PGE2 receptor

By Targets:	Biochemical Assay Reagents (1) Estrogen Receptor/ERR (1) LPL Receptor (1) Progesterone Receptor (1) Prostaglandin Receptor (13)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Endocrinology (6) Inflammation/Immunology (5) Metabolic Disease (4) Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-N7748A

Epi-cryptoacetalide	Estrogen Receptor/ERR Prostaglandin Receptor	Inflammation/Immunology Endocrinology
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with K_i values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .

HY-128039

17-Phenyl-ω-trinor-PGE2	Prostaglandin Receptor	Others
17-Phenyl-ω-trinor-PGE2 is a PGE2 (HY-101952) analog, which is an agonist for EP1 and EP3 receptor. 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 .

HY-136696

11-Deoxy-16,16-dimethyl-PGE2	Prostaglandin Receptor	Metabolic Disease
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 .

HY-157495

EP3 antagonist 6	Prostaglandin Receptor	Endocrinology
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 .

HY-108562

SC-51322	Prostaglandin Receptor	Neurological Disease
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-108559

L-161982	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-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-114379

AS2717638 1 Publications Verification	LPL Receptor	Inflammation/Immunology
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-, PGF_2α-, and AMPA-induced allodynia .

HY-19360

Sulprostone SHB 286; CP-34089; ZK-57671
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 .

HY-138868

17-Phenyl trinor prostaglandin E2 ethyl amide 17-Phenyl trinor PGE2 ethyl amide	Prostaglandin Receptor	Metabolic Disease
17-Phenyl trinor prostaglandin E2 ethyl amide (17-Phenyl trinor PGE2 ethyl amide) is a EP1 receptor agonist. 17-Phenyl trinor prostaglandin E2 ethyl amide aggravates renal dysfunction and glomerulosclerosis .

HY-153129

EP2 receptor antagonist-2	Prostaglandin Receptor	Endocrinology
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-106054

Nocloprost	Prostaglandin Receptor	Metabolic Disease Inflammation/Immunology
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 .

HY-156649

Vorbipiprant CR6086	Prostaglandin Receptor	Endocrinology
Vorbipiprant (CR6086) is an EP4 receptor 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 .

HY-10835

DG-041 2 Publications Verification	Prostaglandin Receptor	Cardiovascular Disease
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-B0084

Dienogest 1 Publications Verification STS 557	Progesterone Receptor	Endocrinology
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 .

HY-120973

Butaprost free acid	Biochemical Assay Reagents	Others
(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.)

Cat. No.	Product Name	Type

HY-120973

Butaprost free acid	Biochemical Assay Reagents
(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.)

Butaprost free acid

Biochemical Assay Reagents

(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.)

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N7748A

Epi-cryptoacetalide	Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Estrogen Receptor/ERR Prostaglandin Receptor
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals high affinity to ER-α and PGE2 receptor (EP2 subtype) with K_i values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .

Cat. No.	Product Name	Application	Reactivity

HY-P83597

Prostaglandin E Receptor EP2 Antibody (YA3342) EP2; PGE2 receptor EP2 subtype; Prostaglandin E receptor 2 subtype EP2 53kDa; Prostaglandin E2 receptor EP2 subtype; Prostanoid EP2 receptor; Ptger2	WB, IHC-P, ICC/IF, FC	Human, Mouse, Rat, Cow

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PGE2 receptor

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