A-582941 dihydrochloride

Name: A-582941 dihydrochloride
Brand: MedChemExpress
SKU: HY-59201A
Rating: 4.5 (1 reviews)

Cat. No.: HY-59201A Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

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A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with K_is 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 K_i of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.

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

A-582941 dihydrochloride Chemical Structure

CAS No. : 848591-90-2

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5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 440	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

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)

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.

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 C_max (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.

848591-90-2

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
10 mM	0.2831 mL	1.4153 mL	2.8305 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.78%

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Data Sheet (274 KB) SDS (251 KB)

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

Handling Instructions (2659 KB)

References

[1]. Anderson DJ, et, al. [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain. J Pharmacol Exp Ther. 2008 Jan; 324(1): 179-87. [Content Brief]

[2]. 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. Spring 2008; 14(1): 65-82. [Content Brief]

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