2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Anti-infection Apoptosis NF-κB Metabolic Enzyme/Protease
  3. Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial
  4. Conessine

Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy.

For research use only. We do not sell to patients.

Conessine Chemical Structure

Conessine Chemical Structure

CAS No. : 546-06-5

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Based on 1 publication(s) in Google Scholar

Other Forms of Conessine:

Conessine Related Antibodies

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FOXO1 FOXO3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy[1][2][3][4][5].

In Vitro

Conessine (2.5-20 μM; 24 h) inhibits p53-, NF-κB-, and FoxO3a-dependent transcription in HEK293 cells[1].
Conessine (10 μM) reduces the levels of MuRF1 and atrogin-1 in Dexamethasone (HY-14648)-treated C2C12 myotube cells[1].
Conessine (72 h) has antimalarial activity, with IC50 values of 1.9 and 1.3 μg/mL in the schizont maturation method and pLDH assay, respectively[2].
Conessine (74 h) is cytotoxic to L-6 cells, with an IC50 of 14 μg/mL[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Conessine Related Antibodies
In Vivo

Conessine (10-50 mg/kg; oral administration; 4 days) significantly reduces parasitaemia in mice infected with P. berghei[2].
Conessine (0.1-10 mg/kg; subcutaneously; single dose) can exacerbate ethanol-induced psychostimulant effects in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice aged 4-6 weeks old (22-26 g) were infected with Plasmodium berghei[2]
Dosage: 10, 20 and 50 mg/kg
Administration: Oral administration; 4 days
Result: Significantly reduced parasitaemia in infected mice. The parasite inhibition rates were 88.95% at 10 mg/kg, 56.6% at 20 mg/kg, and 50.99% at 50 mg/kg on day 7. The mean survival time of mice in the 10 mg/kg group was 13.3 days, in the 20 mg/kg group was 11.6 days, and in the 50 mg/kg group was 11.5 days.
Affected the liver and kidney function of mice, as shown by the changes in the levels of alkaline phosphatase (ALP), bilirubin, urea, and creatinine in serum.
Animal Model: Male Swiss mice (30-35 g) treated ethanol[3]
Dosage: 0.1, 1 and 10 mg/kg
Administration: Subcutaneously; single dose
Result: Exacerbated ethanol effects on locomotor activity in a dose-dependent manner.
Had reinforcing proprieties per se in the conditionedplace preference (CPP) procedure at dose of 10 mg/kg, but it did not alter the acquisition of ethanol CPP.
Blocked ethanol effects on dopaminergic and noradrenergic neurotransmission.
Molecular Weight

356.59

Formula

C24H40N2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1[C@]2([H])[C@]3(CN1C)[C@](CC2)([H])[C@@]4([H])[C@]([C@@]5(C(C[C@H](CC5)N(C)C)=CC4)C)([H])CC3
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

Ethanol : 25 mg/mL (70.11 mM; Need ultrasonic)

DMSO : 3.33 mg/mL (9.34 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.87%

SDS (393 KB)

COA (252 KB) HNMR (249 KB) RP-HPLC (198 KB) LCMS (77 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.8043 mL 14.0217 mL 28.0434 mL 70.1085 mL
5 mM 0.5609 mL 2.8043 mL 5.6087 mL 14.0217 mL
Ethanol 10 mM 0.2804 mL 1.4022 mL 2.8043 mL 7.0109 mL
15 mM 0.1870 mL 0.9348 mL 1.8696 mL 4.6739 mL
20 mM 0.1402 mL 0.7011 mL 1.4022 mL 3.5054 mL
25 mM 0.1122 mL 0.5609 mL 1.1217 mL 2.8043 mL
30 mM 0.0935 mL 0.4674 mL 0.9348 mL 2.3370 mL
40 mM 0.0701 mL 0.3505 mL 0.7011 mL 1.7527 mL
50 mM 0.0561 mL 0.2804 mL 0.5609 mL 1.4022 mL
60 mM 0.0467 mL 0.2337 mL 0.4674 mL 1.1685 mL
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Conessine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Conessine546-06-5Histamine ReceptorParasiteMDM-2/p53NF-κBFOXOBacterialNuclear factor-κBNuclear factor-kappaBForkhead box Ohistamine H3 receptormalarialinfectionparasitaemia model HEK293 cellsC2C12 myotube cellsL-6 cellsInhibitorinhibitorinhibit

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