Cat. No.: HY-59201A

A-582941 dihydrochloride

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A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with K_i values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a K_i of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia.

For research use only. We do not sell to patients.

Purity: 99.78%
CAS No.: 848591-90-2
Formula: C₁₇H₂₂Cl₂N₄
Molecular Weight:353.29

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

A-582941 dihydrochloride Chemical Structure

CAS No.: 848591-90-2

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

α7 nAChR

10.8 nM (Ki, for rat α7 receptors)

α7 nAChR

16.7 nM (Ki, for human α7 receptors)

5-HT₃ Receptor

150 nM (Ki)

All ERK Isoforms :

All Epigenetic Reader Domain Isoforms :

All 5-HT Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	>100 μM Compound: 32	Agonist activity at human recombinant alpha4beta2 nicotinic acetylcholine receptor expressed in HEK293 cells assessed as changes in intracellular calcium level by FLIPR Agonist activity at human recombinant alpha4beta2 nicotinic acetylcholine receptor expressed in HEK293 cells assessed as changes in intracellular calcium level by FLIPR	[PMID: 19552432]
Oocyte	EC₅₀	4.26 μM Compound: 32	Agonist activity at human recombinant alpha7 nicotinic acetylcholine receptor expressed in xenopus laevis oocytes by parallel oocyte electrophysiological assay Agonist activity at human recombinant alpha7 nicotinic acetylcholine receptor expressed in xenopus laevis oocytes by parallel oocyte electrophysiological assay	[PMID: 19552432]

Chemical Information

CAS No. 848591-90-2
Appearance Solid
Molecular Weight 353.29
Formula C₁₇H₂₂Cl₂N₄
Color Light yellow to yellow
SMILES

CN1CC(CN(C2=NN=C(C3=CC=CC=C3)C=C2)C4)C4C1.[H]Cl.[H]Cl
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)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (283.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8305 mL

14.1527 mL

28.3054 mL

5 mM

0.5661 mL

2.8305 mL

5.6611 mL

10 mM

0.2831 mL

1.4153 mL

2.8305 mL

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.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tietje KR, et al. Preclinical characterization of A-582941: a novel alpha7 neuronal nicotinic receptor agonist with broad spectrum cognition-enhancing properties. CNS Neurosci Ther. 2008;14(1):65-82. [Content Brief]

[2]. Thomsen MS, et al. The selective alpha7 nicotinic acetylcholine receptor agonist A-582941 activates immediate early genes in limbic regions of the forebrain: Differential effects in the juvenile and adult rat. Neuroscience. 2008;154(2):741-753. [Content Brief]

[3]. Buccafusco JJ, et al. Profile of nicotinic acetylcholine receptor agonists ABT-594 and A-582941, with differential subtype selectivity, on delayed matching accuracy by young monkeys. Biochem Pharmacol. 2007;74(8):1202-1211. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8305 mL	14.1527 mL	28.3054 mL	70.7634 mL
	5 mM	0.5661 mL	2.8305 mL	5.6611 mL	14.1527 mL
	10 mM	0.2831 mL	1.4153 mL	2.8305 mL	7.0763 mL
	15 mM	0.1887 mL	0.9435 mL	1.8870 mL	4.7176 mL
	20 mM	0.1415 mL	0.7076 mL	1.4153 mL	3.5382 mL
	25 mM	0.1132 mL	0.5661 mL	1.1322 mL	2.8305 mL
	30 mM	0.0944 mL	0.4718 mL	0.9435 mL	2.3588 mL
	40 mM	0.0708 mL	0.3538 mL	0.7076 mL	1.7691 mL
	50 mM	0.0566 mL	0.2831 mL	0.5661 mL	1.4153 mL
	60 mM	0.0472 mL	0.2359 mL	0.4718 mL	1.1794 mL
	80 mM	0.0354 mL	0.1769 mL	0.3538 mL	0.8845 mL
	100 mM	0.0283 mL	0.1415 mL	0.2831 mL	0.7076 mL

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A-582941 dihydrochloride

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All ERK Isoforms

All Epigenetic Reader Domain Isoforms

All 5-HT Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

A-582941 dihydrochloride Related Classifications

HY-59201A Related Classifications