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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
human EP4 receptors
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "human EP4 receptors" in MCE Product Catalog:
9
9 Publications Verification
Cat. No.: HY-16963
CAS No.: 439288-66-1
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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 .
9
9 Publications Verification
Cat. No.: HY-16978
CAS No.: 1415716-58-3
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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 .
4
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Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors .
3
3 Cited Publications
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KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor .
2
2 Cited Publications
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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 .
Synonyms: CR6086
Research Areas:
Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (Ki: 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 .
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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 .
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AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis 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
.
Cat. No.: HY-178465
CAS No.: 3068255-86-4
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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 .
Cat. No.: HY-116099
CAS No.: 1155773-15-1
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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 .
Cat. No.: HY-150068
CAS No.: 691869-12-2
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EP4 receptor agonist 1 (compound 11) is an EP4 receptor agonist with the human pEC50 value of 6.3 .
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ASP7657 free base is an orally active EP4 receptor antagonist, with Kis of 2.21 and 6.02 nM for the human and rat EP4 receptors .
Cat. No.: HY-163651
CAS No.: 2502965-92-4
Synonyms: (R)-CR6086
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(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 .
Cat. No.: HY-182969
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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) .
Cat. No.: HY-114822
CAS No.: 36614-31-0
Synonyms: PGA3
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Prostaglandin A3 is a non-enzymatic dehydration product of prostaglandin E3 (PGE3). Prostaglandin A3 showed good affinity for canine EP2 and EP4 receptors with IC50 values of 120 and 20 nM, respectively. The Ki value of Prostaglandin A3 for human PPARγ was 188 μM .
Cat. No.: HY-119236
CAS No.: 431990-08-8
Synonyms: CP-734432
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CP-432 (CP-734432) is a EP4 receptor agonist with an IC50 of 2 nM for human sources, 8 nM for canine sources, and an EC50 of 1 nM for human sources. CP-432 stimulates cAMP production and activates β-lactamase (β-lactamase) activity via the cAMP response element signaling pathway. CP-432 is applicable to research related to glaucoma .
Cat. No.: HY-185643
CAS No.: 1201925-19-0
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PF-04475270 is a prodrug of CP-734432 (HY-119236), as well as an agonist of the EP4 prostaglandin receptor, with IC50 values of 2 nM and 8 nM against human and canine sources, respectively. PF-04475270 is rapidly hydrolyzed into its active metabolite CP-734432 by ocular esterases or corneal homogenate, stimulates cAMP production, and activates cAMP response element-mediated β-lactamase activity in cells expressing EP4. PF-04475270 can be used in research related to glaucoma .
Cat. No.: HY-111539R
CAS No.: 1613264-40-6
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BAY-1316957 (Standard) is the analytical standard of BAY-1316957 (HY-111539). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-183037
CAS No.: 1354060-46-0
Research Areas:
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 .
Cat. No.: HY-189067
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IP/EP4 receptor agonist-1 is a PGI2 analog and also an IP/EP4 receptor agonist. IP/EP4 receptor agonist-1 inhibits PAR-mediated integrin αIIbβ3 activation, P-selectin exposure, platelet aggregation and thrombus formation. IP/EP4 receptor agonist-1 can be used in research related to pulmonary hypertension .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
