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Results for "

non-peptide antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Angiotensin Receptor (11) Apoptosis (9) Bombesin Receptor (6) Bradykinin Receptor (11) CCR (5) CGRP Receptor (3) Cholecystokinin Receptor (14) Complement System (1) CRFR (8) CXCR (6) Drug Derivative (1) Drug Isomer (1) Endogenous Metabolite (2) Endothelin Receptor (15) GCGR (3) GnRH Receptor (9) HIV (1) Integrin (13) Interleukin Related (1) Isotope-Labeled Compounds (3) mAChR (1) Neurokinin Receptor (19) Neuropeptide S Receptor (3) Neuropeptide Y Receptor (4) Neurotensin Receptor (6) NF-κB (1) Nuclear Factor of activated T Cells (NFAT) (6) Orexin Receptor (OX Receptor) (6) Oxytocin Receptor (9) Protease Activated Receptor (PAR) (7) Reactive Oxygen Species (ROS) (1) Reference Standards (19) Somatostatin Receptor (2) Thymidylate Synthase (2) Trk Receptor (1) Vasopressin Receptor (4)
By Research Areas:	Cancer (31) Cardiovascular Disease (45) Endocrinology (48) Infection (1) Inflammation/Immunology (31) Metabolic Disease (18) Neurological Disease (68)
Click Chemistry:	Alkynes (1)

169

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Products

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10095

Olcegepant 40+ Cited Publications BIBN-4096; BIBN 4096BS	CGRP Receptor	Neurological Disease
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the *calcitonin gene-related peptide* 1 (CGRP1) receptor with IC₅₀ of 0.03 nM and K_i** of 14.4 pM for human CGRP .

HY-16711

SB225002 Maximum Cited Publications 60 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits ¹²⁵I-IL-8 binding to CXCR2 with an IC₅₀ of 22 nM.

HY-18347A

Conivaptan hydrochloride 10+ Cited Publications YM 087	Vasopressin Receptor	Cardiovascular Disease Endocrinology
Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with K_i values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

HY-14184

Macitentan 10+ Cited Publications ACT-064992	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-12080

BX471 20+ Cited Publications ZK-811752	CCR	Inflammation/Immunology Endocrinology
BX471 (ZK-811752) is an orally active, potent and selective non-peptide CCR1 antagonist with a K_i of 1 nM, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

HY-108677

L-368,899 hydrochloride 5+ Cited Publications	Oxytocin Receptor	Endocrinology
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC₅₀s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent .

HY-103377

Antalarmin hydrochloride 5+ Cited Publications	CRFR	Inflammation/Immunology Endocrinology
Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a K_i of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome .

HY-14369

Elagolix sodium NBI-56418 sodium	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Metabolic Disease Cancer
Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-110155

LM11A-31 dihydrochloride 5+ Cited Publications	Neurotensin Receptor	Neurological Disease
LM11A-31 dihydrochloride, a non-peptide p75 ^NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. LM11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression .

HY-123617

AZ8838	Protease Activated Receptor (PAR)	Inflammation/Immunology
AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK_i of 6.4 for hPAR2 .

HY-19947

PF-06291874 1 Publications Verification Glucagon receptor antagonists-4	GCGR	Metabolic Disease
PF-06291874 is a highly potent, non-peptide and orally active glucagon receptor antagonist. PF-06291874 is under the study for type 2 diabetes mellitus (T2DM) .

HY-10095A

Olcegepant hydrochloride 40+ Cited Publications BIBN-4096 hydrochloride; BIBN4096BS hydrochloride	CGRP Receptor	Neurological Disease
Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the *calcitonin gene-related peptide* 1 (CGRP1) receptor with IC₅₀ of 0.03 nM and with a K_i** of 14.4 pM for human CGRP .

HY-12080A

BX471 hydrochloride 20+ Cited Publications ZK-811752 hydrochloride	CCR	Inflammation/Immunology Endocrinology
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with K_i of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

HY-14789

(R)-Elagolix NBI-56418	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Endocrinology Cancer
Elagolix is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-120261

GB-88 2 Publications Verification	Protease Activated Receptor (PAR)	Inflammation/Immunology
GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca ²⁺ release with an IC₅₀ of 2 μM .

HY-10898

SB-674042 2 Publications Verification	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-674042 is a potent and selective non-peptide orexin OX₁ receptor antagonist (K_d=5.03 nM), exhibits 100-fold selectivity for OX₁ over OX₂ receptors with IC₅₀ values of 3.76 nM and 531 nM, respectively .

HY-108625

SHA 68 1 Publications Verification	Neuropeptide S Receptor	Neurological Disease
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC₅₀s of 22.0 and 23.8 nM for NPSR Asn ¹⁰⁷ and NPSR Ile ¹⁰⁷, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .

HY-15522

WAY-267464 2 Publications Verification	Oxytocin Receptor	Neurological Disease
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .

HY-101844

ML-18	Bombesin Receptor	Cancer
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC₅₀ of 4.8 μM.

HY-135542

NBI-27914 2 Publications Verification	CRFR	Others
NBI-27914 is a highly selective, high-affinity non-peptide competitive antagonist of human corticotropin-releasing factor receptor 1 (CRFR1). NBI-27914 primarily binds to the His199 and Met276 sites in the transmembrane domain of the receptor .

HY-108626

ML154 NCGC84	Neuropeptide S Receptor	Neurological Disease
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA₂ of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC₅₀ values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .

HY-B0780

Fimasartan 4 Publications Verification BR-A-657	Angiotensin Receptor Apoptosis NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology Endocrinology
Fimasartan (BRA-657) is an orally effective angiotensin receptor AT1 non-peptide antagonist. Fimasartan has antihypertensive effects. Fimasartan improves neuroinflammation and brain injury mediated by NLRP3 inflammatome after intracerebral hemorrhage, and has neuroprotective effect. Fimasartan inhibits the expression of inducible nitric oxide synthase through the inactivation of NF-κB and activator protein-1 .

HY-15039

SSR240612	Bradykinin Receptor	Metabolic Disease Inflammation/Immunology Endocrinology
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with K_is of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

HY-16992A

W-54011 5+ Cited Publications	Complement System Reactive Oxygen Species (ROS)	Inflammation/Immunology
W-54011 is a potent and orally active non-peptide C5a receptor antagonist. W-54011 inhibits the binding of ¹²⁵I-labeled C5a to human neutrophils with a K_i value of 2.2 nM. W-54011 also inhibits C5a-induced intracellular Ca ²⁺ mobilization, chemotaxis, and generation of ROS in human neutrophils with IC₅₀s of 3.1 nM, 2.7 nM, and 1.6 nM, respectively .

HY-109093

Linzagolix KLH-2109; OBE-2109	GnRH Receptor	Inflammation/Immunology Cancer
Linzagolix (KLH-2109; OBE-2109) is a potent, non-peptide, and orally active GnRH antagonist. Linzagolix can be used for uterine fibroids, endometriosis, adenomyosis research .

HY-70068

SB-408124	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-408124 is a non-peptide OX1 receptor antagonist with K_is of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor .

HY-N2600

Kuwanon H	Bombesin Receptor	Cancer
Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a K_i value of 290 nM in cells .

HY-108483

RP 67580	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a K_i value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .

HY-124767

SR 142948A	Neuropeptide Y Receptor	Neurological Disease
SR 142948A is a non-peptide neuropeptide neuropeptin (NT) receptor antagonist. SR 142948A is able to bind to neuropeptin receptors, especially with high affinity for NT1 and NT2 receptors. SR 142948A is mainly used to study the role of neuropeptide in the neurotransmitter system, especially the dopamine system .

HY-106840

L-365260 2 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .

HY-123499

SRA880	Somatostatin Receptor	Cardiovascular Disease
SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .

HY-19431

Ro 46-8443	Endothelin Receptor	Cardiovascular Disease
Ro 46-8443 is the first non-peptide endothelin ET_B receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ET_B (IC₅₀: 34-69 nM) over ET_A receptors (IC₅₀: 6800 nM) .

HY-108679

WAY-267464 hydrochloride 2 Publications Verification	Oxytocin Receptor	Neurological Disease
WAY-267464 (hydrochloride) is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 (hydrochloride) can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 (hydrochloride) can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .

HY-121156A

Anatibant hydrochloride LF 16-0687 hydrochloride; XY-2405 hydrochloride	Bradykinin Receptor	Neurological Disease
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with K_i values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .

HY-107691

GR 159897	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide neurokinin 2 (NK₂) receptor antagonist. GR 159897 has little or no affinity for NK₁ and NK₃ receptors. GR 159897 inhibits binding of [ ³H]GR100679 to human NK₂ (hNK₂)-CHO cells and rat colon membranes with pK_is of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .

HY-19529

Ro 46-2005	Endothelin Receptor	Cardiovascular Disease Endocrinology
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

HY-14184S

Macitentan-d4 ACT-064992-d₄	Isotope-Labeled Compounds Endothelin Receptor Apoptosis	Cardiovascular Disease
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-110155A

(Rac)-LM11A-31 dihydrochloride	Drug Isomer	Neurological Disease
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 ^NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist .

HY-14184R

Macitentan (Standard) ACT-064992 (Standard)	Reference Standards Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-101764

Lintitript SR 27897	Cholecystokinin Receptor	Metabolic Disease
Lintitript (SR 27897) is a highly potent, selective, orally active, competitive and non-peptide cholecystokinin (CCK1) receptor antagonist with an EC₅₀ of 6 nM and a K_i of 0.2 nM. Lintitript displays > 33-fold selectivity more selective for CCK1 than CCK2 receptors (EC₅₀ value of 200 nM). Lintitript increases plasma concentration of leptin and food intake as well as plasma concentration of insulin .

HY-103304

SB 268262	Others	Neurological Disease
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes .

HY-19374

BAY-27-9955	GCGR	Metabolic Disease
BAY-27-9955 is an orally active non-peptide glucagon receptor antagonist. Bay 27-9955 competitively blocks the interaction of glucagon with the human glucagonreceptor at an IC₅₀ value of 110 nM. BAY-27-9955 can be used for the study of type 2 diabetes .

HY-108479

Nolpitantium SR140333	Neurokinin Receptor	Neurological Disease
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK₁ receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation .

HY-106840A

L-365260 hemihydrate 2 Publications Verification	Cholecystokinin Receptor	Neurological Disease Metabolic Disease
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with K_is of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .

HY-106994A

Nebentan potassium YM598	Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ET_A receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ ¹²⁵I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

HY-135500

ACT-373898	Endothelin Receptor	Endocrinology
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .

HY-14184A

Macitentan n-butyl analogue	Endothelin Receptor	Cardiovascular Disease Endocrinology
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).

HY-116854

NNC 92-1687	GCGR	Metabolic Disease
NNC 92-1687 is a non-peptide competitive human glucagon receptor antagonist (IC₅₀=20 μM; K_i=9.1 μM). NNC 92-1687 can be used in the research of type 2 diabetes .

HY-76612

SB-408124 Hydrochloride	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with K_is of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor .

HY-16741

Erlosiban OBE001	Oxytocin Receptor	Endocrinology
Erlosiban (OBE001) is an orally active non-peptide type oxytocin receptor antagonist. Erlosiban inhibits the increase of intracellular calcium concentration, thereby reducing uterine smooth muscle contraction. Erlosiban can be used for research on premature birth and to improve embryo implantation and pregnancy rate in assisted reproductive technology (AR).

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2600

Kuwanon H	Flavonoids Classification of Application Fields Flavones Phenols Polyphenols Plants Moraceae Disease Research Fields Morus alba Linn. Source Classification Cancer	Bombesin Receptor
Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a K_i value of 290 nM in cells .

HY-N2600R

Kuwanon H (Standard)	Structural Classification Flavonoids Flavones Phenols Polyphenols Plants Moraceae Morus alba Linn. Source Classification	Reference Standards Bombesin Receptor
Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells .

Cat. No.	Product Name	Chemical Structure

HY-14184S

Macitentan-d4
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-W751574

Elagolix-d6 sodium
Elagolix-d₆ (sodium) (NBI-56418-d₆ (sodium)) is deuterium labeled Elagolix sodium. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

HY-115633S

Elagolix-d9
Elagolix-d₉ is the deuterium labeled Elagolix. Elagolix sodium is a highly effective, selective, oral-active, short-term, non-peptide gonadotropin-releasing hormone receptor (GnRH receptor) antagonist (K_D = 54 pM) and NFAT inhibitor, which can be used to study pain related to endometriosis. .

Cat. No.	Product Name		Classification

HY-105346

WIN 51708		Alkynes
WIN 51708 is a nonpeptide antagonist of neurokinin (NK)-1 receptor. WIN 51708 has a higher affinity for the rat NK-1 receptor compared to the human NK-1 receptor .

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non-peptide antagonist

Inhibitors & Agonists

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Isotope-Labeled Compounds

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