EP4 receptor agonist-4
EP4 receptor agonist-4 is an orally active, selective EP4 receptor agonist, with a binding IC50 of 18 nM against human receptors, and agonistic EC50 values of 2.1 nM and 0.11 μM against human and murine receptors, respectively. EP4 receptor agonist-4 inhibits hERG channel activity with an IC50 of 10.2 μM. It can be used in the research of inflammatory bowel disease (colitis).
For research use only. We do not sell to patients.
- Formula: C22H26F3N5O3
- Molecular Weight:465.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EP4 receptor agonist-4 (Compound 11a) inhibits LPS (HY-D1056)-induced TNFα release in human whole blood, with an IC50 of 0.039 μM[1].
EP4 receptor agonist-4 inhibits LPS-induced TNFα release in mouse whole blood, with an IC50 of 0.42 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | CL | Vss | T1/2 | MRT |
|---|---|---|---|---|---|---|---|
| Mice[1] | 3 mg/kg | i.v. | 19800 nM·h | 5.4 mL/min/kg | 1.4 L/kg | 5.1 h | 4.4 h |
EP4 receptor agonist-4 (15-50 mg/kg; p.o.; single administration) induces target-related hemodynamic changes (decreased mean arterial pressure, increased heart rate) in conscious male mice, and systemic exposure saturates EP4 pathway signaling at both tested doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male (telemetry study); unspecified strain (DSS-induced colitis model)[1]
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Dosage:15 mg/kg; 50 mg/kg
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Administration:p.o.; daily for 10 days
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Result:Attenuated bodyweight loss in DSS-treated mice at 15 and 50 mg/kg.
Reduced colon shortening by 78% compared to vehicle at 50 mg/kg.
Reduced circulating FITC-dextran concentrations, protected the epithelial barrier, and lowered serum TNFα and IL-17A levels (IL-17A reduced by 108% compared to vehicle) at 50 mg/kg.
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Animal Model:male (telemetry study)[1]
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Dosage:15 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Induced a maximum decrease in mean arterial pressure of ~9-12 mmHg (~9-12%) that lasted approximately 20 hours postdose at 15 and 50 mg/kg.
Induced a maximum increase in heart rate of ~150-160 bpm (~21-23%) that lasted approximately 8 hours postdose at 15 and 50 mg/kg.
Left locomotor activity unaffected at 15 and 50 mg/kg.
Reached a mean maximum whole blood concentration of 11.81 μM at 1 hour for the 15 mg/kg dose, and 49.02 μM at 1 hour for the 50 mg/kg dose.
Chemical Information
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Molecular Weight 465.47
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Formula C22H26F3N5O3
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SMILES
O=C(O)CCC(N1CCN(C2=NC(C(F)(F)F)=CC(N[C@H](C3=CC=CC=C3)C)=N2)[C@@H](C1)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EP4 receptor agonist-4 Related Classifications
HY-182969 Related Classifications
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