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

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.

For research use only. We do not sell to patients.

PHA-543613 Chemical Structure

PHA-543613 Chemical Structure

CAS No. : 478149-53-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 148 In-stock
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5 mg USD 135 In-stock
10 mg USD 220 In-stock
25 mg USD 480 In-stock
50 mg USD 820 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PHA-543613:

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  • Purity & Documentation

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Description

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[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]

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 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

271.31

Formula

C15H17N3O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (921.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (368.58 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6858 mL 18.4291 mL 36.8582 mL
5 mM 0.7372 mL 3.6858 mL 7.3716 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.95%

References

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 3.6858 mL 18.4291 mL 36.8582 mL 92.1455 mL
5 mM 0.7372 mL 3.6858 mL 7.3716 mL 18.4291 mL
10 mM 0.3686 mL 1.8429 mL 3.6858 mL 9.2146 mL
15 mM 0.2457 mL 1.2286 mL 2.4572 mL 6.1430 mL
20 mM 0.1843 mL 0.9215 mL 1.8429 mL 4.6073 mL
25 mM 0.1474 mL 0.7372 mL 1.4743 mL 3.6858 mL
30 mM 0.1229 mL 0.6143 mL 1.2286 mL 3.0715 mL
40 mM 0.0921 mL 0.4607 mL 0.9215 mL 2.3036 mL
50 mM 0.0737 mL 0.3686 mL 0.7372 mL 1.8429 mL
60 mM 0.0614 mL 0.3072 mL 0.6143 mL 1.5358 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 0.9215 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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PHA-543613 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    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
Cat. No.:
HY-105670
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