1. MAPK/ERK Pathway Neuronal Signaling GPCR/G Protein Membrane Transporter/Ion Channel Stem Cell/Wnt Epigenetics
  2. Epigenetic Reader Domain nAChR 5-HT Receptor ERK
  3. A-582941 dihydrochloride

A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki 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 Ki 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.

A-582941 dihydrochloride

A-582941 dihydrochloride Chemical Structure

CAS No. : 848591-90-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki 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 Ki 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[1][2][3].

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)

Molecular Weight

353.29

Formula

C17H22Cl2N4

CAS No.
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8305 mL 14.1527 mL 28.3054 mL
5 mM 0.5661 mL 2.8305 mL 5.6611 mL
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.78%

References

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 2.8305 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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
A-582941 dihydrochloride
Cat. No.:
HY-59201A
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