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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- CAS No.: 478148-58-2
- 화학식: C15H19Cl2N3O2
- 분자량:344.24
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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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분자량 344.24
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
순도&문서
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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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