dp1

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

DP-1, a Ganetespib degradation product, represents a fragment derived from SDC-TRAP-0063. Ganetespib itself functions as an inhibitor of heat shock protein 90 (HSP90), exhibiting notable anti-tumor properties.

Fructo-oligosaccharide DP14, an oligosaccharide derived from Atractylodes lancea [1], represents a specific polysaccharide subclass with a degree of polymerization of 14.

Fructo-oligosaccharide DP13 is an inulin-type fructan that can be isolated from Morinda officinalis [1].

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

Fructo-oligosaccharide DP11/GF10 is a fructooligosaccharide (FOS) compound with a degree of polymerization (DP) equal to 11. FOS consists of 10 fructose units connected by (2→1)-β-glycosidic bonds, with a single D-glucosyl unit present at the non-reducing end.

TDP1 Inhibitor-1 is a potent inhibitor of Tyrosyl-DNA Phosphodiesterase 1 (TDP1) (IC50 of 7 μM).

TDP1 Inhibitor-2 is a potent inhibitor of TDP1 (tyrosyl-DNA phosphodiesterase 1) (IC50: 99 nM) and inhibits SCAN1 (spinal cerebellar ataxia syndrome with axonal neuropathy) (IC50: 3.5 μM).

MDP1, derived from Melittin, disrupts the membrane integrity of both Gram-positive and Gram-negative bacteria, leading to bacterial death through membrane damage. This compound exhibits potent antibacterial activity against multidrug-resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa [1].

Fructo-oligosaccharide DP12/GF11 is a member of fructooligosaccharides (FOS) characterized by a degree of polymerization (DP) of 12. FOS compounds consist of 11 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.

SDP116, a synthetic peptide derivative of the GPR116 Stachel sequence, exhibits ADGRF5 agonistic activity [1].

Fructo-oligosaccharide DP10/GF9 is a compound classified as a fructooligosaccharide (FOS) with a degree of polymerization (DP) of 10. FOS consists of a chain of 9 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.

MDP1 acetate, a derivative of Melittin, compromises the membrane integrity of both Gram-positive and Gram-negative bacteria leading to bacterial death through membrane damage. It exhibits potent antibacterial activity against multidrug-resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa [1].

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).

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.

Ralinepag (APD811) is a potent, orally bioavailable agonist of non-prostanoid prostacyclin (IP) receptor, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

BW 245C is a selective prostaglandin-like DP receptor (DP1) agonist, a prostaglandin analogue with inhibitory effects on the aggregation response of collagen, which can be used to study diseases such as stroke.

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6 1.9 6.2 nM).

L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively).

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

Asapiprant (S-555739) is a potent and selective DP1 receptor antagonist (Ki: 0.44 nM). It exhibited high affinity and selectivity for the DP1 receptor.

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

AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of As

S-5751, a prostanoid DP (DP1) antagonist, is used potentially for the treatment of bronchial asthma.

Laropiprant analog is an antagonist of the prostaglandin PGD2 receptor DP1.

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).

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

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2/DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

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.

Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.

Treprostinil Palmitil (TP), a prodrug of the DP1 and EP2 agonist Treprostinil (UT-15), exhibits EC50 values of 0.6 and 6.2 nM, respectively. It is a pure prodrug without any inherent binding affinity for G-protein coupled receptors, including prostanoid receptors.

CAY10471 Racemate (TM30089 Racemate) is a potent, highly selective CRTH2/DP 2 receptor antagonist. CAY10471 Racemate binds to the human CRTH2/DP2, DP1, and TP receptors( Ki values of 0.6, 1200, and >10,000 nM,respectively)