2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. nAChR 5-HT Receptor
  4. A-582941 dihydrochloride

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.

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A-582941 dihydrochloride Chemical Structure

A-582941 dihydrochloride Chemical Structure

CAS No. : 848591-90-2

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Based on 1 publication(s) in Google Scholar

A-582941 dihydrochloride Related Antibodies

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Description

A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research[1][2].

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)

In Vitro

A-582941 (0.1-100 μM) protects against cell death induced by NGF withdrawal in PC12 cells[2].
A-582941 (100 nM) increases the number of inhibitory postsynaptic potentials (IPSCs) by 260±70%, the sum of amplitudes by 220±30%, and the sum of areas by 210±40%[2].
A-582941 increases ERK1/2 phosphorylation with an EC50 of 95 nM in PC12 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

A-582941 dihydrochloride Related Antibodies
In Vivo

A-582941 (3 μM/kg, i.p. once daily for 3 d) induces a moderate increase in ACh release in the medial prefrontal cortex (mPFCx) of freely moving rats[2].
A-582941 (0.01-1.00 μM/kg, i.p.) produces a dose-dependent increase in ERK1/2 phosphorylation in the cingulate cortex and hippocampus, and increases cAMP response element-binding protein (CREB) phosphorylation in the cingulate cortex in mice[2].
A-582941 (0.1-1.0 μM/kg, i.p.) evokes dose-dependent increases in Ser-9 GSK-3β phosphorylation in the mouse cingulate cortex[2].
A-582941 shows high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and Cmax (mouse 18, rat 114, dog 79, monkey 39 ng/mL) following oral administration (mouse 1.0, rat 6.2, dog 3.0, monkey 3.0 μM/kg)[2].
A-582941 shows terminal elimination half-lives (mouse 1.4, rat 1.5, dog 1.4, monkey 2.0 h), plasma clearance (mouse 7.9, rat 4.7, dog 5.3, monkey 1.6 L/h/kg) and volumes of distribution (mouse 11.4, rat 9.2, dog 7.9, monkey 3.9 L/kg) following intravenous administration (mouse 1.0, rat 6.2, dog 0.5, monkey 0.5 μM/kg)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley CD rats (250-275 g)[2]
Dosage: 3 μM/kg
Administration: I.p. once daily for 3 days
Result: Increased the releases of Ach.
The effect remained stable after the second and third administration.
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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.78%

COA (246 KB) HNMR (259 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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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A-582941 dihydrochloride Related Classifications

Help & FAQs
  • 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.

Keywords:

A-582941848591-90-2A582941A 582941nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptorpartialα75-HT3cognitivedeficitsneurodegenerativepsychiatricInhibitorinhibitorinhibit

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