2. Neuronal Signaling Membrane Transporter/Ion Channel
  3. Cholinesterase (ChE) Potassium Channel Sodium Channel
  4. Ipidacrine

Ipidacrine  (Synonyms: NIK-247 free base)

Cat. No.: HY-W027553 Purity: 99.81%
COA Handling Instructions

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Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases.

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

Ipidacrine Chemical Structure

Ipidacrine Chemical Structure

CAS No. : 62732-44-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
100 mg USD 60 In-stock
500 mg USD 80 In-stock
1 g USD 110 In-stock
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Based on 1 publication(s) in Google Scholar

Ipidacrine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases[1][2][3][4][5].

In Vitro

Ipidacrine showes a concentration-dependent and reversible inhibition of AChE and BuChE activity with IC50 values of 1 μM and 1.9 μM, respectively[1].

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

Ipidacrine Related Antibodies
In Vivo

Ipidacrine (1 mg/kg, p.o., repeated and a single dose for 5 days) by repeated administration has more potent antiamnesic effects than by single administration in induced by nucleus basalis of meynert (NBM) induced rats[1].
Ipidacrine (10 mg/kg p.o., a single dose) significantly decreases spontaneous movements, which is more selective as an antiamnesic than either Tacrine (HY-111338) and E-2020 (HY-B0034) in rats[1].
Ipidacrine (6.7 mg/kg, intragastrically, daily for 14 days) leads to statistically more efficient evolving of intracavernous pressure (ICPmax)/maxipressure (MAP) compared with control group in Streptozotocin (STZ) (HY-13753)-induced diabetic rats[3].

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

Animal Model: Rats[1]
Dosage: 1 mg/kg
Administration: p.o., repeated and a single dose for 5 days
Result: The repeated administration of ipidacrine improved amnesia induced by nucleus basalis of meynert (NBM) lesions in the passive avoidance task in rats.
Animal Model: Rats[1]
Dosage: 3, 10, 30 mg/kg
Administration: p.o., a single dose
Result: Decreased pupil size and increased salivation at 3 mg/kg, decreased spontaneous movements at 10 mg/kg and decreased body temperature and induced tremor at 30 mg/kg in rats.
Animal Model: Rats with streptozotocin (STZ) (HY-13753) induced diabetes mellitus-induced erectile dysfunction (DMED)[1]
Dosage: 6.7 mg/kg
Administration: crushed, suspended in 1% starch solution and administered intragastrically daily for 14 days
Result: Ipidacrine was as effective as sildenafil and could significantly improve DMED symptoms.
Molecular Weight

188.27

Formula

C12H16N2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=C(CCC2)C2=NC3=C1CCCC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (354.12 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 5.3115 mL 26.5576 mL 53.1152 mL
5 mM 1.0623 mL 5.3115 mL 10.6230 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 (protect from light). 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)

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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 (13.28 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 (13.28 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.81%

COA (251 KB) HNMR (130 KB) RP-HPLC (254 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 5.3115 mL 26.5576 mL 53.1152 mL 132.7880 mL
5 mM 1.0623 mL 5.3115 mL 10.6230 mL 26.5576 mL
10 mM 0.5312 mL 2.6558 mL 5.3115 mL 13.2788 mL
15 mM 0.3541 mL 1.7705 mL 3.5410 mL 8.8525 mL
20 mM 0.2656 mL 1.3279 mL 2.6558 mL 6.6394 mL
25 mM 0.2125 mL 1.0623 mL 2.1246 mL 5.3115 mL
30 mM 0.1771 mL 0.8853 mL 1.7705 mL 4.4263 mL
40 mM 0.1328 mL 0.6639 mL 1.3279 mL 3.3197 mL
50 mM 0.1062 mL 0.5312 mL 1.0623 mL 2.6558 mL
60 mM 0.0885 mL 0.4426 mL 0.8853 mL 2.2131 mL
80 mM 0.0664 mL 0.3320 mL 0.6639 mL 1.6599 mL
100 mM 0.0531 mL 0.2656 mL 0.5312 mL 1.3279 mL
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Ipidacrine 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.

Keywords:

Ipidacrine62732-44-9NIK-247NIK247NIK 247Cholinesterase (ChE)Potassium ChannelSodium ChannelKcsANa channelsNa+ channelsorally activebrain-penetrantAChEBuChEM2-cholinergic receptorsanti-pain effectK+ and Na+-channelsAlzheimer’s diseaseischaemic strokediabetes mellitus-induced erectile dysfunctionother deficits in central or peripheral cholinergic deseasesInhibitorinhibitorinhibit

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