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 ).

Physicochemical Properties

Molecular Formula	C24H28FNO5
Molecular Weight	429.48
Exact Mass	429.195
CAS #	144734-36-1
PubChem CID	24745966
Appearance	White to off-white solid powder
LogP	3.836
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	8
Heavy Atom Count	31
Complexity	462
Defined Atom Stereocenter Count	0
SMILES	C1CN(CCC1C(=O)C2=CC=C(C=C2)F)CCCCC3=CC=CC=C3.C(=O)(C(=O)O)O
InChi Key	VUJYJCRJPFMHEM-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H26FNO.C2H2O4/c23-21-11-9-19(10-12-21)22(25)20-13-16-24(17-14-20)15-5-4-8-18-6-2-1-3-7-18;3-1(4)2(5)6/h1-3,6-7,9-12,20H,4-5,8,13-17H2;(H,3,4)(H,5,6)
Chemical Name	(4-fluorophenyl)-[1-(4-phenylbutyl)piperidin-4-yl]methanone;oxalic acid
HS Tariff Code	2934.99.9001
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)

Biological Activity

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.

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. 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.