2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Encenicline hydrochloride

Encenicline hydrochloride  (Synonyms: EVP-6124 hydrochloride)

Cat. No.: HY-15430A Purity: 98.77%
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Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

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

Encenicline hydrochloride Chemical Structure

Encenicline hydrochloride Chemical Structure

CAS No. : 550999-74-1

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10 mM * 1 mL in DMSO
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Based on 6 publication(s) in Google Scholar

Other Forms of Encenicline hydrochloride:

Encenicline hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Encenicline hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2017 Sep 15;811:110-116.  [Abstract]

    Effects of EVP-6124 on the novel object recognition test in rats. EVP-6124 (0.3-1 mg/kg) is orally administered 1 h before the acquisition trial.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

    IC50 & Target

    α7 nAChR[1]
    In Vitro

    Encenicline (EVP-6124) displaces [3H]-MLA (Methyllycaconitine) (Ki=9.98 nM, pIC50=7.65±0.06, n=3) and [125I]-α-bungarotoxin (Ki=4.33 nM, pIC50=8.07±0.04, n=3). Encenicline (EVP-6124) is approximately 300 fold more potent than the natural agonist ACh (Ki=3 μM), measured in binding assays using [3H]-MLA. Encenicline hydrochloride inhibits the 5-HT3 receptor by 51% at 10 nM, the lowest concentration tested. Evaluation of the human 5-HT2B receptor expressed in CHO cells demonstrates displacement of [3H]-mesulergine (Ki=14 nM) and only antagonist activity in the rat gastric fundus assay at an IC50 of 16 μM. In binding and functional experiments, Encenicline (EVP-6124) shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs[1].

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

    Encenicline hydrochloride Related Antibodies
    In Vivo

    Encenicline hydrochloride has good brain penetration and an adequate exposure time. Encenicline hydrochloride (0.3 mg/kg, p.o.) significantly restores memory function in scopolamine-treated rats (0.1 mg/kg, i.p.) in an object recognition task (ORT). Although donepezil at 0.1 mg/kg, p.o. or Encenicline hydrochloride at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory. In a natural forgetting test, an ORT with a 24 h retention time, Encenicline hydrochloride improved memory at 0.3 mg/kg, p.o. This improvement is blocked by the selective α7 nAChR antagonist methyllycaconitine (0.3 mg/kg, i.p. or 10 μg, i.c.v.). Encenicline hydrochloride is found to bind moderately to rat plasma proteins with a mean fu of 0.11±0.01 (mean±SD) or 11%. Over a range of 0.1-30 mg/kg, p.o., Encenicline hydrochloride demonstrates proportional dose escalation. Tmax is at 4 h in plasma and 2 h brain, although the brain concentrations remained similar between 2 and 8 h. The B:P ratios are 1.7-5.1 between 1 and 8 h[1]. Pharmacokinetic studies have shown that Encenicline hydrochloride (0.4 mg/kg, i.p.) reaches peak brain concentration 2 hr after administration and remains at effective concentrations for at least 4 hr. Encenicline hydrochloride is administered to WT mice at ZT0 (0.4 mg/kg i.p single dose) and significantly increases the saturation index of NMDARs in slices obtained 4 hr later without causing prolonged wakefulness or enhanced locomotor activity [2].

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

    357.30

    Formula

    C16H18Cl2N2OS
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC2=C(C(Cl)=CC=C2)S1)N[C@H]3CN4CCC3CC4.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (139.94 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7988 mL 13.9938 mL 27.9877 mL
    5 mM 0.5598 mL 2.7988 mL 5.5975 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

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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

    Concentration (start)

    C1

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    Volume (start)

    V1

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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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.00 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 DMSO 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.00 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 DMSO 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)

    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
    References
    Animal Administration
    [1][2]

    Rats[1]
    Twenty-four 2.5-month-old male Wistar rats (average body weight: 329 g) are used. Before testing EVP-6124, the effects of scopolamine alone at 0.03, 0.1, or 0.3 mg/kg, i.p. in the ORT are determined (n=8 per treatment). Scopolamine (0.1 mg/kg, i.p.) injected 30 min before T1 resulted in a robust deficit at T2 when a 1 h interval is used. The d2 index is not significantly different from the chance level of performance; and there are no changes in exploratory behavior for 0.1 mg/kg, i.p. of scopolamine compared with saline. Subsequently, the ability of Encenicline (EVP-6124) to reverse the memory impairment induced by 0.1 mg/kg of scopolamine is tested. First, scopolamine and then Encenicline (EVP-6124) (0.03, 0.1, 0.3, and 1.0 mg/kg, p.o.) are administered 30 min before T1. For the control treatments, animals received either deionized water (p.o.) plus saline (i.p.) or deionized water (p.o.) plus 0.1 mg/kg scopolamine (i.p.).
    Mice[2]
    Adult male mice (3-6 months old) are used throughout this study. Encenicline (EVP-6124) is injected i.p. (0.4 mg/kg) at Zeitgeber time (ZT0) in awake mice (9 mice total for this experiment), in the animal facility. Mice are then immediately returned to their home cage with their siblings and left undisturbed for 4 hr (ZT4). During this time, they are closely monitored to check for possible behavioral effects of Encenicline (EVP-6124) injection. All of the 9 injected mice nested and are immobile in the hour following the injection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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). 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 1 mM 2.7988 mL 13.9938 mL 27.9877 mL 69.9692 mL
    5 mM 0.5598 mL 2.7988 mL 5.5975 mL 13.9938 mL
    10 mM 0.2799 mL 1.3994 mL 2.7988 mL 6.9969 mL
    15 mM 0.1866 mL 0.9329 mL 1.8658 mL 4.6646 mL
    20 mM 0.1399 mL 0.6997 mL 1.3994 mL 3.4985 mL
    25 mM 0.1120 mL 0.5598 mL 1.1195 mL 2.7988 mL
    30 mM 0.0933 mL 0.4665 mL 0.9329 mL 2.3323 mL
    40 mM 0.0700 mL 0.3498 mL 0.6997 mL 1.7492 mL
    50 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3994 mL
    60 mM 0.0466 mL 0.2332 mL 0.4665 mL 1.1662 mL
    80 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8746 mL
    100 mM 0.0280 mL 0.1399 mL 0.2799 mL 0.6997 mL
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    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:

    Encenicline550999-74-1EVP-6124EVP6124EVP 6124nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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