tp receptor

TP receptor antagonist-1 (compound 7m) serves as an antagonist for the thromboxane A2 receptor (TP receptor), exhibiting IC50 values of 9.46 μM for TPa and 8.49 μM for TPb. It is utilized in the study of cardiovascular diseases [1].

TP Receptor Antagonist-2 (example 7n), a thromboxane A2 receptor (TP receptor) antagonist, exhibits inhibitory activity with IC50 values of 5.64 μM for TPα and 5.27 μM for TPβ. It effectively inhibits platelet aggregation [1].

Synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. Thymopentin (TP5) is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.

TP003 is a novel non-selective GABAA receptor benzodiazepine site agonist with affinity for α1β2gam2, α2β3gam2, α3β3gam2, α5β2gam2, EC50 of 20.3, 10.6, 3.24, 5.64 nM, respectively. TP003 has antianxiety and partial anticonvulsant activity via the α2GABAA receptor.

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).

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.

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

I-SAP is a high affinity TP receptor antagonist. At physiologic pH, I-SAP produces platelet shape change, but not aggregation, with an EC50 value of 9.7 nM. I-SAP binds to human platelets with the maximum binding obtained between pH 6.5 and pH 7.4. In washed human platelets, the Kd for I-SAP is 468 pM at pH 7.4 and 490 pM at pH 6.5.

TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.

(±)16,17-EDT, an oxylipin metabolite of adrenic acid produced through the cytochrome P450 (CYP) pathway, effectively induces dilation in isolated porcine arterioles (EC50 = 11 pM) and promotes relaxation of isolated bovine coronary arteries previously contracted by the TP receptor agonist U-46619.

KP496 is a selective, dual antagonist for the Thromboxane A2 receptor (TP) and the Leukotriene D4 receptor (cysLT1).

Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng/ml.

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

TP-5801 TFA is an orally active inhibitor of TNK1, a non-receptor tyrosine kinase, with an IC50 of 1.40 nM, demonstrating anti-tumor activity [1].

Dubermatinib (TP0903) is a potent and selective Axl kinase inhibitor.

Seratrodast (ABT-001) (INN), a thromboxane A2 (TXA2) receptor (TP receptor) antagonist, is mainly used in the therapy of asthma. It was the first TP receptor antagonist developed as an anti-asthmatic drug and attained marketing qualification in Japan in 1997.

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

I-BOP is an agonist (KD=0.61 nM) at the thromboxane A2 receptor (TP). I-BOP promotes cell proliferation by activating the PI3K pathway in vascular smooth muscle.

ONO-AE3-208 is an EP4 receptor antagonist with a Ki of 1.3 nM, exhibiting less potent activity against EP3, FP, and TP receptors (Ki values of 30, 790, and 2,400 nM, respectively), while showing no effect on other prostanoid receptors. In wild type mice, treatment with ONO-AE3-208, in conjunction with 3% dextran sodium sulfate, results in severe colitis characterized by epithelial loss, crypt damage, and inflammation, thereby mimicking the effects of EP4 deletion. Further, this compound has been utilized to investigate the role of EP4 signaling in various biological contexts, including immune and autoimmune responses, inflammation, and cancer.

TP-5801 is an orally active non-receptor tyrosine kinase (TNK1) inhibitor with an IC50 of 1.40 nM and exhibits antitumor effects.

cAC 253 acetate (TP2135 Free base) is an amylin antagonist. cAC 253 acetate inhibits 125I-adrenomedullin binding, with an IC50 of 25 nM.

(±)13,14-EDT, an oxylipin metabolite derived from adrenic acid through the cytochrome P450 (CYP) pathway, acts as a potent activator of large-conductance calcium-activated potassium channels (KCa1.1/BK) in isolated rat coronary small arterial smooth muscle cells at 50 nM, promoting dilation. Additionally, it induces arteriole dilation in isolated porcine samples with an EC50 of 12 pM and relaxes isolated bovine coronary arteries previously contracted by TP receptor agonist U-46619.

GW627368 (GW 627368X)X is a novel, potent and selective antagonist of prostanoid EP4 receptor.

Prostaglandin J2 (PGJ2), a derivative of Prostaglandin D2 (PGD2), serves as a potent agonist for PGD2 receptors (DP), exhibiting affinity constants (K i) of 0.9 nM and 6.6 nM for hDP and hCRTH2 receptors, respectively. It activates cyclic AMP production with an EC50 of 1.2 nM, induces oxidative stress, neuronal apoptosis, and promotes the accumulation of ubiquitinated (Ub) proteins. Notably, PGJ2's neurotoxic properties are implicated in the progression of neurodegenerative diseases such as Alzheimer's (AD) and Parkinson's (PD) [1] [2] [3] [4].