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.
For research use only. We do not sell to patients.
- CAS No.: 478148-58-2
- Formula: C15H19Cl2N3O2
- Molecular Weight:344.24
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
Ki: 8.8 nM (α7 nAChR)[1]
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 mice with (intracerebral hemorrhage) ICH-induction or sham surgery[3]
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Dosage:4 and 12 mg/kg
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Administration:Intraperitoneal injection; 4 and 12 mg/kg; 1 hour after surgery
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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.
Chemical Information
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CAS No. 478148-58-2
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Appearance Solid
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Molecular Weight 344.24
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Formula C15H19Cl2N3O2
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Color White to off-white
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SMILES
O=C(C1=CC2=C(OC=C2)C=N1)N[C@H]3CN4CCC3CC4.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocols
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Donn G Wishka, et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49(14):4425-36. [Content Brief]
[2]. Nóra Bruszt, et al. Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task. Psychopharmacology (Berl). 2021 Nov;238(11):3273-3281. [Content Brief]
[3]. Krafft PR, et al. α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage. Stroke. 2012 Mar;43(3):844-50. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PHA-543613 dihydrochloride Related Classifications
HY-105670B Related Classifications
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