2. Signaling Pathways
  3. GPCR/G Protein
  4. Prostaglandin Receptor
  5. EP Isoform
  6. EP Antagonist

EP Antagonist

EP Antagonists (36):

Cat. No. Product Name Effect Purity
  • HY-18966
    PF-04418948
    		Antagonist 99.56%
    PF-04418948 is an orally active, potent and selective prostaglandin EP2 receptor antagonist with an IC50 of 16 nM.
  • HY-50901
    ONO-AE3-208
    		Antagonist 98.65%
    ONO-AE3-208 is a selective and orally active EP4 receptor antagonist with a Ki of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (Ki of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer.
  • HY-163651
    (R)-Vorbipiprant
    		Antagonist
    (R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with Ki of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC50 of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice.
  • HY-15274
    L-798106
    		Antagonist 99.81%
    L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has ?micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM, respectively.
  • HY-10835
    DG-041
    		Antagonist ≥99.0%
    DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier.
  • HY-16781
    Grapiprant
    		Antagonist 99.57%
    Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment[3] .
  • HY-16963
    GW627368
    		Antagonist 99.81%
    GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively.
  • HY-10797
    CJ-42794
    		Antagonist 98.84%
    CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers.
  • HY-115487
    MF-766
    		Antagonist 99.69%
    MF-766 is a highly potent, selective and orally active EP4 antagonist with a Ki of 0.23 nM. MF-766 behaves as a full antagonist with an IC50 of 1.4 nM (shifted to 1.8 nM in the presence of 10% HS) in the functional assay. MF-766 can be used for cancer and inflammation diseases research.
  • HY-10794
    MF498
    		Antagonist 99.26%
    MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a Ki value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis.
  • HY-18971
    TG4-155
    		Antagonist 99.91%
    TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a Ki of 9.9 nM. TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1. TG4-155 has an EP2 Schild KB of 2.4 nM and displays 550-4750-fold selectivity for EP2 over EP1, EP3, EP4 and IP, but only 14-fold selectivity against the DP1 receptor.
  • HY-153129
    EP2 receptor antagonist-2
    		Antagonist 98.69%
    EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA).
  • HY-108562
    SC-51322
    		Antagonist 98.90%
    SC-51322 is a potent and selective antagonist of prostaglandin E2 (PGE2) receptor (EP 1), with a pA2 of 8.1. SC-51322 has the pain-relieving effect.
  • HY-108563A
    SC 51089 free base
    		Antagonist 98.64%
    SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with Kis of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.
  • HY-147226
    EP3 antagonist 3
    		Antagonist 99.57%
    EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research.
  • HY-19361
    L-826266
    		Antagonist ≥98.0%
    L-826266 is a selective and competitive EP3 receptor antagonist. L-826266 can be used for convulsive disorders research.
  • HY-16635
    Setipiprant
    		Antagonist 98.23%
    Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.
  • HY-15853
    MK-7246
    		Antagonist 99.63%
    MK-7246 is a potent and selective CRTH2 antagonist with a Ki of 2.5±0.5 nM.
  • HY-102065
    SC-19220
    		Antagonist 99.71%
    SC-19220 is a competitive prostaglandinn E2 receptor antagonist. SC-19220 increases the bladder capacity and reduced the voiding efficiency of micturition (elicited by slow transvesical filling) of urethane-anesthetized rats. SC-19220 can restores the balance in bone marrow granulocyte and monocyte production after burn sepsis.
  • HY-111539
    BAY-1316957
    		Antagonist 99.73%
    BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research.