dp2

Dp2mT is an iron chelator which inhibits HIV-1 transcription.

CAY10595 is an antagonist of the CRTh2 (DP2) receptor with a Ki of 10 nM.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

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.

BI-671800 (AP-761) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2 CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has the potential to treat poorly controlled asthma[2].

Fevipiprant (NVP-QAW039) is a selective, potent, reversible competitive CRTh2 antagonist.

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

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.

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.

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.

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

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra

Timapiprant (OC000459) is a potent and selective D prostanoid receptor 2 (DP2) antagonist (IC50: 13 nM).

LAS191859 is a CRTH2/DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2/DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasti

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.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) is a synthetic analogue of PGD2 and a selective and potent CRTH2 DP2 receptor agonist that modulates eosinophil CD11b expression, actin polymerisation and chemotaxis.

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.

Pexopiprant, a potent oral antagonist of the prostaglandin D2 receptor 2 (DP2) with a K i value less than 100nM, is a valuable compound for asthma research.

AM-461 sodium is the sodium salt of AM-461 --- a novel DP2 receptor antagonist

AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay.

AM-461 is a DP2 receptor antagonist.

AM211 (AM211 free acid) is a potent and orally bioavailable antagonist of prostaglandin D2 (PGD2) receptor type 2 (DP2)

HAP-1, a synovial-targeted transduction peptide, selectively mediates the internalization of protein complexes into synovial cells of human and rabbit origin. When fused with the antimicrobial peptide (KLAK)2, HAP-1 forms the proapoptotic peptide DP2 [1].