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

Encenicline hydrochloride (Synonyms: EVP-6124 hydrochloride)

Cat. No.: HY-15430A Purity: 98.82%
Handling Instructions

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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 377 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 377 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 343 In-stock
Estimated Time of Arrival: December 31
10 mg USD 443 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1195 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2154 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Encenicline hydrochloride:

Top Publications Citing Use of Products

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

    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].

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

    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].

    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.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (139.94 mM)

    *"≥" 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
    10 mM 0.2799 mL 1.3994 mL 2.7988 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.00 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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
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    Keywords:

    EnceniclineEVP-6124EVP6124EVP 6124nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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