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EVP-6124 hydrochlorideAlpha7 nAChR agonist

EVP-6124 hydrochloride

Catalog No. A3407
Size Price Stock Qty
10mM (in 1mL DMSO) $330.00 In stock
5mg $287.00 In stock
10mg $369.00 In stock
50mg $997.00 In stock
200mg $2,262.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

EVP-6124 hydrochloride

Biological Activity

Description Ercalcidiol is a metabolite of vitamin D2.
Targets            
IC50            

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Chemical Properties

Cas No. 550999-74-1 SDF Download SDF
Synonyms EVP 6124 hydrochloride;EVP6124 hydrochloride
Chemical Name N-[(3R)-1-azabicyclo[2.2.2]octan-3-yl]-7-chloro-1-benzothiophene-2-carboxamide;hydrochloride
Canonical SMILES C1CN2CCC1C(C2)NC(=O)C3=CC4=C(S3)C(=CC=C4)Cl.Cl
Formula C16H18Cl2N2OS M.Wt 357.3
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

EVP-6124 Hydrochloride is a hydrochloride form of EVP-6124. EVP-6124 is partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs) that was proved high-affinity in vitro and in vivo. [1]
EVP-6124 was proved to show selectivity for α7 but low-affinity of α4β2 nAChRs in some binding and functional experiments. EVP-6124 had good brain penetration and an adequate exposure time. [1,2]
Co-administration of EVP-6124 and the selective nAChRs antagonist could contribute to the release of DA, ACH, and Glu. This could be used to treat cognitive impairment and possibly other dimensions of psychopathology. Co-administration of donepezil at 0.1 mg/kg, p.o. and EVP-6124 at 0.03 mg/kg proved to be fully restored memory while each of these did not improve memory in this task. [1] Pretreatment with the selective α7 nAChR antagonist, methyllycaconitine (MLA, 1.0 mg/kg), significantly blocked cortical DA and Glu efflux induced by EVP-6124 (0.1 mg/kg). [2,3]
References:
1. Jos Prickaerts, Nick P. van Goethem, 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, 2012,62 (2): 1099-1110.
2. Mei Huang, Anna R. Felix, et al. Chaya Bhuvaneswaran, Dana Hilt, Gerhard K?nig, Herbert Y. Meltzer, The alpha-7 receptor agonist EVP-6124 increases dopamine and glutamate efflux in rat medial prefrontal cortex and nucleus accumbens. Biochemical Pharmacology, 2011, 82 (8): 1040.
3. Mei Huang, Anna R. Felix, et al. The novel α7 nicotinic acetylcholine receptor agonist EVP-6124 enhances dopamine, acetylcholine, and glutamate efflux in rat cortex and nucleus accumbens. Psychopharmacology, 2014, 231:4541-4551.