| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
5-HT2 Receptor
Uncarine E primarily targets M1 muscarinic acetylcholine receptors and 5-HT2 receptors, where it acts as a positive regulator. This modulation of cholinergic and serotonergic signaling underlies its effects on the nervous system and smooth muscle contraction. As a PXR activator, it can influence the expression of genes involved in drug metabolism and transport. Its antimicrobial activity and immune-stimulating properties suggest additional targets related to pathogen defense and immune cell function. The compound's diverse pharmacological profile makes it a valuable tool for studying receptor pharmacology and immunomodulation. |
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| ln Vitro |
In vitro, Uncarine E has demonstrated antimicrobial activity against various pathogens. It stimulates the immune system, indicating effects on immune cell function. As a positive regulator of M1 muscarinic and 5-HT2 receptors, it modulates receptor-mediated signaling in cell-based assays. Its activity as a PXR activator has been characterized in cell-based reporter gene assays. The compound induces contraction of rat myometrium in vitro, demonstrating its effects on smooth muscle. These activities confirm its potential as a modulator of neurotransmission, immune response, and muscle contraction.
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| ln Vivo |
In vivo, Uncarine E has been studied for its effects on the immune system and smooth muscle contraction. Its PXR activation suggests potential for modulating drug metabolism and transport in animal models. The compound's antimicrobial activity indicates potential for studying infectious disease models. However, detailed in vivo efficacy and safety data are limited. As a natural product from Uncaria tomentosa, which is used traditionally for various conditions, Uncarine E may contribute to the overall pharmacological effects of the plant. Further research is needed to fully characterize its in vivo biological activity and therapeutic potential.
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| Enzyme Assay |
For in vitro receptor binding assays (cell-free), Uncarine E is evaluated for its affinity and activity at M1 muscarinic and 5-HT2 receptors. Radioligand binding assays are performed using membrane preparations from cells expressing these receptors. Competitive binding experiments with specific radiolabeled ligands allow determination of binding affinity (Ki or Kd). Functional assays, such as GTPγS binding or second messenger measurements, can assess receptor activation or modulation. PXR activation can be measured using cell-free transcription assays with purified receptor and response elements. These cell-free systems help characterize the compound's direct molecular interactions and receptor modulation profile.
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| Cell Assay |
In vitro cellular assays for Uncarine E are performed using cells expressing M1 muscarinic and 5-HT2 receptors. Cells are cultured in appropriate media and treated with the compound at various concentrations. Receptor activation is assessed by measuring downstream signaling events such as calcium mobilization, MAPK activation, or inositol phosphate production. Immune cell function is assessed by measuring cytokine production, proliferation, or activation markers. Antimicrobial activity is tested against bacterial or fungal cultures by measuring growth inhibition. PXR activation is assessed using reporter gene assays in cells transfected with PXR and a reporter construct. These cellular assays help validate the compound's receptor modulation and immune-stimulating activities.
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| Animal Protocol |
In vivo animal experiments with Uncarine E are not extensively documented. As a compound from Uncaria tomentosa, it may be studied in models relevant to the plant's traditional uses, such as inflammation, infection, or neurological conditions. Uncarine E could be administered via oral gavage, intraperitoneal injection, or intravenous injection. Efficacy endpoints would depend on the specific disease model and could include inflammation markers, pathogen load, or behavioral changes. The compound's PXR activation could be studied by measuring the expression of CYP450 enzymes and drug transporters in tissues. Researchers should consult the primary literature for any available in vivo protocols and data.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Uncarine E are not extensively documented. As an alkaloid with a molecular weight of 368.43 and a logP of 2.138, it is expected to have moderate oral bioavailability and good tissue distribution. The compound is soluble in DMSO (50 mg/mL). For in vivo studies, it can be formulated in suitable vehicles. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are not available in the literature. The compound should be stored as a powder at -20°C for up to three years and in solution at -80°C for up to six months. It requires protection from light during transportation and storage.
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| Toxicity/Toxicokinetics |
The toxicological profile of Uncarine E is not extensively characterized. As a natural alkaloid from Uncaria tomentosa, it is generally considered to have a moderate safety profile, but comprehensive toxicity studies are limited. The compound is intended for research use only and not for human therapeutic applications. Its effects at high concentrations and potential interactions with other drugs or compounds have not been fully investigated. Researchers should follow standard laboratory safety practices when handling Uncarine E. As with all research compounds, appropriate safety assessments should be conducted for specific experimental applications.
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| References | |
| Additional Infomation |
Uncariae E belongs to the indoleazine class of compounds. Uncariae has been reported in Uncaria sinensis, Uncaria rhynchophylla, and other organisms with available data. See also: Uncaria rhynchophylla (partial).
Uncarine E is a valuable research tool for studying muscarinic and serotonergic receptor pharmacology, particularly as a positive modulator of M1 and 5-HT2 receptors. It is used to investigate the role of these receptors in neurological function, smooth muscle contraction, and immune regulation. Its PXR activating properties make it relevant for studies on drug metabolism and transport. The compound's antimicrobial and immune-stimulating activities provide opportunities for research into infectious diseases and immunomodulation. As a natural product from Uncaria tomentosa, it is also relevant for ethnopharmacology and natural product chemistry research. |
| Molecular Formula |
C21H24N2O4
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|---|---|
| Molecular Weight |
368.43
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| Exact Mass |
368.174
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| CAS # |
5171-37-9
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| PubChem CID |
9885603
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| Appearance |
White to off-white solid
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| Density |
1.33g/cm3
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| Boiling Point |
555.2ºC at 760 mmHg
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| Melting Point |
209-211 °C
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| Flash Point |
289.6ºC
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| Index of Refraction |
1.635
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| LogP |
2.138
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
692
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC1C2CN3CCC4(C3CC2C(=CO1)C(=O)OC)C5=CC=CC=C5NC4=O
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| InChi Key |
JMIAZDVHNCCPDM-PFDNRQJHSA-N
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| InChi Code |
InChI=1S/C21H24N2O4/c1-12-14-10-23-8-7-21(16-5-3-4-6-17(16)22-20(21)25)18(23)9-13(14)15(11-27-12)19(24)26-2/h3-6,11-14,18H,7-10H2,1-2H3,(H,22,25)/t12-,13-,14-,18-,21-/m0/s1
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| Chemical Name |
methyl (1S,4aS,5aS,6S,10aS)-1-methyl-2'-oxospiro[1,4a,5,5a,7,8,10,10a-octahydropyrano[3,4-f]indolizine-6,3'-1H-indole]-4-carboxylate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~50 mg/mL (~135.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 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 25.0 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: ≥ 2.5 mg/mL (6.79 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 25.0 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 | 2.7142 mL | 13.5711 mL | 27.1422 mL | |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 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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