| Bioactivity | EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors[1]. | |||||||||
| Target | IC50: 6.1 nM (human EP4 receptor), 16.2 nM (mouse EP4 receptor) | |||||||||
| Invitro | The antagonistic effect of EP4 receptor antagonist 1 (Compounds 59) on human EP4 in calcium flux assay with an IC50 of 6.1±0.2 nM in CHO-Gα16 cells overexpressing human EP4 receptor. The antagonistic effect of EP4 receptor antagonist 1 on human EP4 in calcium flux assay with an IC50 of 16.2±1.7 nM in CHO-Gα16 cells overexpressing mouse EP4 receptor[1].EP4 receptor antagonist 1 dose dependently inhibits PGE2-stimulated cAMP accumulation in HEK293-EP4 cells with an IC50 of 18.7±0.6 nM. EP4 receptor antagonist 1 dose-dependently inhibits the activity of the CRE reporter in HEK293 cells with an IC50 of 5.2±0.4 nM.EP4 receptor antagonist 1 dose-dependently inhibits PGE2-stimulated β-arrestin recruitment in HEK293-EP4 cells with an IC50 of 0.4±0.1 nM[1].EP4 receptor antagonist 1 (1 nM-10 μM) reverses PGE2-induced ERK phosphorylation in a concentration-dependent manner[1]. Western Blot Analysis[1] Cell Line: | |||||||||
| In Vivo | EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; orally; once daily for two weeks) causes significant inhibition of tumor growth in BALB/c female mice. No significant body weight loss is found in any mouse cohorts. EP4 receptor antagonist 1 is well tolerated in mice at the tested dosage[1].EP4 receptor antagonist 1 (1 mg/kg; intravenously) demonstrates moderate clearance (CL=1.7 L/h/kg) in mice with a corresponding favorable half-life (t1/2) of 4.1 h. EP4 receptor antagonist 1 (5 mg/kg; orally) exhibits good bioavailability (F=48.0%) in mice with a corresponding favorable half-life (t1/2) of 4.7 h[1]. Animal Model: | |||||||||
| Name | EP4 receptor antagonist 1 | |||||||||
| CAS | 2287259-07-6 | |||||||||
| Formula | C23H21F3N4O3 | |||||||||
| Molar Mass | 458.43 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Yang JJ, et al. Discovery and Characterization of 1H-1,2,3-Triazole Derivatives as Novel Prostanoid EP4 Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2020 Jan 23;63(2):569-590. |
EP4 receptor antagonist 1
CAS: 2287259-07-6 F: C23H21F3N4O3 W: 458.43
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer imm
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