CRTH2

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.

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

Setipiprant (ACT-129968) is an orally available, selective CRTH2 antagonist (IC50: 6.0 nM). CRTH2, a G protein-coupled receptor for prostaglandin (PGD2), mediates key inflammatory responses related to allergy and asthma. PGD2, produced by mast cells, binds to CRTH2 on blood-borne cells, inducing chemotaxis of Th2 cells, basophils, and eosinophils, and stimulating cytokine release.

MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

CRTh2 antagonist 2 is a selective and potent CRTH2 antagonist, IC50≤10 nM. CRTh2 antagonist 2 can be used to study the direction of androgenic alopecia.

(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid is a prostaglandin-like CRTH2 antagonist with an IC50 < 10 μM, which can be used in studies of rhinitis, COPD, rheumatoid arthritis, eczema and conjunctivitis.

CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the

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.

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

NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro.

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).

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].

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.

MK-7246 S enantiomer is a potent and selective CRTH2 antagonist.

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).

Vidupiprant (AMG 853) is an effective dual antagonist of CRTH2 and prostanoid D receptor with IC50s of 8 nM and 35 nM in human plasma. Vidupiprant can be used in studies about the treatment of asthma.

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

TASP0376377 is a potent antagonist of CRTH2.

TASP0412098 is a potent, selective CRTH2 antagonist with oral activity.

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.