tmbim-6 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.

(1R,5S,6r)-N-(2-methyl-1-((3-methylpyridin-2-yl)oxy)propan-2-yl)-3-azabicyclo[3.1.0]hexane-6-carboxamide L(+)-Tartaric acid is a potential SSTR4 agonist.

1-[2,4-Dihydroxy-6-methoxy-3-(3-methyl-2-buten-1-yl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one (Xanthohumol) , prenylchacone flavonoid, is a natural product with multi-biofunctions purified from Hops Humulus lupulus,is effective against HIV-1 and might serve as an interesting lead compound. It may represent a novel chemotherapeutic agent for HIV-1 infection.

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

Ethyl 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate has an inhibitory effect on coagulation factor Xa, and it can be used in the study of thrombophlebitis, atherosclerosis, cerebral embolism, stroke and pulmonary embolism.

1-Ethyl-6-aminouracil (6-AMINO-1-ETHYL-1H-PYRIMIDINE-2,4-DIONE) is an intermediate in the synthesis of a series of new substituted Xanthines which have high affinity and selectivity for the human adenosine A2B receptors.

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.

CCR1 antagonist 6 is a CCR1 antagonist (IC50: 3 nM).

2,5-Morpholinedione, 4-methyl-6-(1-methylethyl)-3-(phenylmethyl)- is the trans structure of Lateritin.

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.

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.

β-amyloid 1-11 acetate is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.

CDK4/6/1 Inhibitor (Crozbaciclib) is a type of CDK4/6 inhibitor (IC50s: 3 and 1 nM). CDK4/6 inhibitor is a class of compounds used for the treatment of some types of hormone receptor positive, HER2-negative breast cancer, which can block the process of breast cancer cell division and reproduction.

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

Angiotensin I/II (1-6) is a peptide (ASP-ARG-VAL-TYR-ILE-HIS) that contains the amino acids 1-6 and is converted from Angiotensin I/II peptide.

6-chloro-1-ethyl-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is a compound used as a molecular structural unit for pefloxacin impurities.

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.

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

Acth (1-4) acetate is the ACTH N-terminal tetrapeptide.

6-(4-methylpiperazin-1-yl)-4-o-tolylnicotinamide can be used in the synthesis of befetupitant and netupitant.

1-(2,3-DIHYDRO-BENZO[1,4]DIOXIN-6-YL)-5-OXO-PYRROLIDINE-3-CARBOXYLIC ACID targets GRK2.

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

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

(25R)-3β,17α-dihydroxy-5α- spirostan-6-one3-O-α-L- rhamnopyranosyl-(1→2)-β- D-glucopyranoside is a natural product isolated from the bulbs of Lilium brownii var. viridulum.

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).

Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.

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.

1H-benzo[d][1,2,3]triazol-1-yl 8-methoxy-6-nitrophenanthro[3,4-d][1,3]dioxole-5-carboxylate is a useful organic compound for research related to life sciences and the catalog number is T72065.

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].

6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine, an alkaloid, markedly alters the characteristics of cellular organelles—specifically, early endosomes, mitochondria, and autophagosomes—in Parkinson’s Disease patient-derived olfactory cells [1].

Hederagenin 28-O-{β-D-xylopyranosyl-(1→6)-β-D-glucopyranosyl ester}3-O-{α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranosyl} is a saponin known for its antitumor and anti-inflammatory properties [1].

6-Chloro-1-tetralone (6-chloro-3;5-Chloro-1-Indomone) is an important intermediate for the synthesis of pharmaceutical compounds.

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

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

1-(6-Methoxy-2-naphthyl)ethanol is used as pharmaceutical intermediates.

Borneol 7-O-[beta-D-apiofuranosyl-(1->6)]-beta-D-glucopyranoside is a natural product from Radix ophiopogonis.