16 phenoxy tetranor prostaglandin f2α

16-phenoxy PGF2α is a metabolically stable analog of PGF2α. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α.

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 (16-phenoxy tetranor PGF2α) is a metabolically stable form of PGF2α containing a 16-phenoxy group at the ω-terminus. It binds to the FP receptor on ovine luteal cells with much greater affinity (440%) than PGF2α. 16-phenoxy tetranor PGF2α methyl ester is a lipophilic analog of 16-phenoxy tetranor PGF2α. Methyl esters of PGs serve as prodrugs, as they are efficiently hydrolyzed in certain tissues to generate the bioactive free acid.

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.

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.

Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1 2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

Asperphenamate is a fungal metabolite of Aspergillus flatiipes. The IC50s for T47D cells, MDA-MB-231 cells, and HL-60 cells are 92.3 μM, 96.5 μM, and 97.9 μM. Asperphenamate shows an anticancer effect.

Moracin C, a natural compound found in Morus mesozygia, Morus alba var. multicaulis, is an anti-inflammatory agent. moracin C inhibits nitric oxide (NO) release and LPS-activated reactive oxygen species (ROS) in cells.

PF-04753299 is a potent and selective inhibitor of UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC), demonstrating bactericidal effects against gonococcal isolates and exhibiting inhibitory activity against E. coli, P. aeruginosa, and K. pneumoniae, with minimum inhibitory concentration (MIC) 90 values of 2 μg ml, 4 μg ml, and 16 μg ml, respectively. This compound is utilized in researching gram-negative bacterial infections [1].

SARS-CoV-2 3CLpro-IN-16 is a covalent inhibitor of SARS-CoV-2 3CLpro activity, exerting its effect by forming a covalent bond with Cys145.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).

PKI-402 is a potent PI3K and mTOR inhibitor. PKI-402 inhibits PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ with IC50s of 2, 3, 7, 14 and 16 nM, respectively.

2'-Deoxycytidine is one of the major nucleosides of DNA consisting of cytosine and deoxyribose and inhibits the biological effects of bromodeoxyuridine (Brdu). The nucleoside consists only of a pentose sugar attached to a purine or pyrimidine base and has no phosphate group. When N1 is attached to C1 of deoxyribose, deoxyribosides and nucleotides are formed from cytosine and deoxyribose; deoxycytidine monophosphate (dCMP), deoxycytidine diphosphate (dCDP), and deoxycytidine triphosphate (dCTP). cTP is the source of cytosine in RNA (ribonucleic acid) and deoxycytidine triphosphate (dCTP) is the source of deoxycytidine in DNA (deoxyribonucleic acid). Itaconic acid is a polymer.

Leonurine (SCM-198) is an alkaloid that has been found in H. leonuri and with anti-oxidative and anti-inflammatory.

Myrcene is a terpene that has been found in Cannabis and has antioxidative properties.

4-Hydroxyacetophenone (4-Acetylphenol) is a potent xanthine oxidase inhibitor.

DL-Pyroglutamic acid exhibited a strong inactivating effect on hepatitis B surface antigen.

Coumaran (2,3-Dihydrobenzofuran), an acetylcholinesterase (AChE) inhibitor isolated from the leaves of L. camara, can be used as a biopesticide and belongs to the class of 1-benzofurans as the 2,3-dihydro derivative of benzofuran with a role as a metabolite.

(-)-Cedrene (Alpha-Cedrene) is a sesquiterpene from cedar oil that has anti-leukemia, antibacterial and anti-obesity properties.