1. PI3K/Akt/mTOR Epigenetics
  2. Akt PI3K Epigenetic Reader Domain
  3. PI3K/Akt/CREB activator 1

PI3K/Akt/CREB activator 1 (compound AE-18) is a potent, orally active PI3K/Akt/CREB activator. PI3K/Akt/CREB activator 1 promotes neuronal proliferation, induced differentiation of Neuro-2a cells into a neuron-like morphology, and accelerated the establishment of axon-dendrite polarization of primary hippocampal neurons through upregulating brain-derived neurotrophic factor via the PI3K/Akt/CREB pathway. PI3K/Akt/CREB activator 1 can be used in research of vascular dementia (VaD).

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PI3K/Akt/CREB activator 1 Chemical Structure

PI3K/Akt/CREB activator 1 Chemical Structure

CAS No. : 2708177-73-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

PI3K/Akt/CREB activator 1 (compound AE-18) is a potent, orally active PI3K/Akt/CREB activator. PI3K/Akt/CREB activator 1 promotes neuronal proliferation, induced differentiation of Neuro-2a cells into a neuron-like morphology, and accelerated the establishment of axon-dendrite polarization of primary hippocampal neurons through upregulating brain-derived neurotrophic factor via the PI3K/Akt/CREB pathway. PI3K/Akt/CREB activator 1 can be used in research of vascular dementia (VaD)[1].

In Vitro

PI3K/Akt/CREB activator 1 (compound AE-18; 10 and 20 μM; 48 h) induces neurite outgrowth and proliferation through upregulating BDNF via the PI3K/Akt/CREB pathway Neuro-2a cells[1].
PI3K/Akt/CREB activator 1 (10 and 20 μM; neurons) enhances neuronal differentiation and axon-dendrite polarization in cultured hippocampal neurons through the PI3K/AKT signal pathway[1].

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

Western Blot Analysis[1]

Cell Line: Neuro-2a cells
Concentration: 10 and 20 μM
Incubation Time: 48 hours
Result: Increased the expressions of BDNF and the phosphorylated form of AKT (pAKT) and CREB (pCREB).
In Vivo

PI3K/Akt/CREB activator 1 (compound AE-18; 5 and 10 mg/kg; i.g.; male Sprague-Dawley rats with chronic cerebral hypoperfusion (CCH) model) improves cerebral blood flow (CBF) recovery after bilateral common carotid artery occlusion (BCCAO)[1].
PI3K/Akt/CREB activator 1 (5 and 10 mg/kg; i.g.; for 5 d) mitigates impairment of learning and memory in chronic cerebral hypoperfusion (CCH) rat model and alleviates CCH-induced pathological injury in the hippocampus after BCCAO[1].

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

Animal Model: Male Sprague-Dawley rats (200-220 g) with chronic cerebral hypoperfusion (CCH) model[1]
Dosage: 5 and 10 mg/kg
Administration: Oral gavage; daily, for 6 weeks
Result: Promoted the recovery of CBF after BCCAO.
Animal Model: Male Sprague-Dawley rats (200-220 g) with chronic cerebral hypoperfusion (CCH) model[1]
Dosage: 5 and 10 mg/kg
Administration: Oral gavage; daily, for 5 days
Result: Reduced escape latency from day 1 to day 5 of the morris water maze (MWM) test compared with the CCH group.
Improved cognitive deficits in CCH rat model.
Molecular Weight

381.32

Formula

C19H15F4NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C(O)=O)CC1=CC=C(C=C1)F)/C=C/C2=CC=C(C=C2)C(F)(F)F

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 : 250 mg/mL (655.62 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 2.6225 mL 13.1123 mL 26.2247 mL
5 mM 0.5245 mL 2.6225 mL 5.2449 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (5.45 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.45 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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. 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 2.6225 mL 13.1123 mL 26.2247 mL 65.5617 mL
5 mM 0.5245 mL 2.6225 mL 5.2449 mL 13.1123 mL
10 mM 0.2622 mL 1.3112 mL 2.6225 mL 6.5562 mL
15 mM 0.1748 mL 0.8742 mL 1.7483 mL 4.3708 mL
20 mM 0.1311 mL 0.6556 mL 1.3112 mL 3.2781 mL
25 mM 0.1049 mL 0.5245 mL 1.0490 mL 2.6225 mL
30 mM 0.0874 mL 0.4371 mL 0.8742 mL 2.1854 mL
40 mM 0.0656 mL 0.3278 mL 0.6556 mL 1.6390 mL
50 mM 0.0524 mL 0.2622 mL 0.5245 mL 1.3112 mL
60 mM 0.0437 mL 0.2185 mL 0.4371 mL 1.0927 mL
80 mM 0.0328 mL 0.1639 mL 0.3278 mL 0.8195 mL
100 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6556 mL
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PI3K/Akt/CREB activator 1 Related Classifications

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  • 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.

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