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| ln Vitro |
PI3K/Akt/CREB activator 1 (compound AE-18; 10 and 20 μM; 48 h) upregulates BDNF via the PI3K/Akt/CREB pathway Neuro-2a cells, thereby inducing neurite outgrowth and proliferation[1]. Via the PI3K/AKT signal pathway, PI3K/Akt/CREB activator 1 (10 and 20 μM; neurons) improves neuronal differentiation and axon-dendrite polarization in cultured hippocampal neurons[1].
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| ln Vivo |
In male Sprague-Dawley rats with chronic cerebral hypoperfusion (CCH) model, compound AE-18, which contains PI3K/Akt/CREB activator 1 at doses of 5 and 10 mg/kg, enhances cerebral blood flow (CBF) recovery following bilateral common carotid artery occlusion (BCCAO)[1]. In the chronic cerebral hypoperfusion (CCH) rat model, PI3K/Akt/CREB activator 1 (5 and 10 mg/kg; ig; for 5 d) reduces learning and memory impairment and lessens CCH-induced pathological injury in the hippocampus following BCCAO[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Neuro-2a cells Tested Concentrations: 10 and 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Increased the expressions of BDNF and the phosphorylated form of AKT (pAKT) and CREB (pCREB). |
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) rats (200-220 g) with chronic cerebral hypoperfusion (CCH) model[1]
Doses: 5 and 10 mg/kg Route of Administration: po (oral gavage); daily, for 6 weeks Experimental Results: Promoted the recovery of CBF after BCCAO. Animal/Disease Models: Male SD (Sprague-Dawley) rats (200-220 g) with chronic cerebral hypoperfusion (CCH) model[1] Doses: 5 and 10 mg/kg Route of Administration: po (oral gavage); daily, for 5 days Experimental Results: diminished 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. |
| References |
| Molecular Formula |
C19H15F4NO3
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|---|---|
| Molecular Weight |
381.320919275284
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| Exact Mass |
381.098
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| CAS # |
2708177-73-3
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| PubChem CID |
165437247
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| Appearance |
White to off-white solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
534
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C=CC(=CC=1)C[C@@H](C(=O)O)NC(/C=C/C1C=CC(C(F)(F)F)=CC=1)=O
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| InChi Key |
VXTNIOWCDILANK-YKXBDCQTSA-N
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| InChi Code |
InChI=1S/C19H15F4NO3/c20-15-8-3-13(4-9-15)11-16(18(26)27)24-17(25)10-5-12-1-6-14(7-2-12)19(21,22)23/h1-10,16H,11H2,(H,24,25)(H,26,27)/b10-5+/t16-/m0/s1
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| Chemical Name |
(2S)-3-(4-fluorophenyl)-2-[[(E)-3-[4-(trifluoromethyl)phenyl]prop-2-enoyl]amino]propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 250 mg/mL (655.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2622 mL | 1.3112 mL | 2.6225 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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