4F 4PP oxalate

Cat No.:V71151 Purity: ≥98%
4F 4PP (oxalate) is a selective 5-HT2A antagonist (inhibitor) with almost as high affinity as ketotryptamine (Ki= 5.3 nM) but much lower affinity for the 5-HT2C site (Ki= 620 nM ).
4F 4PP oxalate Chemical Structure CAS No.: 144734-36-1
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
4F 4PP (oxalate) is a selective 5-HT2A antagonist (inhibitor) with almost as high affinity as ketotryptamine (Ki= 5.3 nM) but much lower affinity for the 5-HT2C site (Ki= 620 nM ).
Biological Activity I Assay Protocols (From Reference)
Targets
5-HT2A Receptor 5.3 nM (Ki) 5-HT2C Receptor 620 nM (Ki)
ln Vivo
In addition to producing a considerable depression of evoked field potentials, 4F 4PP (100 nM) lowers the lowest concentration of [D-ala2,N-me-phe4,gly.l5]-enkephalin (DAMGO)[1].
References
[1]. Aira Z, et al. Selective impairment of spinal mu-opioid receptor mechanism by plasticity of serotonergic facilitation mediated by 5-HT2A and 5-HT2B receptors. Pain. 2012;153(7):1418-1425.
[2]. Lee SH, et al. Peripheral serotonin receptor 2B and transient receptor potential channel 4 mediate pruritus to serotonergic antidepressants in mice. J Allergy Clin Immunol. 2018;142(4):1349-1352.e16.
[3]. Rodríguez-Muñoz M, et al. Fenfluramine diminishes NMDA receptor-mediated seizures via its mixed activity at serotonin 5HT2A and type 1 sigma receptors. Oncotarget. 2018;9(34):23373-23389. Published 2018 May 4.
[4]. Gerhold KJ, et al. Pronociceptive and Antinociceptive Effects of Buprenorphine in the Spinal Cord Dorsal Horn Cover a Dose Range of Four Orders of Magnitude. J Neurosci. 2015;35(26):9580-9594.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H28FNO5
Molecular Weight
429.48
CAS #
144734-36-1
SMILES
C(O)(=O)C(O)=O.FC1C=CC(C(C2CCN(CCCCC3C=CC=CC=3)CC2)=O)=CC=1
Solubility Data
Solubility (In Vitro)
DMSO: 12.5 mg/mL (29.10 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 1.67 mg/mL (3.89 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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: ≥ 1.67 mg/mL (3.89 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 16.7 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.

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Solubility in Formulation 3: ≥ 1.67 mg/mL (3.89 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 16.7 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 2.3284 mL 11.6420 mL 23.2840 mL
5 mM 0.4657 mL 2.3284 mL 4.6568 mL
10 mM 0.2328 mL 1.1642 mL 2.3284 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.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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