 9.8 mg/kg (i.v.) and 21.3 mg/kg (s.c.) in mice. Detailed toxicological data are not extensively reported. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is supplied for research use only. Given its alpha-2 adrenergic receptor agonist activity, potential cardiovascular effects would be a key safety consideration.
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| References | |
| Additional Infomation |
Lirinidine has reportedly been found in magnolias (Magnolia officinalis), Neostenanthera gabonensis, and other organisms with available data.
Lirinidine is also known as (+)-Lirinidine and 北美鹅掌楸尼定碱 in Chinese. It has CAS number 54383-28-7. It is a tertiary aporphine alkaloid isolated from Liriodendron tulipifera leaves. It exhibits antioxidative activity, inhibits melanoma cell proliferation, and shows potent inhibition of melanogenesis. It also inhibits platelet aggregation induced by collagen, arachidonic acid, and platelet-activating factor. It is a selective alpha-2 adrenergic receptor agonist with hypotensive and spasmolytic actions. Purity is 98.76%. |
| Molecular Formula |
C18H19NO2
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| Molecular Weight |
281.34896
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| Exact Mass |
281.142
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| CAS # |
54383-28-7
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| PubChem CID |
31069
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| Appearance |
White to off-white solid powder
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| Density |
1.216g/cm3
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| Boiling Point |
451.4ºC at 760 mmHg
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| Flash Point |
226.8ºC
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| Index of Refraction |
1.633
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| LogP |
3.09
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
387
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1CCC2=CC(=C(C3=C2[C@@H]1CC4=CC=CC=C43)O)OC
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| InChi Key |
YXVXMURDCBMPRH-AWEZNQCLSA-N
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| InChi Code |
InChI=1S/C18H19NO2/c1-19-8-7-12-10-15(21-2)18(20)17-13-6-4-3-5-11(13)9-14(19)16(12)17/h3-6,10,14,20H,7-9H2,1-2H3/t14-/m0/s1
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| Chemical Name |
(6aS)-2-methoxy-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinolin-1-ol
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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
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| 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.
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