ep1

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

EP1013 is a broad-spectrum selective inhibitor of Caspase used in the study of type 1 diabetes.

PEP1 is a biologically active peptide that interacts with POPC supported lipid bilayers (SLBs), binding at low concentrations, while higher concentrations induce POPC SLB lysis.

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

EP12, a c-Myc inhibitor and G4 stabilizer, induces apoptosis and DNA damage in multiple myeloma cells while obstructing P65/P50 nuclear translocation by disrupting the NF-κB signaling pathway, effectively inhibiting multiple myeloma growth [1].

ZA3-Ep10, a zwitterionic lipid, is utilized in the formulation of lipid nanoparticles for RNA delivery in vivo and non-viral CRISPR/Cas gene editing applications.

Peptide containing the 'TGL' motif that corresponds to the C-terminus of GluR1 subunit

TAT-NEP1-40 TFA, a blood-brain barrier-permeable peptide, safeguards PC12 cells against oxygen and glucose deprivation (OGD) and fosters neurite outgrowth. Additionally, it enhances neurological outcomes post-ischemia by curtailing apoptosis in ischemic cerebral tissues. This compound has utility in investigating central nervous system (CNS) injuries, encompassing axonal regeneration and functional recuperation following a stroke [1].

TAT-NEP1-40 acetate, a potential therapeutic for axonal regeneration and functional recovery post-stroke, safeguards PC12 cells from oxygen and glucose deprivation (OGD) and encourages neurite outgrowth. This compound also affords cerebral protection against ischemia/reperfusion injury by hindering neuronal apoptosis and can be effectively administered into rat brains [1] [2].

TAT-NEP1-40, a blood-brain barrier (BBB) permeable peptide, confers protection to PC12 cells against oxygen and glucose deprivation (OGD) while promoting neurite outgrowth. Furthermore, it enhances neurologic outcomes post-ischemia by mitigating apoptosis in affected cerebral regions. This compound holds potential for central nervous system (CNS) injury research, including studies on axonal regeneration and post-stroke functional recovery [1].

Pep19-2.5, a synthetic antitoxin peptide, inhibits the intracellular signaling cascade triggered by endotoxins by blocking the activity of lipopeptides (LP) and lipopolysaccharides (LPS) mediated through both transmembrane and cytosolic pattern recognition receptors (PRRs). This action disrupts the signaling pathways that normally result in inflammation and cell pyroptosis [1].

Analog of Pep1-TGL

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.

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).

ONO-8130 is an orally available antagonist of EP1 receptor.

19(R)-hydroxy Prostaglandin E1 is an agonist of EP1 and EP3 receptor subtypes and exhibits contractile activity on smooth muscle and is the major prostaglandin in primate semen.

Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration. Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl displays only a weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropy

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β/Smad2 signaling pathway [1] [2] [3].

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

AH 6809 is an antagonist of EP and DP receptor(with Kis of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptor respectively). AH 6809 has a Ki of 350 nM for mouse EP2 receptor.

EP1 receptor antagonist

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(S)-Iloprost potently inhibits platelet aggregation with an IC50 value of 3.5 nM.

SC 51322 is an EP1 prostanoid receptor antagonist.

ONO-8711 is a potent and selective competitive antagonist of EP1 receptor with Kis of 0.6 nM and 1.7 nM for human and mouse EP1, respectively. ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer [1].

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.

17-Phenyl trinor Prostaglandin E2 (17-phenyl trinor PGE2) is a synthetic analog of PGE2, functioning as an agonist at the EP1 and EP3 receptors. It induces contraction of the guinea pig ileum at a 11 µM concentration and displays slightly less potency than PGE2 in stimulating the gerbil colon and rat uterus. Notably, with an ED50 value of 350 µg/kg, 17-phenyl trinor PGE2 exhibits 4.4 times greater antifertility efficacy in hamsters compared to PGE2.

Alprostadil sodium is a prostaglandin receptor ligand with Ki values of 36, 10, 1.1, 2.1, and 33 nM for EP1, EP2, EP3, EP4, and IP, respectively, in mice.It induces vasodilatation and inhibits platelet aggregation, and it can be used as a vasodilator for the study of peripheral vascular disease.

Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 |Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels

SC 51089 free base is a selective antagonist of the prostaglandin E2 EP1 receptor, demonstrating neuroprotective activity. It exhibits binding affinities (Kis) of 1.3 μM for EP1, 11.2 μM for TP, 17.5 μM for EP3, and 61.1 μM for FP receptors, respectively.

BW A868C, a hydantoin compound and structural analogue of BW245C, functions as a selective and potent competitive antagonist of prostaglandin D2 (PGD2), showing no activity on other prostaglandin receptors (IP, EP1, EP2, TP, and FP) [1].

GW848687X, a potent and selective prostaglandin EP1 receptor antagonist, is used for the treatment of inflammatory pain.

EP3 and EP1 receptor agonist

CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3) (IC50 : 8.5 (pKi )).

15(R)-Prostaglandin E2, the C-15 epimer of the more physiologically abundant 15(S)-PGE2 (sc-201225) isomer, is produced mainly from arachidonic acid (sc-200770) via the action of COX and PGES enzymes. Present in nearly all cell types, PGE2 interacts with four distinct receptors, EP1 to EP4, leading to a wide range of biological effects. However, 15(R)-Prostaglandin E2 exhibits significantly lower efficacy in most biological assays compared to its 15(S) counterpart. Notably, acid catalyzed epimerization can transform 15(R)-Prostaglandin E2 into the more active 15(S)-Prostaglandin E2 form.

SC 51089 is a selective prostaglandin receptor PGE2 antagonist with selectivity for prostaglandin receptor subtypes and antinociceptive activity that improves motor deficits and rescues memory decline in the Huntington's disease R6/1 mouse model .

Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6]

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

ONO-8539 is a prostanoid EP1 receptor antagonist.

Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(R)-Iloprost inhibits platelet aggregation with an IC50 value of 65 nM.

GSK-269984A is an antagonist of Prostaglandin E2 Receptor 1 (EP1) (pIC50: 7.9).

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.

ONO-DI-004 is a selective EP1 Prostanoid receptor agonist.

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

GSK-269984B is a novel antagonist of EP1 receptor.

17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to increase lipid solubility, thereby improving uptake into tissues and further lowering the effective concentration. Ethyl amide groups are then removed by amidases, regenerating the active free acid.

Omidenepag (UR-7276) is a selective and potent prostaglandin E2 receptor 2 (EP2) agonist and a novel topical ocular hypotensive agent.Omidenepag is used in the study of glaucoma and hypertension.

8-iso Prostaglandin E1 causes spasm in the pulmonary veins of dogs and also acts as a vasodilator.