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Results for "

non-peptide antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CGRP Receptor (3) Angiotensin Receptor (7) Apoptosis (7) Bombesin Receptor (4) Bradykinin Receptor (10) CCR (4) CFTR (4) Cholecystokinin Receptor (10) Complement System (1) CRFR (6) CXCR (6) Drug Isomer (1) Endogenous Metabolite (2) Endothelin Receptor (13) GCGR (3) GnRH Receptor (6) HIV (1) Integrin (11) Interleukin Related (1) Isotope-Labeled Compounds (2) mAChR (1) Neurokinin Receptor (15) Neuropeptide S Receptor (3) Neuropeptide Y Receptor (5) Neurotensin Receptor (4) NF-κB (1) Nuclear Factor of activated T Cells (NFAT) (3) Orexin Receptor (OX Receptor) (3) Oxytocin Receptor (6) Protease Activated Receptor (PAR) (5) Reactive Oxygen Species (ROS) (1) Reference Standards (7) Somatostatin Receptor (2) Thymidylate Synthase (1) Trk Receptor (1) Vasopressin Receptor (4)
By Research Areas:	Cancer (23) Cardiovascular Disease (36) Endocrinology (41) Infection (1) Inflammation/Immunology (27) Metabolic Disease (18) Neurological Disease (51)
Click Chemistry:	Alkynes (4)

139

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Formyl Peptide Receptor (FPR) Connective Peptide Peptide-Drug Conjugates (PDCs) Natriuretic Peptide Receptor (NPR) TNK1 RXFP Receptor CGRP Receptor Amyloid-β

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-16711

SB225002 Maximum Cited Publications 40 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-139035

CRHR1 antagonist 1	CRFR	Neurological Disease
CRHR1 antagonist 1 (compound 10a) is a non-peptide corticotropin-releasing hormone type 1 receptor (CRHR1) antagonist. CRHR1 antagonist 1 can be utilized in mental disorders research .

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-117053

ZM 253270	Neurokinin Receptor	Neurological Disease
ZM 253270 is a species-selective non-peptide NK-2 receptor (NK-2R) antagonist. ZM 253270 competitively inhibits the binding of [ ³H]NKA to native or cloned NK-2R from hamster bladder (K_i=2 nM), but has a weaker inhibitory effect (48-fold) on the binding of [ ³H]NKA to cloned human NK-2R .

HY-105137

Lanepitant dihydrochloride LY303870 dihydrochloride	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
Lanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide neurokinin-1 receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities .

HY-10308

Lefradafiban	Others	Metabolic Disease
Lefradafiban is an orally active glycoprotein IIb/IIIa receptor antagonist. Lefradafiban can be metabolized to its active form, Fradafiban, a non-peptide GP IIb/IIIa receptor antagonist .

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-19214

Elisartan HN 65021	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Elisartan is an orally active non-peptide pro-agent of angiotensin II AT1 receptor antagonist HN-12206, and shows anti-hypertension activities.

HY-120261

GB-88 1 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-125075

PD 165929	Bombesin Receptor
PD 165929 is a high affinity and competitive non-peptide neuromedin-B (NMB) receptor selective antagonist (K_i: 6.3 nM; IC₅₀: 150 nM for rat NMB receptor) .

HY-101986C

BIIE-0246 dihydrochloride AR-H 053591 dihydrochloride	Neuropeptide Y Receptor	Neurological Disease
BIIE-0246 dihydrochloride (AR-H 053591 dihydrochloride) is a potent and highly selective non-peptide neuropeptide Y (NPY) Y₂ receptor antagonist, with an IC₅₀ value of 15 nM .

HY-107723A

CGP71683	Neuropeptide Y Receptor	Metabolic Disease
CGP 71683 Free base serves as a powerful and highly selective non-peptide antagonist targeting the NPY Y(5) receptor, making it a valuable tool in obesity research.

HY-107533

T-98475	GnRH Receptor	Endocrinology
T-98475 (Compound 26d) is a potent, orally active, non-peptide luteinizing hormone-releasing hormone (LHRH) receptor antagonist with an IC₅₀ of 0.2 nM .

HY-18347A

Conivaptan hydrochloride 5+ 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-103357

LY288513	Cholecystokinin Receptor	Neurological Disease
LY288513 is a selective non-peptide CCK-B receptor antagonist with an IC₅₀ value of 16 nM. LY288513 produces an anxiolytic-like action in mice .

HY-10049A

CP 122721 hydrochloride	Neurokinin Receptor	Neurological Disease
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide neurokinin NK1 antagonist, with a pIC₅₀ of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .

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-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-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-108555

FR-171113	Protease Activated Receptor (PAR)	Cardiovascular Disease
FR171113 is a specific and non-peptide thrombin receptor antagonist. FR171113 exhibits the antithrombotic effects of a PAR1 antagonist. FR171113 inhibits thrombin-induced platelet aggregation with an IC₅₀ of 0.29 μM. .

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-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 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-10095

Olcegepant 35+ 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-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-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-12080

BX471 15+ 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-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-103304

CGRP antagonist 4	CGRP Receptor	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-12080A

BX471 hydrochloride 15+ 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-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-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-120308

(R)-Nolpitantium SR140603	Neurokinin Receptor	Neurological Disease
(R)-Nolpitantium is the R-enantiomer of Nolpitantium (HY-108479). 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-116066

YM471 free base	Endogenous Metabolite	Endocrinology
YM471 free base is a non-peptide antagonist of vasopressin V1A and V2 receptors with potent and persistent antagonistic activity. YM471 exhibits high affinity for rat V1A and V2 receptors with K values of 0.16 and 0.77 nM, respectively .

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-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-W370556

(Rac)-LM11A-31	Neurokinin Receptor	Neurological Disease
(Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist .

HY-18347AR

Conivaptan hydrochloride (Standard) YM 087 (Standard)	Reference Standards Vasopressin Receptor	Cardiovascular Disease Endocrinology
Conivaptan (hydrochloride) (Standard) is the analytical standard of Conivaptan (hydrochloride). This product is intended for research and analytical applications. 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-139799

Sch 202596	Neuropeptide Y Receptor	Metabolic Disease
Sch 202596 is a non-peptide antagonist of the galanin receptor subtype GalR1. Sch 202596 blocks the action of galanin by binding to GalR1, thereby reducing food intake. Sch 202596 can be used in the study of obesity and related eating disorders .

HY-U00235

SR121566A	Integrin	Inflammation/Immunology
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC₅₀s of 46±7.5, 56±6 and 42±3 nM, respectively.

HY-14369

Elagolix sodium NBI-56418 sodium	GnRH Receptor Nuclear Factor of activated T Cells (NFAT)	Endocrinology 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-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-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-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-108677

L-368,899 hydrochloride 3 Publications Verification	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-10898

SB-674042 1 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-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-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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2600

Kuwanon H	Structural Classification Flavonoids Classification of Application Fields Flavones Source classification Phenols Polyphenols Plants Moraceae Disease Research Fields Morus alba Linn. 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 Source classification Phenols Polyphenols Plants Moraceae Morus alba Linn.	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. .

Cat. No.	Product Name		Classification

HY-106203A

Crinecerfont hydrochloride SSR-125543 hydrochloride		Alkynes
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203

Crinecerfont SSR-125543		Alkynes
Crinecerfont (SSR-125543) hydrochloride is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research . Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-106203B

(R)-Crinecerfont (R)-SSR-125543		Alkynes
(R)-Crinecerfont is the R-enantiomer of Crinecerfont (HY-106203). Crinecerfont (SSR-125543) is a potent, orally active, non-peptide CRF1 receptor antagonist. Crinecerfont can be used for Classic congenital adrenal hyperplasia (CAH) research. Crinecerfont is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups .

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

NaturalProducts

Isotope-Labeled Compounds

Click Chemistry

Natural
Products