nAChR agonist 1

Name: nAChR agonist 1
Brand: MedChemExpress
SKU: HY-133011
Rating: 4.5 (1 reviews)

Cat. No.: HY-133011 Purity: 98.35%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1394371-75-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 407	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 407	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1220	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
IMR-32	EC₅₀	324 nM Compound: 28	Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay	[PMID: 31755711]

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,T_1/2, CL, and Vss are 1.3 h μM, 0.9 μM, 1.4 hours, 31 mL/min/kg, 3 L/kg, respectively^[1].

MedChemExpress (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

Appearance

Solid

Color

Off-white to yellow

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

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (297.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.35%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (252 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Sinha N, et al.Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relati [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3813 mL	11.9065 mL	23.8129 mL	59.5323 mL
	5 mM	0.4763 mL	2.3813 mL	4.7626 mL	11.9065 mL
	10 mM	0.2381 mL	1.1906 mL	2.3813 mL	5.9532 mL
	15 mM	0.1588 mL	0.7938 mL	1.5875 mL	3.9688 mL
	20 mM	0.1191 mL	0.5953 mL	1.1906 mL	2.9766 mL
	25 mM	0.0953 mL	0.4763 mL	0.9525 mL	2.3813 mL
	30 mM	0.0794 mL	0.3969 mL	0.7938 mL	1.9844 mL
	40 mM	0.0595 mL	0.2977 mL	0.5953 mL	1.4883 mL
	50 mM	0.0476 mL	0.2381 mL	0.4763 mL	1.1906 mL
	60 mM	0.0397 mL	0.1984 mL	0.3969 mL	0.9922 mL
	80 mM	0.0298 mL	0.1488 mL	0.2977 mL	0.7442 mL
	100 mM	0.0238 mL	0.1191 mL	0.2381 mL	0.5953 mL

nAChR agonist 1 Related Classifications

Neurological Disease

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.

Keywords:

nAChR agonist 11394371-75-5nAChR agonist1nAChR agonist-1nAChRNicotinic acetylcholine receptorsAlzheimer’sdiseasebrain-permeableoralneuroblastomacellscognitivedeficitsInhibitorinhibitorinhibit

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nAChR agonist 1

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Complete Stock Solution Preparation Table

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