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EP2 receptor antagonist-2 615273-95-5

EP2 receptor antagonist-2 615273-95-5

CAS No.: 615273-95-5

EP2 receptor antagonist-2 (CID891729) is an EP2 receptor antagonist. EP2 receptor antagonist-2 inhibits PGE2-induced EP2
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EP2 receptor antagonist-2 (CID891729) is an EP2 receptor antagonist. EP2 receptor antagonist-2 inhibits PGE2-induced EP2 receptor activation. EP2 receptor antagonist-2 also inhibits lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).

Physicochemical Properties


Molecular Formula C15H14F3N3O
Molecular Weight 309.29
Exact Mass 309.108
CAS # 615273-95-5
PubChem CID 891729
Appearance White to off-white solid powder
Density 1.3±0.1 g/cm3
Boiling Point 451.8±55.0 °C at 760 mmHg
Flash Point 227.0±31.5 °C
Vapour Pressure 0.0±1.1 mmHg at 25°C
Index of Refraction 1.533
LogP 3.81
Hydrogen Bond Donor Count 0
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 2
Heavy Atom Count 22
Complexity 354
Defined Atom Stereocenter Count 0
InChi Key GCCXGRJKBSVDIZ-UHFFFAOYSA-N
InChi Code

InChI=1S/C15H14F3N3O/c16-15(17,18)13-10-12(11-4-2-1-3-5-11)19-14(20-13)21-6-8-22-9-7-21/h1-5,10H,6-9H2
Chemical Name

4-[4-phenyl-6-(trifluoromethyl)pyrimidin-2-yl]morpholine
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: This product requires protection from light (avoid light exposure) during transportation and storage.
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 EP
ln Vitro With a CC50 of 575 μM, EP2 receptor antagonist-2 is cytotoxic to C6G cells[1]. In rat primary hippocampal neurons (DIV14), NMDA (30 μM)-induced LDH release is lessened by EP2 receptor antagonist-2 (20 μM; 30 min) [1].
References

[1]. Discovery of 2-Piperidinyl Phenyl Benzamides and Trisubstituted Pyrimidines as Positive Allosteric Modulators of the Prostaglandin Receptor EP2. ACS Chem Neurosci. 2018 Apr 18;9(4):699-707.


Solubility Data


Solubility (In Vitro) DMSO: 125 mg/mL (404.15 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 2.08 mg/mL (6.73 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 20.8 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 3.2332 mL 16.1661 mL 32.3321 mL
5 mM 0.6466 mL 3.2332 mL 6.4664 mL
10 mM 0.3233 mL 1.6166 mL 3.2332 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.