Encenicline hydrochloride
Based on 5 publication(s) in Google Scholar
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.
- Purity: 98.04%
- CAS No.: 550999-74-1
- Formula: C16H18Cl2N2OS
- Molecular Weight:357.30
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Membrane Transporter/Ion Channel Compound Library
HY-L011
-
Neuronal Signaling Compound Library
HY-L013
-
Neurotransmitter Receptor Compound Library
HY-L062
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Ion Channel Compound Library
HY-L166
-
MCE Bioactive Compound Library
HY-L001V
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) Encenicline hydrochloride
More
Customer Validation & Images
-
Cell Proliferation/Viability Assay
Biological Activity
α7 nAChR[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 550999-74-1
-
Appearance Solid
-
Molecular Weight 357.30
-
Formula C16H18Cl2N2OS
-
Color White to off-white
-
SMILES
O=C(C1=CC2=C(C(Cl)=CC=C2)S1)N[C@H]3CN4CCC3CC4.[H]Cl
-
Synonyms
EVP-6124 hydrochloride
-
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)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Neuron
Septal Cholinergic Neuromodulation Tunes the Astrocyte-Dependent Gating of Hippocampal NMDA Receptors to Wakefulness. [Abstract]2017 May 17;94(4):840-854.e7. PMID: 28479102 -
Eur J Pharmacol
Pharmacological characterization of a novel potent, selective, and orally active phosphodiesterase 2A inhibitor, PDM-631. [Abstract]2017 Sep 15:811:110-116. PMID: 28587776
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.
-
Psychopharmacology
Selective adrenergic alpha2C receptor antagonist ameliorates acute phencyclidine-induced schizophrenia-like social interaction deficits in rats. [Abstract]2019 Apr;236(4):1245-1253. PMID: 30535904 -
-
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (284 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Prickaerts J, et al. EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylcholine receptors. Neuropharmacology. 2012 Feb;62(2):109 [Content Brief]
[3]. Papouin T, et al. Septal Cholinergic Neuromodulation Tunes the Astrocyte-Dependent Gating of Hippocampal NMDA Receptors to Wakefulness. Neuron. 2017 May 17;94(4):840-854.e7. [Content Brief]
[4]. Maehara S, et al. Pharmacological characterization of a novel potent, selective, and orally active phosphodiesterase 2A inhibitor, PDM-631. Eur J Pharmacol. 2017 Sep 15;811:110-116. [Content Brief]
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 |
Encenicline hydrochloride Related Classifications
HY-15430A Related Classifications
Powered by Bioz