| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Imperialine targets the M2 muscarinic receptor. It acts as a short-acting selective M2 muscarinic receptor antagonist. By blocking M2 receptors, Imperialine modulates cholinergic neurotransmission, which is believed to underlie its antitussive and expectorant effects. The compound's selectivity for the M2 subtype makes it a valuable tool for studying muscarinic receptor pharmacology.
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| ln Vitro |
In vitro, Imperialine acts as a selective M2 muscarinic receptor antagonist. Its activity is typically assessed in receptor binding assays measuring affinity for M2 and other muscarinic receptor subtypes. The compound's selectivity for M2 over other subtypes (M1, M3, M4, M5) can be determined by competitive binding studies using radiolabeled antagonists.
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| ln Vivo |
No specific in vivo activity data is publicly available for Imperialine beyond its use as an antitussive and expectorant agent. As a natural product-derived alkaloid, its in vivo efficacy has not been extensively characterized in the available literature. Further studies would be needed to establish its in vivo activity and potential therapeutic applications.
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| Enzyme Assay |
In cell-free receptor binding assays, Imperialine's activity is evaluated by measuring its affinity for M2 muscarinic receptors. Membrane preparations from cells expressing the M2 receptor are incubated with a radiolabeled antagonist (e.g., [3H]N-methylscopolamine) and varying concentrations of Imperialine. The displacement of the radioligand is measured, and the Ki is calculated from the competition curve.
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| Cell Assay |
In vitro cell-based experiments with Imperialine typically involve cell lines expressing muscarinic receptor subtypes, such as CHO cells transfected with M2 receptors. Cells are treated with the compound in the presence of a muscarinic agonist (e.g., carbachol), and the inhibition of agonist-induced intracellular calcium mobilization or cAMP modulation is measured. The IC50 for antagonism is determined from concentration-response curves.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for Imperialine. If in vivo studies were to be conducted, typical protocols might involve animal models of cough or airway disease, where the compound would be administered, and antitussive or expectorant effects would be measured.
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| ADME/Pharmacokinetics |
No pharmacokinetic data is publicly available for Imperialine. As a natural product alkaloid, its absorption, distribution, metabolism, and excretion (ADME) properties have not been characterized. The compound has a molecular formula of C27H43NO3 and a molecular weight of 429.64.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for Imperialine. As a natural product, its safety profile has not been well established. The compound is for research use only and is not intended for human therapeutic applications.
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| References | |
| Additional Infomation |
Sipeimine is an alkaloid. It has been reported to be found in Fritillaria thunbergii, Fritillaria var. ...
Imperialine has a molecular formula of C27H43NO3 and a molecular weight of 429.64. It is also known as Sipeimine or Kashmirine. The compound is an isosteroidal alkaloid from Fritillaria species and a short-acting selective M2 muscarinic receptor antagonist. It has been used as an antitussive and expectorant agent. It is available for research purposes only. |
| Molecular Formula |
C27H43NO3
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|---|---|
| Molecular Weight |
429.64
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| Exact Mass |
429.324
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| CAS # |
61825-98-7
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| PubChem CID |
442977
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
567.1±50.0 °C at 760 mmHg
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| Flash Point |
296.8±30.1 °C
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| Vapour Pressure |
0.0±3.5 mmHg at 25°C
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| Index of Refraction |
1.585
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
31
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| Complexity |
755
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H]1CC[C@H]2[C@@]([C@@H]3CC[C@@H]4[C@H]([C@@H]3CN2C1)C[C@H]5[C@H]4CC(=O)[C@@H]6[C@@]5(CC[C@@H](C6)O)C)(C)O
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| InChi Key |
IQDIERHFZVCNRZ-LRCDAWNTSA-N
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| InChi Code |
InChI=1S/C27H43NO3/c1-15-4-7-25-27(3,31)21-6-5-17-18(20(21)14-28(25)13-15)11-22-19(17)12-24(30)23-10-16(29)8-9-26(22,23)2/h15-23,25,29,31H,4-14H2,1-3H3/t15-,16-,17+,18+,19-,20-,21+,22-,23+,25-,26+,27-/m0/s1
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| Chemical Name |
(1R,2S,6S,9S,10S,11R,14S,15S,18S,20S,23R,24S)-10,20-dihydroxy-6,10,23-trimethyl-4-azahexacyclo[12.11.0.02,11.04,9.015,24.018,23]pentacosan-17-one
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| Synonyms |
Sipeimine; Kashmirine
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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 |
| 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 : ~8.33 mg/mL (~19.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (1.79 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 7.7 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: ≥ 0.77 mg/mL (1.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 7.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.77 mg/mL (1.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3275 mL | 11.6377 mL | 23.2753 mL | |
| 5 mM | 0.4655 mL | 2.3275 mL | 4.6551 mL | |
| 10 mM | 0.2328 mL | 1.1638 mL | 2.3275 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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