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Purity: ≥98%
Farampator (also known as CX-691 or Org24448) is a positive and allosteric modulator of the AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoazolepropionic acid) receptor. CX691 attenuated a scopolamine-induced impairment of cued fear conditioning following acute administration (0.1 mg/kg p.o.) and a temporally induced deficit in novel object recognition following both acute (0.1 and 1.0 mg/kg p.o.) and sub-chronic (bi-daily for 7 days) administration (0.01, 0.03, 0.1 mg/kg p.o.). It also improved attentional set-shifting following sub-chronic administration (0.3 mg/kg p.o.). Thus, Farampator may have utility for the treatment of cognitive impairment such as such as Alzheimer's disease and schizophrenia.
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| ln Vivo |
Farampator may be used to treat conditions like schizophrenia and Alzheimer's disease that are characterized by cognitive impairments. CX691 reduces the effects of scopolamine on cued fear conditioning after acute administration (0.1 mg/kg po) and a temporally induced deficit in novel object recognition after sub-chronic (bi-daily for 7 days) and acute (0.1 and 1.0 mg/kg po) administration (0.01, 0.03, 0.1 mg/kg po). Additionally, after sub-chronic dosing (0.3 mg/kg po), it enhances attentional set-shifting[1]. Unquestionably, farampator (500 mg) enhances short-term memory, but it seems to degrade episodic memory. Moreover, it tends to reduce the CTMT's number of switching faults. Among the drug-induced side effects (SEs) were nausea, somnolence, and headache. Compared to participants without SEs, subjects with SEs had noticeably greater plasma levels of farampator[2].
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| References |
[1]. Woolley ML, et al. Evaluation of the pro-cognitive effects of the AMPA receptor positive modulator, 5-(1-piperidinylcarbonyl)-2,1,3-benzoxadiazole (CX691), in the rat. Psychopharmacology (Berl). 2009 Jan;202(1-3):343-54.
[2]. Wezenberg E, et al. Acute effects of the ampakine farampator on memory and information processing in healthy elderly volunteers. Neuropsychopharmacology. 2007 Jun;32(6):1272-83 |
| Molecular Formula |
C12H13N3O2
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| Molecular Weight |
231.26
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| CAS # |
211735-76-1
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| SMILES |
O=C(N1CCCCC1)C2=CC3=NON=C3C=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.81 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 25.0 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: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3241 mL | 21.6207 mL | 43.2414 mL | |
| 5 mM | 0.8648 mL | 4.3241 mL | 8.6483 mL | |
| 10 mM | 0.4324 mL | 2.1621 mL | 4.3241 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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