EVP 6124
- Product Name
- EVP 6124
- CAS No.
- 550999-75-2
- Chemical Name
- EVP 6124
- Synonyms
- EVP-6124;EVP 6124;encenicline;EVP-6124 (Encenicline);Encenicline (EVP-6124);Encenicline, 10 mM in DMSO;(R)-7-Chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide;7-chloro-n-((1s,3r,4s)-quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide;Benzo[b]thiophene-2-carboxamide, N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-7-chloro-;inhibit,nAChR,Encenicline,EVP 6124,Nicotinic acetylcholine receptors,EVP6124,Inhibitor
- CBNumber
- CB42645140
- Molecular Formula
- C16H17ClN2OS
- Formula Weight
- 320.84
- MOL File
- 550999-75-2.mol
EVP 6124 Property
- Boiling point:
- 545.1±40.0 °C(Predicted)
- Density
- 1.38±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO
- form
- Powder
- pka
- 13.53±0.20(Predicted)
- Appearance
- white solid
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- A3406
- Product name
- 7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide
- Packaging
- 5mg
- Price
- $287
- Updated
- 2021/12/16
- Product number
- A3406
- Product name
- 7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide
- Packaging
- 10mg
- Price
- $369
- Updated
- 2021/12/16
- Product number
- A3406
- Product name
- 7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide
- Packaging
- 50mg
- Price
- $997
- Updated
- 2021/12/16
- Product number
- A3406
- Product name
- 7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide
- Packaging
- 200mg
- Price
- $2262
- Updated
- 2021/12/16
- Product number
- CM161630
- Product name
- (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide
- Purity
- 98%
- Packaging
- 100mg
- Price
- $1093
- Updated
- 2021/12/16
EVP 6124 Chemical Properties,Usage,Production
Uses
Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (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[1]. Pharmacokinetic studies have shown that Encenicline (EVP-6124) (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 (EVP-6124) 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].
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 DOI:10.1016/j.neuropharm.2011.10.024
[2] Thomas Papouin, et al. Septal Cholinergic Neuromodulation Tunes the Astrocyte-Dependent Gating of Hippocampal NMDA Receptors to Wakefulness. Neuron. 2017 May 17;94:1-15.
EVP 6124 Preparation Products And Raw materials
Raw materials
Preparation Products
EVP 6124 Suppliers
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