L-826266 is a selective and competitive EP3 receptor blocker (antagonist) that may be utilized in the research/study of convulsive diseases.

Physicochemical Properties

Molecular Formula	C27H21BRCLNO4S
Molecular Weight	570.88
Exact Mass	569.006
CAS #	244101-03-9
PubChem CID	9808643
Appearance	White to off-white solid powder
Density	1.5±0.1 g/cm3
Index of Refraction	1.662
LogP	8.29
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	7
Heavy Atom Count	35
Complexity	847
Defined Atom Stereocenter Count	0
SMILES	COC1=C(C=C(C=C1)Br)S(=O)(=O)NC(=O)/C=C/C2=C(C=CC(=C2)Cl)CC3=CC4=CC=CC=C4C=C3
InChi Key	DYXFUJYHEDGCLS-UKTHLTGXSA-N
InChi Code	InChI=1S/C27H21BrClNO4S/c1-34-25-12-10-23(28)17-26(25)35(32,33)30-27(31)13-9-22-16-24(29)11-8-21(22)15-18-6-7-19-4-2-3-5-20(19)14-18/h2-14,16-17H,15H2,1H3,(H,30,31)/b13-9+
Chemical Name	(E)-N-(5-bromo-2-methoxyphenyl)sulfonyl-3-[5-chloro-2-(naphthalen-2-ylmethyl)phenyl]prop-2-enamide
Synonyms	L-826266 L826266 L 826266
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

ln Vitro	L-826266 (1 μM) inhibits the PGE2-induced reduction in Na+,K+-ATPase activity in adult rat hippocampus slices [2].
ln Vivo	PTZ-induced clonic and generalized tonic-clonic seizures exhibit delayed seizure start and increased latency when treated with L-826266 (0.01-1 nmol/site; icv; once) [1].
Animal Protocol	Animal/Disease Models: Adult male Wistar rats (250-300 g) were injected with pentylenetetrazole (PTZ) [1] Doses: 0.01 nmol/site, 0.1 nmol/site or 1 nmol/site Route of Administration: icv; Experimental Results: Increased latency of PTZ-induced clonic and generalized tonic-clonic seizures.
References	[1]. Modulation of pentylenetetrazol-induced seizures by prostaglandin E2 receptors. Neuroscience. 2008 Apr 9;152(4):1110-8. [2]. Prostaglandin E2 modulates Na+,K+-ATPase activity in rat hippocampus: implications for neurological diseases. J Neurochem. 2009 Apr;109(2):416-26.

Solubility Data

Solubility (In Vitro)

DMSO : ~10 mg/mL (~17.52 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 1.67 mg/mL (2.93 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 (2.93 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	1.7517 mL	8.7584 mL	17.5168 mL
	5 mM	0.3503 mL	1.7517 mL	3.5034 mL
	10 mM	0.1752 mL	0.8758 mL	1.7517 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.