1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. nAChR
  3. nAChR agonist 1

nAChR agonist 1 

Cat. No.: HY-133011
Handling Instructions

nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.

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

nAChR agonist 1 Chemical Structure

nAChR agonist 1 Chemical Structure

CAS No. : 1394371-75-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease[1].

In Vivo

Acute (single-dose) oral administration of nAChR agonist 1 (compound 28) prior to memory acquisition, significantly increased the discrimination index in both time-delay and scopolamine-induced 8 amnesia at 1 and 3 mg/kg dose levels in male Wistar rats.nAChR agonist 1 also significantly improved the discrimination index in the memory consolidation paradigm, when administered immediately after the memory acquisition trial[1].
nAChR agonist 1 treatment (10 mg/kg; p.o.) shows that the AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively[1].
nAChR agonist 1 (1 mg/kg; i.v.) treatment shows that the AUC, Cmax,T1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice[1]
Dosage: 10 mg/kg
Administration: p.o.(Pharmacokinetic Analysis)
Result: The AUC, Cmax, and F values are 63 h μM, 2.3 μM, 63%, respectively.
Molecular Weight

419.94

Formula

C₂₀H₁₈ClNO₃S₂

CAS No.

1394371-75-5

SMILES

NS(C1=CC=C(C2=C(C(CC)=O)SC(C3=CC=C(Cl)C=C3)=C2C)C=C1)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (297.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3813 mL 11.9065 mL 23.8129 mL
5 mM 0.4763 mL 2.3813 mL 4.7626 mL
10 mM 0.2381 mL 1.1906 mL 2.3813 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

nAChR agonist 1nAChR agonist1nAChR agonist-1nAChRNicotinic acetylcholine receptorsAlzheimer’sdiseasebrain-permeableoralneuroblastomacellscognitivedeficitsInhibitorinhibitorinhibit

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nAChR agonist 1
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