fp receptor

Omidenepag isopropyl (DE-117) is a selective prostaglandin EP2 receptor agonist and a novel topical ocular blood pressure lowering compound.Omidenepag isopropyl has a weak affinity for EP1, EP2, and FP receptors.Omidenepag isopropyl is used in studies of glaucoma and hypertension. Omidenepag isopropyl can be used to study glaucoma and hypertension.

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).

ONO-AE3-208 (AE 3-208) is an EP4 antagonist. It suppresses cell migration, invasion, and metastasis of prostate cancer.

Latanoprost lactone diol is an important intermediate compound in the synthesis of Latanoprost. Latanoprost, classified as a prostaglandin F2α analogue, functions as an agonist for the FP prostanoid receptor, resulting in a reduction in intraocular pressure (IOP).

RIP2 kinase inhibitor 1 is a potent and selective receptor interacting inhibitor of protein 2 (RIP2) kinase(RIP2 FP with an IC50 of 0.03 μM ),and is used for autoinflammatory disorders.

Latanoprost acid is a selective agonist of prostanoid receptors and inhibits RANKL-induced osteoclastogenesis and function through the inhibition of c-fos NFATc1 pathway. Latanoprost acid can be used in studies about lowering pressure inside the eyes.

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

CAY10509 is a PGF2α analogue and acts as an FP receptor inhibitor with an IC50 of 30 nM. It shows potential for use in studying the physiological regulatory mechanisms related to prostaglandins.

Latanoprosttris(triethylsilyl) ether is a precursor in the synthesis of Latanoprost, which serves as an agonist for the prostaglandin F2α (PGF2α) receptor, also known as the FP receptor.

Bimatoprost acid (17-phenyl trinor PGF2α) is a metabolically stable analog of PGF2α and has a potential antagonistic activity for the FP receptor. It has a relative potency of 756% compared to PGF2α for binding to the FP receptor on ovine luteal cells.

AL-8810, an 11β-fluoro analog of PGF 2α, acts as a selective antagonist at the PGF 2α receptor (FP receptor) [1].

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

AS604872 is a selective antagonist of the FP receptor.. AS604872 significantly accelerated degeneration of the media in both cerebral artery and aorta as evidenced by thinning of the media and disruption of the elastic lamina and promoted IA and aortic di

(+) - cloprostenol sodium is a kind of water-soluble prostaglandin F2 α ( PGF2 α) Analogues. It is an FP receptor agonist and a potent luteinizing agent in rats and hamsters.

AL-3138 is a prostaglandin F2alpha (PGF2alpha) analogue which antagonizes FP prostanoid receptor-mediated inositol phosphates generation.

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity in commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. From what can be inferred from the study of other trans isomers of F-type prostaglandins, the biological activity of this isomer is likely to be similar to that of the cis isomer. However, there are no specific published reports on the biological activity, and on reducing intraocular pressure in particular, of 5-trans latanoprost.

(+)-Cloprostenol is a synthetic analog of prostaglandin F2α (PGF2α). It is an FP receptor agonist and a potent luteolytic agent in rats and hamsters. It is 200 times and 100 times more potent than PGF2α in terminating pregnancy in hamsters and rats, respectively, without the side effects associated with PGF2α. Cloprostenol is also used in veterinary medicine as a luteolytic agent for the induction of estrus and the treatment of reproductive disorders in cattle, swine, and horses. (+)-Cloprostenol methyl ester is a more lipid soluble form of cloprostenol, which may be more amenable for certain formulations.

There are currently four prostaglandin (PG) derivatives which have been approved for human clinical use for the treatment of glaucoma. The names of the PGs and the concentrations of the approved doses are: travoprost (40 μg/ml), latanoprost (50 μg/ml), bimatoprost (300 μg/ml), and unoprostone (1,500 μg/ml). All of these compounds are modified at C-1 in order to act as lipophilic prodrugs in the eye. All have also been postulated to function via activation of the prostanoid FP receptor. Unoprostone and bimatoprost stand out in this class due to their lack of potency. Both are also claimed to have alternate mechanisms of actions: as a docosanoid in the case of unoprostone and as a prostamide in the case of bimatoprost. Lumula is a hybrid eicosanoid analog which incorporates the docosanoid features of unoprostone as well as the prostamide features of bimatoprost. Based on classical structure-activity relationships which have been established for prostanoid receptors

Prostaglandin F2α (PGF2α), acting through the FP receptor, causes smooth muscle contraction and exhibits potent luteolytic activity. 17-trifluoromethylphenyl trinor Prostaglandin F2α (17-trifluoromethylphenyl trinor PGF2α) is an analog of PGF2α that shares the meta-trifluoromethyl group of travoprost with the 17-phenyl trinor modification of latanoprost. It is anticipated to be a potent and selective agonist of the FP receptor, with potential applications in glaucoma and luteolysis. 17-trifluoromethylphenyl trinor PGF2α ethyl amide is a lipophilic analog of 17-trifluoromethylphenyl trinor PGF2α. Ethyl amides of PGs can serve as prodrugs, as they are hydrolyzed in certain tissues to generate the bioactive free acid.

Prostaglandin F1α (PGF1α) is the putative metabolite of dihomo-γ-linolenic acid (DGLA) via the cyclooxygenase (COX) pathway. Both PGF1α and PGF2α have been shown to act as priming pheromones for male Atlantic salmon with a threshold concentration of 10-11 M. [1] PGF1α binds to the ovine corpus luteum FP receptor at only 8% of the relative potency of PGF2α. [2] It is only half as active as PGF2α in inducing human respiratory smooth muscle contractions in vitro. [3]

17-phenyl trinor Prostaglandin F2α N-ethyl amide (17-phenyl trinor PGF2α) is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name 17-phenyl trinor PGF2α ethyl amide. Investigations in our lab have shown that 17-phenyl trinor PGF2α ethyl amide is converted by an amidase enzymatic activity in the human cornea to yield the corresponding free acid, with a conversion rate of about 25 μg/cornea/24 hours. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist. 15(R)-17-phenyl trinor PGF2α is the 15-epi, or unnatural isomer of this active free acid metabolite. It has much diminished FP receptor-mediated activity

15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys. 15(S)-Latanoprost is a potential impurity in most commercial preparations of the latanoprost bulk drug product.

The actions of many clinical F-series prostaglandins (PGs), including those used for estrous synchronization and for reduction of intraocular pressure (IOP), are mediated through the PGF2α (FP) receptor. 16-phenoxy tetranor Prostaglandin F2α cyclopropyl methyl amide (16-phenoxy tetranor PGF2α cyclopropyl methyl amide) is an analog of PGF2α containing a 16-phenoxy group on the lower (ω) side chain and a cyclopropyl methyl amide at the C-1 position. There are no published reports on the biological activity of 16-phenoxy tetranor PGF2α cyclopropyl methyl amide.

Prostaglandin F2α (PGF2α) drives luteolysis and smooth muscle contraction by activating the FP receptor. Stable, lipophilic analogs of PGF2α are used to modulate luteolysis and treat glaucoma. 16-phenoxy tetranor Prostaglandin F2α isopropyl ester (16-phenoxy tetranor PGF2α isopropyl ester) is a lipophilic analog of 16-phenoxy tetranor PGF2α. Isopropyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.