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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] .
L-161982 is a selective EP4receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .
17-Phenyl-ω-trinor-PGE2 is a PGE2 (HY-101952) analog, which is an agonist for EP1 and EP3receptor. 17-Phenyl-ω-trinor-PGE2 inhibits the PAF-induced aggregation of human platelet-rich plasma (PRP) and Cicaprost (HY-19583) induced Cyclic AMP (HY-B1511) production .
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.
9-keto Fluprostenol is an analog of prostaglandin E2 (PGE2) with structural modifications intended to give it a prolonged half-life and greater potency. Fluprostenol is a well-studied, potent analog of PGF2α and acts primarily through the FP receptor. Oxidation at C-9 of fluprostenol yields 9-keto fluprostenol. It is anticipated that this analog will have strong affinity for EP receptors and act as a PGE2 agonist.
11-Deoxy-16,16-dimethyl-PGE2, a Prostaglandin E2 analog, is a EP2 and EP3 receptors agonist. 11-Deoxy-16,16-dimethyl-PGE2 protects proximal renal tubular epithelial cells from potent nephrotoxicity-induced cell damage by exerting anti-oxidative stress .
EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC50 of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats .
ER-819762 is an orally active, highly selective prostaglandin E2(PGE2)EP4receptor antagonist with an EC50 of 70 nM against human EP4receptor. ER-819762 can be used for rheumatoid arthritis research .
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC50 of 38 nM for hLPA5. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia .
Sulprostone (SHB 286) is a potent and selective EP3 receptor agonist. Sulprostone (SHB 286) is a prostaglandin E2 (PGE2) analogue and has antiulcer and nonsteroidal abortifacient effects. Sulprostone has potential for the research of pregnancy termination and hemorrhages during delivery .
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) .
19(R)-hydroxy Prostaglandin E2 (19(R)-hydroxy PGE2) is found in the semen of primates, including man. It is a potent smooth muscle relaxant and a selective agonist for the EP2 receptor. It has an EC50 value of 200 nM for relaxing cat tracheal rings which express EP2 receptors.
Nocloprost, a prostaglandin E2 (PGE2) analog, is an orally active EP1- and EP3-receptor agonist. Nocloprost inhibits evoked [ 3H]ACh release. Nocloprost has gastroprotective and ulcer-healing properties. Nocloprost accelerates the healing of chronic gastric ulcerations and enhances mucosal growth in rats .
Vorbipiprant (CR6086) is an EP4receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases .
DG-041 is a potent, high affinity and selective EP3receptor 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 .
Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
(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 .
Dienogest (Standard) is the analytical standard of Dienogest. This product is intended for research and analytical applications. Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
(R)-Butaprost (free acid). Butaprost is a structural analog of prostaglandin E2 (PGE2) with good selectivity for the EP2 receptor subtype. Butaprost is frequently used pharmacologically to define the expression profile of EP receptors in various human and animal tissues and cells. Gardiner caused serious confusion about the structure of butaprost in 1986 when he reported that the epimer of butaprost showing this selective activity was the C-16 (R)-epimer ( See reference 2 and notes). To increase the binding affinity of (R)-butaprost to prostaglandin receptors, we removed the methyl ester of (R)-butaprost and recreated the native C-1 carboxylic acid. Prostaglandin free acids typically bind their cognate receptors with 10 to 100-fold higher affinity than the corresponding ester derivatives. The pharmacology of (R)-butaprost has not been carefully studied, but it is generally considered to be the less active C-16 epimer. (Note: In the 1986 Gardiner paper in the British Journal of Pharmacology, butaprost appears on page 46 under the designation TR 4979. The structure drawn is incorrect because the authors use and refer to the more active C - The 16 epimer, which is actually 16(S). The structure on page 46 shows the structure as 16(R). It was not until the late 1990s that careful studies in the United States and Japan correctly determined the actual structure of C-16 The type is 16(S) in a compound called butaprost.)
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .
Dienogest-13C,15N,d4 (STS 557-13C,15N,d4) is the 13C, 15N and deuterium labeled isotope of Dienogest (HY-B0084). Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE2 synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia .
Prostaglandin E Receptor EP2 Antibody (YA3342) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3342), targeting Prostaglandin E Receptor EP2, with a predicted molecular weight of 40 kDa (observed band size: 52 kDa). Prostaglandin E Receptor EP2 Antibody (YA3342) can be used for WB, IHC-P, ICC/IF, FC experiment in human, mouse, rat, cow background.
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