An agonist of α7 nAChRs
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A-582941

Item No. 42375

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
octahydro-2-methyl-5-(6-phenyl-3-pyridazinyl)-pyrrolo[3,4-c]pyrrole, dihydrochloride
CAS Number
848591-90-2
Molecular Formula
C17H20N4 • 2HCl
Formula Weight
353.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: Slightly Soluble: 0.1-1 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
CN1CC2CN(C(N=N3)=CC=C3C4=CC=CC=C4)CC2C1.Cl.Cl
InChi Code
InChI=1S/C17H20N4.2ClH/c1-20-9-14-11-21(12-15(14)10-20)17-8-7-16(18-19-17)13-5-3-2-4-6-13;;/h2-8,14-15H,9-12H2,1H3;2*1H
InChi Key
PGTCSMQEIJMZTJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $87

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    10 mg

    $157

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    50 mg

    $479

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    100 mg

    $696

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    Product Description

    A-582941 is an agonist of a7 nicotinic acetylcholine receptors (nAChRs).1 It induces inward currents in Xenopus oocytes expressing the rat or human receptor (EC50s = 2.45 and 4.26 µM, respectively), which can be reversed by methyllycaconitine (Item No. 21398). A-582941 selectively binds to a7 nAChRs (Kis = 10.8 and 16.7 nM for the rat and human receptors, respectively) over a panel of greater than 75 receptors and ion channels, including muscarinic receptors, at 10 µM but does bind to the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 154 nM). In vivo, A-582941 (12 mg/kg) improves cognitive deficits in the 3xTg transgenic mouse model of Alzheimer’s disease.2 It increases accuracy in the delayed match-to-sample (DMTS) test in rhesus monkeys when administered at a dose of 10 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bitner, R.S., Bunnelle, W.H., Anderson, D.J., et al. Broad-spectrum efficacy across cognitive domains by α7 nicotinic acetylcholine receptor agonism correlates with activation of ERK1/2 and CREB phosphorylation pathways. J. Neurosci. 10578-10587 (2007).

    2. Medeiros, R., Castello, N.A., Cheng, D., et al. α7 nicotinic receptor agonist enhances cognition in aged 3xTg-AD mice with robust plaques and tangles. Am. J. Pathol. 184(2), (2014).