gli antagonist-1

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

5-HT6/7 antagonist 1 is a dual 5-HT6/7/2A and D2 receptor antagonist for the study of dementia and Alzheimer's disease.

Hepcidin antagonist-1 is an iron-modulating antagonist.Hepcidin antagonist-1 can be used to study metabolic disorders such as iron-deficiency diseases and anemia.

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

ORL1 antagonist 1 is an o antagonist of pioid receptor-like 1 (ORL1) (IC50 of 61 nM).

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist, has weak α1 adrenoceptor blocking activity.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

CRTh2 antagonist 1 is a CRTh2 antagonist (IC50: 89 nM).

5-HT2A antagonist 1 is a 5-HT2A antagonist. It may be useful in the treatment of gastrointestinal disorders circulatory disorders.

A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Sigma-1 receptor antagonist 2 is a potent and selective antagonist of sigma 1 receptor (σ1 R) (σ1 and σ2 receptor with Kis of 3.88 and 1288 nM , respectively).

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC50 of 37.9 μM. GABAB receptor antagonist 1 is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 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.

N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met inhibits endothelin binding to membranes from CHO cells carrying human ETA receptor and human ETB receptor with IC50 of 268nM and 1810nM, respectively.

CCR3 antagonist 1 is a potent CCR3 antagonist, used for the research of inflammatory and immunologic diseases.

CMKLR1 antagonist 1 (compound S-26d) is a potent, orally active antagonist of the chemokine-like receptor 1 (CMKLR1), exhibiting a pIC50 of 7.44 in hCMKLR1-transfected CHO cells. It is applicable in the research of psoriasis and metabolic diseases [1].

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol/L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg/L. Moreover, this compound exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg/adult) and low toxicity to zebrafish (LC50: 42.4 mg/L) [1].

DB21, Galectin-1 Antagonist, is a peptidomimetic conjugated with dibenzofuran, serving as an allosteric inhibitor of galectin-1 (GAL1) interactions with glycans on cell surfaces. This compound enhances the inhibition of angiogenesis and tumor growth in melanoma, lung adenocarcinoma, and ovarian cancer models [1].

GluR6 antagonist-1 inhibits the pY binding site of tyrosine kinase p56lck SH2 domain.

Compound 21, an orally active and selective RARα antagonist, exhibits a potent inhibition of the retinoic acid receptor α with an IC50 of 4.6 nM [1].

mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1].

Histamine H4 receptor antagonist-1 is a potent antagonist of the histamine H4 receptor.

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.

Succinate/succinate receptor antagonist 1 is a potent succinate receptor antagonist. Succinate/succinate receptor antagonist 1 interrupts succinate signals in gingival tissue and inhibits the activation of SucnRl Antagonist 1. Its IC50 value is 20 μsouth of the coast. Succinate/succinate receptor antagonist 1 can be used to treat periodontal disease.

Compound 4a, a mAChR antagonist, exhibits K i values of 255 nM for M1 and M5 subtypes, and lower values of 121 nM and 158 nM for M3 and M4 subtypes, respectively [1].

σ1 Receptor antagonist-1 is a selective sigma 1 receptor antagonist.

XIAP/cIAP1 antagonist-1 is a potent, orally active XIAP/cIAP1 antagonist that acts on XIAP (EC50: 5.1 nM) and cIAP1 (EC50: 0.32 nM). xIAP/cIAP1 antagonist-1 dose-dependently inhibits tumour growth in vivo.

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM, while not affecting CHO-BLT1 cell chemotaxis. It blocks the interaction between LTB4 and the BLT2 receptor with a K_i of 132 nM and may serve as a research tool for inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease [1].

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT 7 R receptor, with a dissociation constant (K i) of 6.5 nM.

Vanilloid receptor antagonist 1 (4-(7-Hydroxy-2-isopropyl-4-oxoquinazolin-3(4H)-yl)benzonitrile) is a potent vanilloid receptor TRPV1 antagonist.

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

NOD1/2 Antagonist-1 is a potent dual inhibitor of nucleotide-binding oligomerization domain-like receptors 1 and 2 (NOD1/2), displaying inhibitory concentrations (IC50) of 1.13 μM for NOD1 and 0.77 μM for NOD2. It exhibits an acceptable half-life (T1/2) of 67.6 minutes. Additionally, NOD1/2 Antagonist-1 enhances the antitumor efficiency of Paclitaxel (PTX).

A2A/A1 AR antagonist-1 (compound 1a) has the potential for ischemic stroke research which is potent A 2A /A 1 AR dual antagonist with Ki s of 5.58 and 24.2 nM, respectively [1].

Protease-Activated Receptor-1 Antagonist 2 is an orally active antagonist of protease-activated receptor-1 (PAR-1), demonstrating significant potency with an IC 50 of 7 nM. It exhibits favorable pharmacokinetic characteristics, making it valuable in cardiovascular disease (CVD) research, including studies on atherosclerosis and restenosis [1].

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

NLRP3 antagonist 1 shows potential for the cancer research that is a potent NLRP3 antagonist. NLRP3 is involved in the body's intrinsic immunity against stress injury and pathogenic infections that is mainly expressed in macrophages and neutrophils [1].

FXR antagonist 1 is a selective, orally active intestinal FXR antagonist with an IC50 value of 2.1 μM. FXR antagonist 1 antagonises intestinal FXR and selectively inhibits intestinal FXR signalling by feedback activation of hepatic FXR. FXR antagonist 1 can improve liver steatosis, inflammation and fibrosis in the NASH (non-alcoholic steatohepatitis) model and can be used to study NASH.

5-HT1A antagonist 1 (compound 6f) is a potent and selective 5-HT1Areceptor antagonist (Ki: 35 nM). 5-HT1A antagonist 1 can be used in the study of central nervous system disorders.

CXCR7 antagonist-1 is a specific antagonist of the binding of the SDF-1 chemokine or I-TAC to the chemokine receptor CXCR7. CXCR7 antagonist-1 prevents tumor cell proliferation and tumor formation and can be used in studies about inflammatory diseases.

TR antagonist 1 is a highly potent thyroid hormone receptor (TR) antagonist (IC50 of 36 and 22 nM for TRα and TRβ, respectively) that can be used to study diseases caused by endocrine abnormalities.

CCK-B Receptor Antagonist 1 is a cholecystokinin B (CCK-B) receptor agonist and has the potential of reducing the secretion of gastric acid.