Omidenepag
Based on 1 publication(s) in Google Scholar
Omidenepag (UR-7276), a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC50 of 1.1 nM. Omidenepag shows binding affinities (IC50) 10 nM for h-EP2. Omidenepag is used in research on diseases related to intraocular pressure.
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- Pureza : 99.86%
- No. CAS: 1187451-41-7
- Fòrmula: C23H22N6O4S
- Peso molecular:478.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-111406
Omidenepag isopropylEP2 Receptor Agonist -
HY-B0584
TravoprostFP Prostaglandin Receptor Agonist -
HY-B0600
TafluprostProstaglandin Receptor Agonist -
HY-108560
(+)-FluprostenolPTGER2 Agonist -
HY-B0584R
Travoprost (Standard) -
HY-B0600R
Tafluprost (Standard)Prostaglandin Receptor Agonist -
HY-108560R
(+)-Fluprostenol (Standard)PTGER2 Agonist
Publications Citing Use of MedChemExpress (MCE) Omidenepag
More
Actividad biológica
Descripciòn
IC50 & Target
[1]|
hEP4 5480 nM (IC50) |
hEP2 10 nM (IC50) |
hEP2 1.1 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1.1 nM
Compound: 13ax; OMD
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Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
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[PMID: 29995405] |
| HEK293 | IC50 |
10 nM
Compound: 13ax; OMD
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Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
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[PMID: 29995405] |
In Vitro
Omidenepag (3-30 μM) significantly inhibits Carbachol (HY-B1208)-induced porcine ciliary muscle (CM) contraction[2].
Omidenepag (10-100 nM; 24 h) significantly inhibits TGF-β2-induced mRNA upregulation of αSMA, COL1A1 and FN in HTM cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1187451-41-7
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Appearance Solid
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Peso molecular 478.52
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Fòrmula C23H22N6O4S
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Color White to off-white
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SMILES
O=C(O)CNC1=NC(CN(CC2=CC=C(N3N=CC=C3)C=C2)S(=O)(C4=CC=CN=C4)=O)=CC=C1
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Synonyms
UR-7276
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Korean J Ophthalmol
Effect of Prostaglandin E2 Agonist Omidenepag on the Expression of Matrix Metalloproteinase in Trabecular Meshwork Cells. [Abstract]2022 Apr;36(2):123-130. PMID: 35067026
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (522.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Iwamura R, et al. Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl. J Med Chem. 2018 Aug 9;61(15):6869-6891. [Content Brief]
[2]. Nakamura N, et al. Effects of selective EP2 receptor agonist, omidenepag, on trabecular meshwork cells, Schlemm's canal endothelial cells and ciliary muscle contraction. Sci Rep. 2021 Aug 10;11(1):16257. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0898 mL | 10.4489 mL | 20.8978 mL | 52.2444 mL |
| 5 mM | 0.4180 mL | 2.0898 mL | 4.1796 mL | 10.4489 mL | |
| 10 mM | 0.2090 mL | 1.0449 mL | 2.0898 mL | 5.2244 mL | |
| 15 mM | 0.1393 mL | 0.6966 mL | 1.3932 mL | 3.4830 mL | |
| 20 mM | 0.1045 mL | 0.5224 mL | 1.0449 mL | 2.6122 mL | |
| 25 mM | 0.0836 mL | 0.4180 mL | 0.8359 mL | 2.0898 mL | |
| 30 mM | 0.0697 mL | 0.3483 mL | 0.6966 mL | 1.7415 mL | |
| 40 mM | 0.0522 mL | 0.2612 mL | 0.5224 mL | 1.3061 mL | |
| 50 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0449 mL | |
| 60 mM | 0.0348 mL | 0.1741 mL | 0.3483 mL | 0.8707 mL | |
| 80 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6531 mL | |
| 100 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5224 mL |
Omidenepag Related Classifications
HY-17642 Related Classifications
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