Art. -Nr.: HY-105670

PHA-543613

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PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a K_i 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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Reinheit: 99.95%
CAS. Nr.: 478149-53-0
Formel: C₁₅H₁₇N₃O₂
Molecular Weight:271.32

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PHA-543613 Chemical Structure

CAS. Nr.: 478149-53-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

Ki: 8.8 nM (α7 nAChR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
SH-SY5Y	IC₅₀	>100 μM Compound: 14, PHA-543613	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	[PMID: 16821801]
SH-SY5Y	IC₅₀	>100 μM Compound: PHA-543613	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	[PMID: 18490160]
TE-671	IC₅₀	>100 μM Compound: 14, PHA-543613	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	[PMID: 16821801]
TE-671	IC₅₀	>100 μM Compound: PHA-543613	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	[PMID: 18490160]

In Vivo

PHA-543613 (0.3 mg/kg) successfully reverses Scopolamine-induced short-term memory deficits in rats^[2].
PHA-543613 (4 and 12 mg/kg; i.p. once) reduces behavioral deficits and brain edema^[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.

Chemical Information

CAS. Nr. 478149-53-0
Appearance Solid
Molecular Weight 271.32
Formel C₁₅H₁₇N₃O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6857 mL

18.4284 mL

36.8568 mL

5 mM

0.7371 mL

3.6857 mL

7.3714 mL

10 mM

0.3686 mL

1.8428 mL

3.6857 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

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PHA-543613

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

3D Diverse Fragment Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PHA-543613

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

3D Diverse Fragment Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PHA-543613 Related Classifications

HY-105670 Related Classifications