Ispronicline (Synonyms: TC-1734; ACD3480)

Name: Ispronicline
Brand: MedChemExpress
SKU: HY-10063
Rating: 4.5 (1 reviews)

Cat. No.: HY-10063 Purity: 98.24%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (K_i=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.

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

Ispronicline Chemical Structure

CAS No. : 252870-53-4

Size	Price	Stock	Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 83	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 83	In-stock	Estimated Time of Arrival: December 31
Liquid
5 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 270	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	106 nM Compound: 110, AZD-3480	Agonist activity at human alpha4beta2 nAChR expressed in HEK293 cells incubated for 5 mins measured every second for 1 mins followed by every 5 secs for 4 mins by calcium flux assay Agonist activity at human alpha4beta2 nAChR expressed in HEK293 cells incubated for 5 mins measured every second for 1 mins followed by every 5 secs for 4 mins by calcium flux assay	[PMID: 23121096]

In Vivo

Ispronicline (10-20 mg/kg; s.c.) induces c-Fos expression in selective regions of the rat forebrain^[1]. Ispronicline pharmacokinetics (half-life of 2 h in rats) contrasts with the long-lasting improvement of working memory (18 h to 2 d)^[2].

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

Animal Model:	Male Wistar rats weighting 180-200 g^[1]
Dosage:	10 and 30 mg/kg
Administration:	s.c.
Result:	Induced c-Fos in medial paraventricular nucleus of hypothalamus. Treatment with 30 mg/kg ispronicline, but not 10 mg/kg, increased the number of c-Fos immunoreactive cells significantly as compared to controls within the medial parvocellular part of paraventricular nucleus (PVN).

Clinical Trial

Molecular Weight

234.34

Formula

C₁₄H₂₂N₂O

CAS No.

252870-53-4

Appearance

Liquid (Density: 0.977±0.06 g/cm³)

Color

Colorless to light yellow

SMILES

C[C@H](NC)C/C=C/C1=CC(OC(C)C)=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (426.73 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	4.2673 mL	21.3365 mL	42.6730 mL
5 mM	0.8535 mL	4.2673 mL	8.5346 mL
10 mM	0.4267 mL	2.1337 mL	4.2673 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: ≥ 2.5 mg/mL (10.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 98.24%

Select Batch:

Data Sheet (269 KB) SDS (393 KB)

COA (242 KB) HNMR (246 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Julie Jacobsen, et al. The α4β2 nicotine acetylcholine receptor agonist ispronicline induces c-Fos expression in selective regions of the rat forebrain. Neurosci Lett. 2012 Apr 25;515(1):7-11. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	4.2673 mL	21.3365 mL	42.6730 mL	106.6826 mL
	5 mM	0.8535 mL	4.2673 mL	8.5346 mL	21.3365 mL
	10 mM	0.4267 mL	2.1337 mL	4.2673 mL	10.6683 mL
	15 mM	0.2845 mL	1.4224 mL	2.8449 mL	7.1122 mL
	20 mM	0.2134 mL	1.0668 mL	2.1337 mL	5.3341 mL
	25 mM	0.1707 mL	0.8535 mL	1.7069 mL	4.2673 mL
	30 mM	0.1422 mL	0.7112 mL	1.4224 mL	3.5561 mL
	40 mM	0.1067 mL	0.5334 mL	1.0668 mL	2.6671 mL
	50 mM	0.0853 mL	0.4267 mL	0.8535 mL	2.1337 mL
	60 mM	0.0711 mL	0.3556 mL	0.7112 mL	1.7780 mL
	80 mM	0.0533 mL	0.2667 mL	0.5334 mL	1.3335 mL
	100 mM	0.0427 mL	0.2134 mL	0.4267 mL	1.0668 mL

Ispronicline 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:

Ispronicline252870-53-4TC-1734 ACD3480TC1734TC 1734ACD3480ACD 3480ACD-3480nAChRNicotinic acetylcholine receptorsα4β2Agonistbrain-selectivememory-enhancingInhibitorinhibitorinhibit

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Ispronicline (Synonyms: TC-1734; ACD3480)

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Complete Stock Solution Preparation Table

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