1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. PHA-543613 dihydrochloride

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.

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PHA-543613 dihydrochloride Chemical Structure

PHA-543613 dihydrochloride Chemical Structure

CAS No. : 478148-58-2

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Description

PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors[1]. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research[2][3].

IC50 & Target

Ki: 8.8 nM (α7 nAChR)[1]

In Vivo

PHA-543613 dihydrochloride (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats[2].
PHA-543613 dihydrochloride (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema is dependent on the PI3K-Akt signaling pathway[3].

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

Animal Model: Male CD-1 mice with (intracerebral hemorrhage) ICH-induction or sham surgery[3]
Dosage: 4 and 12 mg/kg
Administration: Intraperitoneal injection; 4 and 12 mg/kg; 1 hour after surgery
Result: Increased p-Akt and decreased p-GSK-3 and CC3 expressions in the ipsilateral hemisphere and reduced the neuronal cell death in the perihematomal area. Attenuated behavioral deficits and brain edema at 72 hours after ICH.
Molecular Weight

344.24

Formula

C15H19Cl2N3O2

CAS No.
SMILES

O=C(C1=CC2=C(OC=C2)C=N1)N[C@H]3CN4CCC3CC4.[H]Cl.[H]Cl

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PHA-543613 dihydrochloride Related Classifications

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    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:
PHA-543613 dihydrochloride
Cat. No.:
HY-105670B
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