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| Targets |
EP
EP2 receptor (prostaglandin E2 receptor 2). EP2 receptor antagonist-2 (CID891729) is an EP2 receptor antagonist. It blocks the activity of the prostaglandin E2 receptor EP2, inhibiting cAMP signaling and thereby modulating inflammatory responses and cellular functions. By blocking EP2 activation by PGE2, it reduces downstream signaling pathways. |
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| 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].
EP2 receptor antagonist-2 inhibits PGE2-induced EP2 receptor activation. In rat primary hippocampal neurons (DIV14), NMDA (30 μM)-induced LDH release is reduced by EP2 receptor antagonist-2 (20 μM; 30 min). It has a CC50 of 575 μM in C6G cells, indicating its cytotoxicity profile. |
| ln Vivo |
In vivo, EP2 receptor antagonist-2 would be expected to exert anti-inflammatory and neuroprotective effects through its EP2 receptor antagonism. By blocking PGE2-mediated EP2 signaling, it could modulate inflammatory responses and protect against excitotoxic neuronal damage. Its effects in vivo would be assessed in animal models of inflammation, neurodegeneration, and cancer.
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| Enzyme Assay |
In vitro binding assays are used to characterize EP2 receptor antagonist-2 as an EP2 receptor antagonist. Radioligand binding assays or functional assays measuring inhibition of PGE2-induced cAMP accumulation are performed using cells expressing the EP2 receptor to confirm its antagonistic activity.
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| Cell Assay |
Cellular assays for EP2 receptor antagonist-2 involve treating EP2-expressing cells with the compound and measuring inhibition of PGE2-induced responses. Functional readouts include inhibition of cAMP accumulation or downstream signaling. The compound also inhibits NMDA-induced LDH release in rat primary hippocampal neurons, demonstrating neuroprotective activity in cellular models.
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| Animal Protocol |
In vivo studies with EP2 receptor antagonist-2 would be performed in animal models of inflammation, neuroprotection, or cancer. The compound could be administered via injection, and its effects on inflammatory responses, neuronal damage, and tumor growth would be assessed. Its EP2 antagonistic activity makes it a potential tool for studying EP2-mediated diseases.
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| ADME/Pharmacokinetics |
EP2 receptor antagonist-2 has a molecular formula of C15H14F3N3O and a molecular weight of 309.29. It is a small molecule with a LogP of 3.81 and is soluble in DMSO (125 mg/mL). The compound should be protected from light during storage. Powder is stable for 3 years at -20°C and 2 years at 4°C.
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| Toxicity/Toxicokinetics |
EP2 receptor antagonist-2 has a CC50 of 575 μM in C6G cells, indicating its cytotoxicity profile. As an EP2 receptor antagonist, its safety profile would be an important consideration for potential therapeutic applications. Potential toxicities could be related to its effects on PGE2-mediated signaling in various tissues. Standard preclinical safety studies would be required.
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| References | |
| Additional Infomation |
EP2 receptor antagonist-2 (CID891729, CAS#: 615273-95-5) is a prostaglandin EP2 receptor antagonist. It inhibits PGE2-induced EP2 receptor activation and NMDA-induced LDH release. It has a molecular formula of C15H14F3N3O and a molecular weight of 309.29. It is a research tool for studying EP2 receptor function in inflammation, neuroprotection, and cancer.
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| Molecular Formula |
C15H14F3N3O
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|---|---|
| Molecular Weight |
309.29
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| Exact Mass |
309.108
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| CAS # |
615273-95-5
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| PubChem CID |
891729
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
451.8±55.0 °C at 760 mmHg
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| Flash Point |
227.0±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.533
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| LogP |
3.81
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
354
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1C2=NC(=CC(=N2)C(F)(F)F)C3=CC=CC=C3
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| InChi Key |
GCCXGRJKBSVDIZ-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-[4-phenyl-6-(trifluoromethyl)pyrimidin-2-yl]morpholine
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 125 mg/mL (404.15 mM)
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| 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.
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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