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

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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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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Gestonorone Capronate

T137031253-28-7

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

$148

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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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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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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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Tebufelone

T68155112018-00-5In house

Tebufelone is a potent in vitro inhibitor of CO , a novel non-steroidal anti-inflammatory drug (NSAID) belonging to the di-tert-butylphenol (DTBP) class that has shown potent anti-inflammatory, analgesic and anti-reticulitis properties in various animal models. Tebufelone potently inhibits the formation of prostaglandins (PGE2) and blocks the formation of lipoxygenase pathway products [leukotriene (LTB4)] in rat macrophages (IC50 = 20 microM) and human whole blood (IC50 = 22 microM) in vitro. = 20 microM) and human whole blood (IC50 = 22 microM) from the formation of lipoxygenase pathway products [leukotriene (LTB4)] in vitro.

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TG6-129

T289581164464-14-5

TG6-129 is an antagonist of the EP2 receptor. TG6-129 suppresses PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM. TG6-129 reduces the expression of COX-2, IL-1β, IL-6, IL-12, IL-23 and TNF-α induced by the EP2-selective

$123

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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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Angoroside C

T3903115909-22-3

Angoroside C is a Potential anti-inflammatory compound. Inhibitor of prostaglandin E2 release in mouse peritoneal macrophages in vitro. Shows potent antioxidative activity in reducing the oxidized OH adducts of dAMP and dGMP. Reveals some trypanocidal potential.

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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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Friedelin

TN1650559-74-0

Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities.

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CAY10471 Racemate

T7359844639-57-2

CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective CRTH2 DP2 receptor antagonist. It binds to human CRTH2 DP2, DP1, and TP receptors with Ki values of 0.6, 1200, and >10,000 nM, respectively.

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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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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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Taraxasterol

T37701059-14-9

Taraxasterol (Taraxasterin) is compound with 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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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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PF-04418948

T33061078166-57-0

PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).

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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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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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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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Cloprostenol sodium salt

T584755028-72-3

Cloprostenol sodium salt (ICI 80996 sodium salt) is a more water-soluble, crystalline form of cloprostenol compared to the free acid and is a synthetic analog of prostaglandin F2α.

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Anisotropine Methylbromide

T498180-50-2

Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion.

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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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4-O-Cinnamoylquinic acid

TN66475509-70-6

4-O-Cinnamoylquinic acid is a small molecule compound extracted from the dried fruits of Casearia grewiifolia, which has an inhibitory effect on prostaglandins and inhibits the production of superoxide anions in human neutrophils.

$148

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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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EP1-antagonist-1

T10031851204-35-8In house

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

$195

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Carboprost tromethamine

T1486558551-69-2

Carboprost tromethamine, a synthetic 15-methyl analogue of prostaglandin F2α, effectively promotes uterine contractions and significantly reduces bleeding during and post-delivery.

$120

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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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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.

$113

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