| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Plasmodium; H3 Receptor ( Ki = 5.4 nM ); rat H3 receptor ( Ki = 25 nM ); Guinea pig H3 Receptor ( Ki = 6.0 nM ); Dog H3 Receptor ( Ki = 5.7 nM )
Conessine targets the histamine H3 receptor, acting as a selective antagonist. It has pKi values of 7.61 and 8.27 for rat and human H3 receptors, respectively. It is also an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. |
|---|---|
| ln Vitro |
In vitro, Conessine is a potent histamine H3 receptor antagonist. It is active against a variety of Gram-positive and Gram-negative bacteria. It inhibits the multidrug efflux pump system in Pseudomonas aeruginosa.
|
| ln Vivo |
In vivo, Conessine is orally active and can cross the blood-brain barrier. It has been used in traditional medicine for its anti-inflammatory, anti-diarrheal, and anti-malarial properties. It is valuable in neurological research, particularly in studying conditions related to cognition, sleep, and appetite regulation.
|
| Enzyme Assay |
Conessine is evaluated in cell-free receptor binding assays to determine its affinity for the histamine H3 receptor. Radioligand binding displacement assays are performed using membrane preparations expressing H3 receptors. Competition binding experiments are conducted with increasing concentrations of Conessine and a fixed concentration of a labeled reference ligand. Ki values are determined.
|
| Cell Assay |
Conessine is assessed in cell-based assays to measure its antagonist activity at the H3 receptor. Cells expressing the H3 receptor are treated with Conessine, and receptor activity is measured by assessing downstream signaling pathways. Its antibacterial activity is assessed in bacterial cultures.
|
| Animal Protocol |
Conessine is administered in animal models to evaluate its effects on H3 receptor-mediated functions. It has been used in traditional medicine. Efficacy is assessed by measuring physiological parameters and behavioral changes. Its effects on cognition, sleep, and appetite are of research interest.
|
| ADME/Pharmacokinetics |
Conessine has a molecular weight of 356.59 and a molecular formula of C24H40N2. It has a CAS number of 546-06-5. The compound is a crystalline solid with a decomposition temperature of 340°C. It has a very bitter taste. It should be stored under recommended conditions.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Conessine. The compound is for research use only and is not intended for human therapeutic use. It is a potent histamine H3 receptor antagonist used to study neurological and psychiatric disorders.
|
| References |
|
| Additional Infomation |
Conessine is a steroidal alkaloid, a compound in which 5-ene is substituted at the 3-position with an N,N-dimethylamino group. It has been isolated from plants in the Apocynaceae family. Conessine possesses antibacterial, antimalarial, H3 receptor antagonistic, and phytometabolic activities. It is a steroidal alkaloid and a tertiary amine compound functionally related to Conessine. Conessine has been reported to exist in Holarrhena floribunda, Funtumia elastica, and Holarrhena pubescens, and relevant data are available.
Conessine is also known as Conessin, NSC 119994, and Wrightine. It is a natural alkaloid found in the bark of the Holarrhena antidysenterica tree. It has been used in traditional medicine. The compound is not approved for clinical use. |
| Molecular Formula |
C24H40N2
|
|---|---|
| Molecular Weight |
356.5878
|
| Exact Mass |
356.319
|
| Elemental Analysis |
C, 80.84; H, 11.31; N, 7.86
|
| CAS # |
546-06-5
|
| PubChem CID |
441082
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
450.4±45.0 °C at 760 mmHg
|
| Melting Point |
126-127ºC
|
| Flash Point |
199.6±16.5 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.564
|
| LogP |
5.71
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
26
|
| Complexity |
609
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C[C@H]1[C@H]2CC[C@H]3[C@@H]4CC=C5C[C@H](CC[C@]5(C)[C@H]4CC[C@]23CN1C)N(C)C
|
| InChi Key |
GPLGAQQQNWMVMM-MYAJQUOBSA-N
|
| InChi Code |
InChI=1S/C24H40N2/c1-16-20-8-9-22-19-7-6-17-14-18(25(3)4)10-12-23(17,2)21(19)11-13-24(20,22)15-26(16)5/h6,16,18-22H,7-15H2,1-5H3/t16-,18-,19+,20+,21-,22-,23-,24-/m0/s1
|
| Chemical Name |
(1R,2S,5S,6S,9R,12S,13R,16S)-N,N,6,7,13-pentamethyl-7-azapentacyclo[10.8.0.02,9.05,9.013,18]icos-18-en-16-amine
|
| Synonyms |
Neriine; Roquessine; Conessinum; Konessin; Wrightine; Conessine
|
| HS Tariff Code |
2934.99.03.00
|
| 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)
|
| Solubility (In Vitro) |
Ethanol: ~25 mg/mL (~70.1 mM)
|
|---|---|
| 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 | 2.8043 mL | 14.0217 mL | 28.0434 mL | |
| 5 mM | 0.5609 mL | 2.8043 mL | 5.6087 mL | |
| 10 mM | 0.2804 mL | 1.4022 mL | 2.8043 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA