PHA-543613
Based on 1 Customer Validation
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
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- Purity: 99.95%
- CAS No.: 478149-53-0
- 화학식: C15H17N3O2
- 분자량:271.32
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
Ki: 8.8 nM (α7 nAChR)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | IC50 |
>100 μM
Compound: 14, PHA-543613
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Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
Inhibition of alpha-3-beta-4 nAChR expressed in SHSY5Y cells by FLIPR assay
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[PMID: 16821801] |
| SH-SY5Y | IC50 |
>100 μM
Compound: PHA-543613
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Activity at alpha-3-beta-4 nACh receptor expressed in human SH-SY5Y cells by FLIPR assay
Activity at alpha-3-beta-4 nACh receptor expressed in human SH-SY5Y cells by FLIPR assay
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[PMID: 18490160] |
| TE-671 | IC50 |
>100 μM
Compound: 14, PHA-543613
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Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
Inhibition of alpha-1-beta-1-gamma-delta nAChR expressed in TE671cells by FLIPR assay
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[PMID: 16821801] |
| TE-671 | IC50 |
>100 μM
Compound: PHA-543613
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Activity at alpha-1-beta-1-gamma-delta nACh receptor expressed in human TE671 cells by FLIPR assay
Activity at alpha-1-beta-1-gamma-delta nACh receptor expressed in human TE671 cells by FLIPR assay
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[PMID: 18490160] |
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. 478149-53-0
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Appearance Solid
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분자량 271.32
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화학식 C15H17N3O2
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
H2O : 100 mg/mL (368.57 mM; Need ultrasonic)
DMSO : ≥ 100 mg/mL (368.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.6857 mL | 18.4284 mL | 36.8568 mL | 92.1421 mL |
| 5 mM | 0.7371 mL | 3.6857 mL | 7.3714 mL | 18.4284 mL | |
| 10 mM | 0.3686 mL | 1.8428 mL | 3.6857 mL | 9.2142 mL | |
| 15 mM | 0.2457 mL | 1.2286 mL | 2.4571 mL | 6.1428 mL | |
| 20 mM | 0.1843 mL | 0.9214 mL | 1.8428 mL | 4.6071 mL | |
| 25 mM | 0.1474 mL | 0.7371 mL | 1.4743 mL | 3.6857 mL | |
| 30 mM | 0.1229 mL | 0.6143 mL | 1.2286 mL | 3.0714 mL | |
| 40 mM | 0.0921 mL | 0.4607 mL | 0.9214 mL | 2.3036 mL | |
| 50 mM | 0.0737 mL | 0.3686 mL | 0.7371 mL | 1.8428 mL | |
| 60 mM | 0.0614 mL | 0.3071 mL | 0.6143 mL | 1.5357 mL | |
| 80 mM | 0.0461 mL | 0.2304 mL | 0.4607 mL | 1.1518 mL | |
| 100 mM | 0.0369 mL | 0.1843 mL | 0.3686 mL | 0.9214 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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