Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as the primary receptors for one or more of the classical, naturally occurring prostanoids viz., prostaglandin D2, , PGE2, PGF2alpha, prostacyclin (PGI2), thromboxane A2 (TXA2), and PGH2.[1] They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well.

Filter HomeSignaling PathwaysImmunology/Inflammation-GPCR/G ProteinProstaglandin Receptor

Cis-N-Feruloyltyramine

TN366980510-09-4In house

Cis-N-Feruloyltyramine is a naturally occurring compound found in various plants that shows cytotoxicity against the P-388 cancer cell line. Cis-N-Feruloyltyramine is an inhibitor of in vitro prostaglandin (PG) synthesis.

$137

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Aligeron

T3661970713-45-0In house

Aligeron, a non-selective prostaglandin (PG) antagonist, inhibits PGF2α- and PGE2-induced blood pressure decreases in cats and can prevent PGF2α-induced diarrhea in mice and PGE2-induced paw edema in rats. Additionally, Aligeron is recognized for its antioxidant-protective effect against vascular complications.

$700

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Prostaglandin E1

T1626745-65-3

Prostaglandin E1 (Alprostadil) is the naturally occurring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Prostaglandin E1 is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

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sphondin

T5758483-66-9

Sphondin has anticonvulsant, anti-inflammatory, and anti-proliferative activities, it possessed an inhibitory effect on IL-1beta-induced increase in the level of COX-2 protein and PGE(2) release in A549 cells.

$113

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NTP42

T122682055599-51-2

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

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TP-16

T625252332972-26-4In house

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

$462

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Laropiprant

T15712571170-77-9

Laropiprant (MK-0524) is a potent and selective antagonist of prostaglandin D2 (PGD2) receptor (DP) such as and DP DP1 receptor(Ki = 0.57 nM) and TP Receptor(Ki = 2.95 nM).

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Platycodin D

T388958479-68-8

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10 30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

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L-161982

T15681147776-06-5In house

L-161982 is a selective EP4 receptor antagonist that inhibits PGE2-induced ERK phosphorylation and cell proliferation in HCA-7 cells and alleviates collagen-induced arthritis in mice.

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Rutin

T0795153-18-4

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

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Taraxasterol

T37701059-14-9

Taraxasterol (Taraxasterin) is compound with anti-inflammatory activity.

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Tiopinac

T1710161220-69-7In house

Tiopinac (RS 40974) has anti-inflammatory and analgesic activity, and exhibits anti-flammatory activity in adrenalectomized rats.

$208

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Furprofen

T1134066318-17-0In house

Furprofen is a non-steroidal anti-inflammatory agent that inhibits prostate (PGE) synthesis and is used in the study of rheumatoid arthritis and osteoarthritis.

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mPGES-1 Inhibitor-1

T280891381846-21-4In house

mPGES-1 Inhibitor-1 is a novel selective inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with anti-inflammatory and analgesic activity for the study of acute liver injury.

$196

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ONO-8713

T63667459411-08-6In house

ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist used to study diseases of the biblical system and metabolism-related diseases.

$397

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RO1138452

T4436221529-58-4

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

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Octimibate

T2456789838-96-0In house

Octimibate (Octimibato) is a non-prostaglandin platelet aggregation inhibitor and cyclic prostaglandin agonist.Octimibate is used in the treatment of cardiovascular disease and can be used to study atherosclerosis and thrombosis.

$143

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DG-041

T15108861238-35-9

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

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Ginsenoside Ro

T391534367-04-9

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

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RO3244794

T69360361457-01-4

RO3244794 is a selective prostacyclin (IP) receptor antagonist that can be used to study liver injury.

$293

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BAY-6672

T397602247517-53-7

BAY-6672 is a selective human prostaglandin F (FP) receptor antagonist that is highly potent (IC50=11 nM), orally available and well permeable. It exerts antifibrotic effects by inhibiting prostaglandin F2α (PGF₂α) activity through antagonizing the FP receptor, and has in vivo efficacy in animal models of idiopathic pulmonary fibrosis (IPF).

$196

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Gestonorone Capronate

T137031253-28-7

Gestonorone Capronate is a progesterone used to treat benign prostatic hyperplasia and endometrial cancer.

$148

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Latanoprost

T2528130209-82-4

Latanoprost (Xalatan) is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect.

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Beta-Hydroxyisovalerylshikonin

TN14407415-78-3

Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).

$139

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Bimatoprost

T2538155206-00-1

Bimatoprost (AGN 192024) is a cloprostenol-derived amide that is used as an antihypertensive agent in the treatment of open-angle glaucoma and ocular hypertension.

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Evodiamine

T2868518-17-2

Evodiamine (d-Evodiamine) is an alkaloid isolated from the fruit of daylily and has a variety of biological activities including anti-inflammatory, anti-obesity and anti-tumor.

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Treprostinil

T515081846-19-7

Treprostinil (Orenitram) is a potent DP1, IP and EP2 agonist (EC50: 0.6 1.9 6.2 nM).

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Agnuside

T386811027-63-7

Agnuside (chasteberry oil) inhibits COX-2 (IC50: 0.026 mg ml) but exhibits less than 10% inhibition of COX-1 at this concentration. It also inhibits 46.3, 66.8, and 82.1% of P-glycoprotein (P-gp) ATPase activity at concentrations of 5, 25, and 100 μM, respectively.

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Afzelin

TN1362482-39-3

Afzelin (Kaempferol-3-O-rhamnoside) exhibits several cellular activities such as DNA-protective, antibacterial, antioxidant, anti-inflammatory, and UV-absorbing properties, potentially protecting human skin from UVB-induced damage through a combination of UV-absorbing and cellular actions. Afzelin mitigates mitochondrial damage, promotes mitochondrial biogenesis, and reduces levels of mitophagy-related proteins, parkin and PTEN-induced putative kinase 1.

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Isbogrel

T2763089667-40-3In house

Isbogrel (CV4151) is a small molecule thromboxane A2 synthase (TXA2 synthase) inhibitor that can be used to study cardiac arrhythmias, transient ischemic attacks and thrombosis.

$350

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AMG-009

T142111027847-67-1

AMG-009 is a selective and potent dual antagonist of CRTH2 and DP, with an IC50 value of 3 nM for CRTH2 and 12 nM for DP receptors.

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Grapiprant

TQ0292415903-37-6

Grapiprant (AAT-007) is a selective EP4 receptor antagonist. Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor (IC50: 35 nM, Ki: 24 nM).

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Tranilast

T269053902-12-8

Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.

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Treprostinil diethanolamine

T63349830354-48-8

Treprostinil diethanolamine (UT-15C) is a potent agonist of EP2, DP1, and IP, with values of 3.6, 4.4, and 32.1 nM for EP2, DP1, and IP, respectively, and 212, 826, 2505, and 4680 nM for EP1, EP4, EP3, and FPKi, respectively. Treprostinil diethanolamine contributes to the upregulation of cAMP, maintaining vascular homeostasis and causing vasodilation in human pulmonary arteries.

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Rebamipide

T156290098-04-7

Rebamipide (OPC12759) is a quinolinone derivative with anti-ulcer and anti-inflammatory activities. Rebamipide induces cyclooxygenase 2 (COX2) synthesis which results in an increase in endogenous prostaglandin synthesis in the gastric mucosa. This agent also inhibits H. pylori-induced production of tumor necrosis factor (TNF) alpha and subsequent inflammation of the gastric mucosa. In addition, rebamipide scavenges oxygen-derived free radicals that potentially cause mucosal injury, and stimulates prostaglandin EP4 receptor gene expression followed by mucous secretion, thereby enhancing the gastric mucosal defense.

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Vidupiprant

T172321169483-24-2

Vidupiprant (AMG 853) is an effective dual antagonist of CRTH2 and prostanoid D receptor with IC50s of 8 nM and 35 nM in human plasma. Vidupiprant can be used in studies about the treatment of asthma.

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Darbufelone

T10960139226-28-1In house

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

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L-798106

T15689244101-02-8

L-798106 (CM9) is a selective and potent prostaglandin-like EP3 receptor antagonist that inhibits EP4, EP1, and EP2 receptors, suppresses levels of pro-inflammatory cytokines in atherosclerosis, and attenuates PGE2-induced cough.

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Embelin

T6485550-24-3

Embelin (Embelic acid), isolated from the Japanese Ardisia herb, is an inhibitor of the X-linked inhibitor of apoptosis (IC50: 4.1 uM).

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Travoprost

T5841157283-68-6

Travoprost (Fluprostenol isopropyl ester) is used to treat glaucoma and ocular hypertension,is a potent and selective FP prostaglandin receptor agonist.

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3-O-Acetyl-α-boswellic acid

TN125789913-60-0

3-O-Acetyl-α-boswellic acid (α-Boswellic acid acetate) exhibits potent anti-inflammatory activity.

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PGD2-IN-1

T4624885066-67-1In house

PGD2-IN-1 (PGD2-inhibitor) is an effective DP receptor antagonist (IC50:0.3 nM), a compound that can inhibit prostaglandin D2 (PGD2) signaling. PGD2-IN-1 specifically targets and regulates the activity of PGD2 receptors or enzymes involved IN PGD2 synthesis or metabolism.

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Selexipag

T3216475086-01-2

Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH).

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EP4 receptor antagonist 1

T112112287259-07-6

EP4 Receptor Antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist, effective for cancer immunotherapy. It inhibits both human and mouse EP4 receptors with IC50 values of 6.1 nM and 16.2 nM, respectively, while displaying minimal activity (IC50s >10 μM) against human EP1, EP2, and EP3 receptors.

$107

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ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE

T86034815-38-7

ETHYL 2-AMINO-4-METHYL-5-PHENYLTHIOPHENE-3-CARBOXYLATE targets the prostaglandin E2 receptor EP2 subtype (human)

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Darbufelone mesylate

T10960L139340-56-0In house

Darbufelone mesylate (CI-1004 mesylate) inhibited PGF2α and LTB4 in cells and demonstrated IC50 values of 0.19 μM for PGHS-2 and 20 μM for PGHS-1.

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Vedaprofen

T3668371109-09-6In house

Vedaprofen (PM 150) inhibits COX-1 and reduces prostaglandin H2 synthesis with anti-inflammatory activities. Vedaprofen is an inhibitor of Escherichia coli sliding clamp with the IC50 of 222 μM and Ki of 131 μM.

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PF-9184

T217381221971-47-6In house

PF-9184 is a potent and selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 of 16.5 nM, and it inhibits IL-1β-induced PGE2 synthesis in vitro.

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