ot antagonist 3

OT antagonist 3 is an antagonist of oxytocin (OT).

OT antagonist 3 analog is an analogue of OT antagonist 3.

TRPM8 antagonist WS-3 (Cyclohexanecarboxamide) is an agonist of TRPM8( EC50 : 3.7 μM).

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

AMPA receptor antagonist-3 is an AMPA receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).

Estrogen receptor antagonist 3 is a potent degradation agent of the estrogen receptor (ER). Estrogen signaling systems regulate cell growth, differentiation, and apoptosis, and estrogen receptor antagonist 4 has shown potential for cancer research.

Compound 24e, a leukotriene B4 (LTB4) antagonist, exhibits an inhibitory concentration 50 (IC50) of 477 nM and demonstrates anti-inflammatory activity [1].

IL-17A antagonist 3 is an inhibitor of IL-17A.

EP3 antagonist 3 (compound 2) is a potent and specific EP3 receptor antagonist with a significant pKi value of 8.3, high oral bioavailability, and excellent pharmacokinetic properties, making it ideal for experimental overactive bladder (OAB) research [1].

TRPV4 antagonist 3 is a TRPV4 antagonist (pIC50 = 8.4).

Mu opioid receptor antagonist 3 (compound 26) is a potent and selective MOR antagonist with the ability to penetrate the blood-brain barrier (Ki: 0.24 nM, EC50: 0.54 nM). This compound can be used to study opioid use disorder (OUD).

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].

A1AR antagonist 3 (compound 13) is a selective adenylate 1 (A1) receptor antagonist with an affinity for human A1 (Ki: 9.69 nM) and rat A1 (Ki: 0.529 nM). It is suitable for research on neurological diseases.

Androgen receptor antagonist 3 (Compound C18) exhibits anticancer activity as an antagonist of the androgen receptor (AR) with an IC50 value of 2.4 μM [1].

GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a favorable pharmacokinetic profile, suitable for further research and development [1].

Calcium Channel antagonist 3 is a voltage-gated calcium channel inhibitor (IC50 : 5-20 μM).

Compound 5e, a GPR34 receptor antagonist, exhibits selective inhibition of lysophosphatidylserine-induced ERK1 2 phosphorylation in a dose-dependent manner, demonstrating an IC50 value of 0.680 μM without significant cytotoxicity. Additionally, it displays antisensory activity in a mouse neuropathic pain model [1].

GPVI antagonist 3 (Compound 2) is a promising antiplatelet agent that selectively inhibits the interaction between the Glycoprotein VI (GPVI) receptor and its ligands. It demonstrates potent inhibitory effects with IC50 values of 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin, and 51.74 μM for thrombin, positioning it as a potential novel antithrombotic treatment [1].

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

A1/A3 AR Antagonist 3 is a dual A1R/A3R antagonist that demonstrates high affinity within the low-micromolar to nanomolar range, and is potentially useful in the research of chronic heart diseases [1].

Orexin receptor antagonist 3 (example 216) functions as an orexin receptor antagonist.

A2A receptor antagonist 3 (Example 92) is an adenosine A2A receptor antagonist (Ki: 0.4 nM) and a receptor (Ki: 1467 nM).

Protease-Activated Receptor-1 antagonist 3 is a potent antagonist of Protease-Activated Receptor-1 (IC50: 7 nM) and exhibits binding affinity to hERG K+ channels (IC50: 9 μM).

MCHR1 antagonist 3, a potent antagonist of the melanin-concentrating hormone receptor-1 (MCHR1), is employed for the regulation of energy metabolism.

Galectin-3, a β-galactoside-specific carbohydrate recognition protein (lectin), facilitates the migration of B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and demonstrates resistance to pharmaceutical interventions.

hGPR91 antagonist 3 is an orally active, potent, and selective hGPR91 antagonist. hGPR91 antagonist 3 is used to study hypertension, autoimmune diseases, and retinal angiogenesis. hGPR91 antagonist 3 has been shown to be effective in the treatment of hypertension, autoimmune disease, and retinal angiogenesis.

When administered intratumorally, AR antagonist 3 shows effective inhibition on the growth of tumor. AR antagonist 3 is a potent and selective antagonist of androgen receptor (AR) with an IC 50 of 0.47 μM. AR antagonist 3 dose-dependently decrease the FRET signal with an IC50 of 18.05 μM [1].

NMDA receptor antagonist-3 is a NMDA receptor antagonist with a significan recovery rate (40.0%, at 100 μM) and safe toxicological characteristics in SH-SY5Y and human adipose mesenchymal stem cells.

TRPV1 antagonist 3 (Compound 7q) is a highly potent TRPV1 receptor antagonist with an IC50 of 2.66 nM against capsaicin. It exhibits selectivity in its mode of action, is orally bioavailable (60%), and can penetrate the central nervous system [1].

ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist with an IC50 of 0.26 nM, utilized for pulmonary arterial hypertension (PAH) research. This compound demonstrates efficacy in mitigating monocrotaline-induced PAH in a rat model [1].

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

P2X7 receptor antagonist-3 is a potent inhibitor of the P2X7 receptor, with IC50 values of 4.2 nM in humans and 6.8 nM in rats, demonstrating its high efficacy across species.

CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

OT antagonist 1 demethyl derivative, a demethyl derivative of OT antagonist 1, is a selective Oxytocin antagonist with a Ki of 50 nM.

MrgprX2 antagonist-3 is a potent inhibitor of MrgprX2. It holds promising potential for investigating skin inflammatory disorders.

CXCR2 antagonist 3 (compound 11h) is a highly effective inhibitor of CXC chemokine receptor 2 (CXCR2), displaying double-digit nanomolar potencies in inhibiting neutrophil infiltration into the air pouch. Additionally, it reduces neutrophil and MDSC infiltration while enhancing CD3+ T lymphocyte infiltration into Pan02 tumor tissues [1].

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 μM. CCR4 antagonist 3-1 inhibits the binding of radiolabeled [125I]TARC and macrophage-derived chemokine ( MDC) to CEM cell surface and inhibits TARC-mediated CEM cell migration in vitro with an IC50 value of 6.4 μM. CCR4 antagonist 3 inhibited the binding of radiolabeled [125I]TARC and macrophage-derived chemokine (MDC) to the CCR4 receptor on the surface of CEM cells and inhibited TARC-mediated migration of CEM cells in vitro with an IC50 value of 6.4 μM.

H4R antagonist 3 is a novel histamine-4 receptor (H4R) antagonist with an EC50 <10 mM.H4R antagonist 3 has potential inflammatory activity for the study of autoimmune, allergic and ocular diseases.

OT-R antagonist 2 is a nonpeptide, low molecular weight antagonist of OT-R (oxytocin receptor).

CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].

TRPA1 Antagonist 3 is a compound with photoswitchable properties that acts as an agonist on the TRPA1 channel, providing the ability for optical control.

OT antagonist 1 is a potent and selective antagonist of Oxytocin(Ki of 50 nM)

CCR2 antagonist 3 (AZD-2927) is an antagonist of CCR2.