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EP4 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Interleukin Related (4) Isotope-Labeled Compounds (1) MMP (1) PD-1/PD-L1 (1) Prostaglandin Receptor (33) Reference Standards (3)
By Research Areas:	Cancer (16) Cardiovascular Disease (1) Endocrinology (12) Inflammation/Immunology (21) Metabolic Disease (6) Neurological Disease (6)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-136645

EP4 receptor antagonist 2	Prostaglandin Receptor	Cancer
EP4 receptor antagonist 2 (Compound 8) is a tricyclic spiro-based *EP₄* receptor antagonist with microsomal stability .

HY-16781

Grapiprant 4 Publications Verification CJ-023423; RQ-00000007; AAT-007	Prostaglandin Receptor	Metabolic Disease Endocrinology Cancer
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 K_i** value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment ^[3].

HY-50901

ONO-AE3-208 Maximum Cited Publications 12 Publications Verification AE 3-208	Prostaglandin Receptor	Endocrinology Cancer
ONO-AE3-208 is a selective and orally active **EP4 receptor** antagonist with a K_i of 1.3 nM. ONO-AE3-208 shows less potently affects EP3, FP, and TP receptors (K_i of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 suppresses cell invasion, migration, and metastasis of prostate cancer .

HY-16963

GW627368 5+ Cited Publications	Prostaglandin Receptor	Inflammation/Immunology Endocrinology Cancer
GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid *EP4* receptor with additional human TP receptor affinity, with pK_i values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively .

HY-133123

EP4 receptor antagonist 1 2 Publications Verification	Prostaglandin Receptor	Inflammation/Immunology Cancer
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 .

HY-16978

TG6-10-1 5+ Cited Publications	5-HT Receptor Prostaglandin Receptor	Neurological Disease Endocrinology
TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors .

HY-15274

L-798106 1 Publications Verification CM9; GW671021	Prostaglandin Receptor	Cancer
L-798106 is potent and highly selective prostanoid EP₃ receptor antagonist (K_i=0.3 nM), it also has micromolar activities at the EP₄, EP₁ and EP₂ receptors with K_i values of 916 nM, >5000 nM and >5000 nM, respectively .

HY-108559

L-161982 1 Publications Verification	Prostaglandin Receptor	Inflammation/Immunology
L-161982 is a selective *EP4* receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .

HY-156649

Vorbipiprant CR6086	Prostaglandin Receptor Interleukin Related MMP PD-1/PD-L1	Cardiovascular Disease Inflammation/Immunology Cancer
Vorbipiprant (CR6086) is an orally active *EP4* receptor antagonist with high selectivity for the human *EP4* receptor (K_i: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer .

HY-10797

CJ-42794 4 Publications Verification CJ-042794	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
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-18971

TG4-155 1 Publications Verification	Prostaglandin Receptor	Neurological Disease Inflammation/Immunology Endocrinology Cancer
TG4-155 is a potent, brain-permeant and selective EP2 receptor antagonist with a K_i of 9.9 nM . TG4-155 shows low nanomolar antagonist activity against only EP2 and DP1 . TG4-155 has an EP2 Schild K_B 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-10413

MK-2894 2 Publications Verification	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
MK-2894 is a potent, selective, orally active and high affinity (K_i=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC₅₀=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .

HY-169859

EP4 receptor antagonist 7	Prostaglandin Receptor Interleukin Related	Inflammation/Immunology Cancer
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC₅₀ value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC₅₀ value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD ⁸⁺ T cells into tumors in a CT26 murine colon cancer model .

HY-178465

EP4 receptor antagonist 8	Prostaglandin Receptor Interleukin Related	Neurological Disease Inflammation/Immunology
EP4 receptor antagonist 8 is an orally active *EP4* antagonist (human EP4 IC₅₀ = 6.40 nM). EP4 receptor antagonist 8 significantly reduced paw and joint swelling, inflammatory cell infiltration, cartilage damage, pannus formation, and joint bone erosion in arthritis (AIA) mice in a dose-dependent manner. EP4 receptor antagonist 8 can be used for the study of inflammatory pain .

HY-111539

BAY-1316957	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
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 .

HY-122168

AAT-008	Prostaglandin Receptor	Inflammation/Immunology Cancer
AAT-008 is a potent, selective, and orally active prostaglandin **EP4 receptor** antagonist with K_is of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer .

HY-10794

MF498 1 Publications Verification	Prostaglandin Receptor	Metabolic Disease Inflammation/Immunology Cancer
MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a K_i value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis .

HY-163091

EP4 receptor antagonist 5	Prostaglandin Receptor	Inflammation/Immunology
EP4 receptor antagonist 5 is a potent and selective prostanoid EP4 receptor antagonist that can reduce inflammation Freund’s adjuvant (CFA) model .

HY-116099

ER-819762	Prostaglandin Receptor	Inflammation/Immunology
ER-819762 is an orally active, highly selective prostaglandin E₂ (PGE₂) **EP₄ receptor** antagonist with an EC₅₀ of 70 nM against human EP₄ receptor. ER-819762 can be used for rheumatoid arthritis research .

HY-10414

MK-2894 sodium salt	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
MK-2894 sodium salt is a potent, selective, orally active and high affinity (K_i=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC₅₀=2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .

HY-120598

ASP7657 free base	Prostaglandin Receptor	Metabolic Disease Inflammation/Immunology
ASP7657 free base is an orally active **EP4 receptor** antagonist, with K_is of 2.21 and 6.02 nM for the human and rat EP4 receptors .

HY-163651

(R)-Vorbipiprant (R)-CR6086	Prostaglandin Receptor	Inflammation/Immunology
(R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with K_i 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-16781R

Grapiprant (Standard) CJ-023423 (Standard); RQ-00000007 (Standard); AAT-007 (Standard)	Prostaglandin Receptor Reference Standards	Metabolic Disease Endocrinology Cancer
Grapiprant (Standard) is the analytical standard of Grapiprant. This product is intended for research and analytical applications. 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 .

HY-110351

BGC-20-1531 hydrochloride PGN 1531 hydrochloride	Prostaglandin Receptor	Neurological Disease
BGC 20-1531 (PGN 1531) hydrochloride is a potent and selective prostanoid EP₄ receptor antagonist, with a pK_b of 7.6. BGC 20-1531 hydrochloride has the potential for the research of migraine headache .

HY-19849

BGC-20-1531 free base PGN 1531 free base	Prostaglandin Receptor	Neurological Disease
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP₄ receptor antagonist, with a pK_B of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache .

HY-50901A

ONO-AE3-208 sodium salt AE 3-208 sodium salt	Prostaglandin Receptor	Endocrinology Cancer
ONO-AE3-208 (sodium salt) is a selective and orally active **EP4 receptor** antagonist with a K_i of 1.3 nM. ONO-AE3-208 (sodium salt) shows less potently affects EP3, FP, and TP receptors (K_i of 30 nM, 790 nM, and 2400 nM, respectively). ONO-AE3-208 (sodium salt) suppresses cell invasion, migration, and metastasis of prostate cancer .

HY-108559R

L-161982 (Standard)	Prostaglandin Receptor	Inflammation/Immunology
L-161982 (Standard) is the analytical standard of L-161982. This product is intended for research and analytical applications. L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .

HY-115827

AH22921	Prostaglandin Receptor	Others
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.

HY-183845

HTL0039732	Prostaglandin Receptor	Cancer
HTL0039732 is an orally active antagonist of the prostaglandin EP4 receptor (Prostaglandin E2 Receptor EP4). HTL0039732 reverses PGE₂-induced differentiation toward M2-like macrophages. HTL0039732 exhibits efficacy in syngeneic tumor models and acts synergistically with PD-1/PD-L1 pathway blockers. HTL0039732 can be used for the research of advanced solid tumors .

HY-16781S

Grapiprant-d4 CJ-023423-d₄; RQ-00000007-d₄; AAT-007-d₄	Isotope-Labeled Compounds Prostaglandin Receptor	Metabolic Disease Cancer
Grapiprant-d₄ (CJ-023423-d₄) is the deuterium labeled Grapiprant (HY-16781). 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 K_i** value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment ^[3].

HY-10794R

MF498 (Standard)	Reference Standards Prostaglandin Receptor	Metabolic Disease Inflammation/Immunology Cancer
MF498 (Standard) is the analytical standard of MF498 (HY-10794). This product is intended for research and analytical applications. MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a K_i value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis .

HY-183037

AGN 225660	Prostaglandin Receptor Interleukin Related	Neurological Disease Inflammation/Immunology
AGN 225660 is a multi-prostanoid receptor antagonist with human IC₅₀ values of 70, 70, 5, 220 and 180 nM for EP1, *EP4, TP, DP1, FP. AGN 225660 inhibits secretion of RANTES, IL-8, MCP-1, IL-12p70, and IL-23*. AGN 225660 exhibits good ocular bioavailability and reduces ocular inflammation linked to phacoemulsification surgery and uveitis .

HY-10797R

CJ-42794 (Standard) CJ-042794 (Standard)	Reference Standards Prostaglandin Receptor	Inflammation/Immunology Endocrinology
CJ-42794 (Standard) is the analytical standard of CJ-42794 (HY-10797). This product is intended for research and analytical applications. 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 .

Cat. No.	Product Name	Chemical Structure

HY-16781S

Grapiprant-d4
Grapiprant-d₄ (CJ-023423-d₄) is the deuterium labeled Grapiprant (HY-16781). 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 K_i** value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment ^[3].

Grapiprant-d4

Grapiprant-d₄ (CJ-023423-d₄) is the deuterium labeled Grapiprant (HY-16781). 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 K_i value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment ^[3].

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