FSC231 is a PSD-95/DLG/ZO-1 (PDZ) domain inhibitor of PICK1. FSC231 has analgesic effects.

Physicochemical Properties

Molecular Formula	C13H10CL2N2O3
Molecular Weight	313.14
CAS #	1215849-96-9
Appearance	Solid powder ; White to off-white
Density	1.4±0.1 g/cm3
Index of Refraction	1.594
LogP	3.26
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
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	PICK1[1].
ln Vitro	FSC231 (50 μM) blocks the binding between GluR2 and PICK1 in COS7 cells [2].
ln Vivo	FSC231 (78.40 μg/kg in total, daily, seven intraperitoneal injections, 3 hours before paclitaxel administration) can alleviate paclitaxel induced neuropathic pain in rats[1]. FSC231 (39.2 μg/kg/day, intraperitoneal injection, for 4 weeks) inhibits the development of diabetic cardiomyopathy in rats, in part by inhibiting ROS generation and apoptosis through the PICK1/eNOS/cGMP pathway[3].
Animal Protocol	Animal/Disease Models: Paclitaxel induced neuralgia of rats[1] Doses: 78.40 μg/kg in total Route of Administration: i.p., daily, seven times, completed at 3 h before Paclitaxel Experimental Results: Reversed the changes of inflammatory cytokines (IL‐6, TNF‐α and IL‐10). Inhibited the phosphorylation levels of GSK‐3β and ERK1/2.
References	[1]. FSC231 alleviates paclitaxel-induced neuralgia by inhibiting the interactions between PICK1 and GluA2 and activates GSK-3β and ERK1/2. Brain Behav. 2021 Nov;11(11):e2380. [2]. Identification of a small-molecule inhibitor of the PICK1 PDZ domain that inhibits hippocampal LTP and LTD. Proc Natl Acad Sci U S A. 2010 Jan 5;107(1):413-8. [3]. GW27-e1146 PICK1 inhibition restores myocardial injury by suppressing reactive oxygen species generation and apoptosis in diabetic rats. J Am Coll Cardiol. 2016 Oct, 68 (16_Supplement) C67.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~159.67 mM; with ultrasonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.98 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 cam add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.1935 mL	15.9673 mL	31.9346 mL
	5 mM	0.6387 mL	3.1935 mL	6.3869 mL
	10 mM	0.3193 mL	1.5967 mL	3.1935 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.