Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
5-HT1A Receptor
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ln Vivo |
Befiradol (F13640; NLX-112) raises the discharge rate of 80% of mPFC pyramidal neurons in the same dose range (ED50=0.62 μg/kg, iv) and decreases the activity of dorsal raphe serotonergic neurons at 0.2-18.2 μg/kg, iv (cumulative doses; ED50=0.69 μg/kg, iv). Subsequent injection of the 5-HT1A receptor antagonist (±)WAY100635 reverses both effects. Befiradol (F13640; NLX-112) (0.04 -0.63 mg/kg, ip) dose-dependently reduces extracellular 5-HT in the mPFC and hippocampal regions in microdialysis experiments. Similarly, Befiradol (F13640; NLX-112) (0.01-2.5 mg/kg, ip) raises extracellular DA in mPFC in a dose-dependent manner. a result reliant on the mPFC's postsynaptic 5-HT1A receptors being activated. In a concentration-dependent manner, local perfusion of Befiradol in mPFC (1-1,000 μM) likewise raises extracellular DA. Befiradol's local and systemic effects can be avoided by administering (±)WAY100635 beforehand[1].
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References |
[1]. Lladó-Pelfort L, et al. In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat. Psychopharmacology (Berl). 2012 May;221(2):261-72
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Molecular Formula |
C20H23CL2F2N3O
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Molecular Weight |
430.32
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CAS # |
2436760-81-3
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Related CAS # |
Befiradol;208110-64-9
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SMILES |
C(C1C=CC(=C(C=1)Cl)F)(N1CCC(CC1)(F)CNCC1N=CC(=CC=1)C)=O.Cl
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: 125 mg/mL (290.48 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.83 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 (4.83 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 20.8 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: ≥ 2.08 mg/mL (4.83 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 | 2.3239 mL | 11.6193 mL | 23.2385 mL | |
5 mM | 0.4648 mL | 2.3239 mL | 4.6477 mL | |
10 mM | 0.2324 mL | 1.1619 mL | 2.3239 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.