| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary molecular target of Conessine hydrobromide is the histamine H3 receptor, where it acts as a potent and specific antagonist. By blocking H3 receptors, it increases histamine release in the CNS. Conessine also has antiparasitic activity, particularly against Leishmania and Trypanosoma species. The mechanism of antiparasitic action may involve disruption of sterol biosynthesis.
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|---|---|
| ln Vitro |
In vitro, Conessine hydrobromide is a potent and specific antagonist of histamine H3 receptors. It also shows antiparasitic activity against Leishmania and Trypanosoma. Detailed IC50 values have been reported in the context of its development as a research tool.
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| ln Vivo |
In vivo studies with Conessine hydrobromide are limited. As a histamine H3 antagonist, it may modulate histaminergic neurotransmission in the CNS. As an antiparasitic agent, it may demonstrate efficacy in animal models of leishmaniasis or trypanosomiasis. However, detailed in vivo efficacy data are limited.
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| Enzyme Assay |
For histamine H3 receptor binding assays, membranes from cells expressing recombinant H3 receptors or rat brain membranes are incubated with radiolabeled H3 receptor ligands in assay buffer containing 50 mM Tris-HCl (pH 7.4), 5 mM MgCl2, and 0.1% BSA. Serial dilutions of Conessine hydrobromide are added. Incubation is at 25°C for 60 minutes. Bound radioligand is separated by filtration and measured by scintillation counting.
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| Cell Assay |
For antiparasitic assays, Leishmania or Trypanosoma cultures are treated with serial dilutions of Conessine hydrobromide. Parasite growth is assessed by microscopy or [3H]thymidine incorporation. Cytotoxicity against mammalian cells is evaluated using the MTT assay.
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| Animal Protocol |
For in vivo studies, animal models of leishmaniasis or trypanosomiasis may be used. Conessine hydrobromide is administered by intraperitoneal or oral routes at doses determined from preliminary studies. Parasite burden in tissues is assessed. For CNS studies, histamine levels are measured by microdialysis or post-mortem HPLC.
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| References |
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| Additional Infomation |
Conessine dihydrobromide is a steroidal alkaloid.
|
| Molecular Formula |
C24H42BR2N2
|
|---|---|
| Molecular Weight |
518.4117
|
| Exact Mass |
340.215
|
| CAS # |
5913-82-6
|
| PubChem CID |
111109
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| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
450.4ºC at 760 mmHg
|
| Flash Point |
199.6ºC
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| LogP |
3.205
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
28
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| Complexity |
609
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
CN(C)[C@@H]1CC2=CC[C@H]3[C@H](CC[C@@H]4[C@@H](N(C5)C)C)[C@]45CC[C@@H]3[C@@]2(C)CC1.Br.Br
|
| InChi Key |
YYTFAPMEQOGSRL-VEOCRSHVSA-N
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| InChi Code |
InChI=1S/C24H40N2.2BrH/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;2*1H/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;dihydrobromide
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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) |
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 | 1.9290 mL | 9.6449 mL | 19.2898 mL | |
| 5 mM | 0.3858 mL | 1.9290 mL | 3.8580 mL | |
| 10 mM | 0.1929 mL | 0.9645 mL | 1.9290 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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