Art. -Nr.: HY-10063

Ispronicline

Name: Ispronicline
Brand: MedChemExpress
SKU: HY-10063
Price: 45.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: TC-1734; ACD3480)

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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.

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Reinheit : 98.24%
CAS. Nr.: 252870-53-4
Formel: C₁₄H₂₂N₂O
Molecular Weight:234.34

Speicherung:

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

Ispronicline Chemical Structure

CAS. Nr.: 252870-53-4

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

Biologische Aktivität

Beschreibung

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 252870-53-4
Appearance Liquid (Density: 0.977±0.06 g/cm³)
Molecular Weight 234.34
Formel C₁₄H₂₂N₂O
Color Colorless to light yellow
SMILES

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

TC-1734; ACD3480
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

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

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

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.

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)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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]. 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]

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
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

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Ispronicline