Encenicline
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 50mg | $800 | Check With Us |
| 100mg | $1350 | Check With Us |
| 200mg | $2025 | Check With Us |
: Cat #: V20529 CAS #: 550999-75-2 Purity ≥ 98%
Description: Encenicline (EVP-6124; MT-4666) is a novel partial agonist of α7 nicotinic acetylcholine receptor.
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| Molecular Weight (MW) | 320.84 |
|---|---|
| Molecular Formula | C16H17ClN2OS |
| CAS No. | 550999-75-2 |
| Synonyms | EVP-6124; EVP6124; EVP 6124; MT-4666; MT4666; MT 4666; Encenicline |
| Protocol | 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 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 shows selectivity for α7 nAChRs and does not activate or inhibit heteromeric α4β2 nAChRs |
|---|---|---|
| In Vivo | Encenicline (EVP-6124) has good brain penetration and an adequate exposure time. Encenicline (EVP-6124) (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 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 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 (EVP-6124) 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 (EVP-6124) 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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 3.1168 mL | 15.5841 mL | 31.1682 mL | 62.3364 mL |
| 5mM | 0.6234 mL | 3.1168 mL | 6.2336 mL | 12.4673 mL |
| 10mM | 0.3117 mL | 1.5584 mL | 3.1168 mL | 6.2336 mL |
| 20mM | 0.1558 mL | 0.7792 mL | 1.5584 mL | 3.1168 mL |
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ddH2O,mix and clarify.
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