Evatanepag
Based on 2 publication(s) in Google Scholar
Evatanepag (CP-533536) is a non-prostanoid, potent and selective EP2 receptor agonist. Evatanepag can induce local bone formation in vivo. Evatanepag can be used in the research of fractures, bone defects, asthma.
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- Reinheit: 98.58%
- CAS. Nr.: 223488-57-1
- Formel: C25H28N2O5S
- Molecular Weight:468.57
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Publications Citing Use of MedChemExpress (MCE) Evatanepag
More
Biologische Aktivität
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EP2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.3 nM
Compound: 7f, CP-533536
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Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
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[PMID: 19250823] |
| HEK293 | IC50 |
>3200 nM
Compound: 7f, CP-533536
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Inhibition of rat EP4 receptor expressed in HEK293 cells
Inhibition of rat EP4 receptor expressed in HEK293 cells
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[PMID: 19250823] |
| HEK293 | IC50 |
50 nM
Compound: 7f, CP-533536
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Inhibition of rat EP2 receptor expressed in HEK293 cells
Inhibition of rat EP2 receptor expressed in HEK293 cells
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[PMID: 19250823] |
Evatanepag (10 nM, 30 min) inhibits hFcεRI-induced mast cells degranulation in a dose-dependent manner[2].
Evatanepag (0.1 nM-10 μM, 12 min) results in an equivalent increase in intracellular cAMP in HEK-293 cells, with an IC50 of 50 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Evatanepag (0.3, 3.0 mg/kg, intranasal administration, from day1 to day4) reduces HDM aeroallergen-induced increased RL response to methacholine in mice[2].
Evatanepag (1 mg/kg, intravenous injection) demonstrates high i.v. clearance (Cl: 56 mL/min/kg) and a short half-life (t1/2: 0.33 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:0.3, 1.0, 3.0 mg/kg
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Administration:Directly injected into the marrow cavity of the tibia
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Result:Dose-dependently increased in bone area, bone mineral content, bone mineral density.
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Animal Model:HDM (house dust mite)-sensitized BALB/c mice[2]
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Dosage:0.3 mg/kg, 3 mg/kg
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Administration:Intranasal administration, from day1 to day4
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Result:Prevented aeroallergen-driven increased RL (lung resistance) at 0.3 mg/kg.
Prevented the enhanced MC activity by approximately 48% at 3 mg/kg.
Chemical Information
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CAS. Nr. 223488-57-1
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Appearance Solid
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Molecular Weight 468.57
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Formel C25H28N2O5S
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Color White to off-white
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SMILES
CC(C)(C)C(C=C1)=CC=C1CN(S(C2=CN=CC=C2)(=O)=O)CC3=CC(OCC(O)=O)=CC=C3
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Synonyms
CP-533536 free acid
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Adv
Ligand recognition, unconventional activation, and G protein coupling of the prostaglandin E2 receptor EP2 subtype. [Abstract]2021 Apr 2;7(14):eabf1268. PMID: 33811074 -
PLoS One
Impact of Bone Morphogenetic Protein 7 and Prostaglandin receptors on osteoblast healing and organization of collagen. [Abstract]2024 May 16;19(5):e0303202. PMID: 38753641
Lösungsmittel & Löslichkeit
DMSO : ≥ 32 mg/mL (68.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Cameron KO, et al. Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8. [Content Brief]
[2]. Judith Plaza, et al. In Vitro and In Vivo Validation of EP2-Receptor Agonism to Selectively Achieve Inhibition of Mast Cell Activity. Allergy Asthma Immunol Res. 2020 Jul;12(4):712-728. [Content Brief]
[3]. V M Paralkar, et al. An EP2 receptor-selective prostaglandin E2 agonist induces bone healing. Proc Natl Acad Sci U S A. 2003 May 27;100(11):6736-40. [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 | 2.1342 mL | 10.6708 mL | 21.3415 mL | 53.3538 mL |
| 5 mM | 0.4268 mL | 2.1342 mL | 4.2683 mL | 10.6708 mL | |
| 10 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL | 5.3354 mL | |
| 15 mM | 0.1423 mL | 0.7114 mL | 1.4228 mL | 3.5569 mL | |
| 20 mM | 0.1067 mL | 0.5335 mL | 1.0671 mL | 2.6677 mL | |
| 25 mM | 0.0854 mL | 0.4268 mL | 0.8537 mL | 2.1342 mL | |
| 30 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7785 mL | |
| 40 mM | 0.0534 mL | 0.2668 mL | 0.5335 mL | 1.3338 mL | |
| 50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0671 mL | |
| 60 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL |
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