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non-peptide receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CGRP Receptor (3) Angiotensin Receptor (9) Apelin Receptor (APJ) (1) Apoptosis (12) Bacterial (5) Bombesin Receptor (3) Bradykinin Receptor (10) CCR (2) CFTR (3) Cholecystokinin Receptor (10) Complement System (1) CRFR (3) CXCR (1) Endothelin Receptor (13) ERK (1) GCGR (5) GHSR (3) GnRH Receptor (4) Integrin (4) Isotope-Labeled Compounds (2) mAChR (1) Neurokinin Receptor (14) Neuropeptide Y Receptor (7) Neurotensin Receptor (4) NF-κB (1) Nuclear Factor of activated T Cells (NFAT) (2) Opioid Receptor (8) Orexin Receptor (OX Receptor) (5) Oxytocin Receptor (5) PROTACs (1) Protease Activated Receptor (PAR) (3) Reactive Oxygen Species (1) RIP kinase (1) Somatostatin Receptor (4) Thrombopoietin Receptor (10) Vasopressin Receptor (5)
By Research Areas:	Cancer (22) Cardiovascular Disease (45) Endocrinology (40) Infection (5) Inflammation/Immunology (18) Metabolic Disease (23) Neurological Disease (64)
Click Chemistry:	Alkynes (4)

155

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Formyl Peptide Receptor (FPR) CGRP Receptor Amyloid-β

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108625

SHA 68 1 Publications Verification	Neuropeptide Y Receptor	Neurological Disease
SHA 68 is a potent and selective non-peptide *neuropeptide S receptor* (NPSR) antagonist with IC₅₀**s 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-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-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-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-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-115272

GSK894490A	GHSR	Neurological Disease
GSK894490A is a non-peptide ghrelin receptor agonist .

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-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-50844

Ibutamoren Mesylate 5 Publications Verification MK-677; MK-0677	GHSR	Endocrinology
Ibutamoren Mesylate (MK-677) is a potent, non-peptide *Growth hormone secretagogue receptor* (GHSR)** agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.

HY-107094

MT-7716 hydrochloride W-212393 hydrochloride	Opioid Receptor	Neurological Disease
MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide *nociceptin receptor* (NOP)** agonist and promising potential treatment drug for alcohol abuse and relapse prevention .

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-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-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-123376

FR-190997	Bradykinin Receptor	Neurological Disease
FR-190997 is a non-peptide Bradykinin B2 receptor selective agonist, K_i value is 9.8 nM. FR-190997 is also an effective antihypertensive agent .

HY-107723A

CGP71683	Others	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-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-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-107094A

MT-7716 free base W-212393	Opioid Receptor	Neurological Disease
MT-7716 free base (W-212393) is a selective non-peptide *nociceptin receptor* (NOP)** agonist and promising potential treatment drug for alcohol abuse and relapse prevention .

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-103536

Galnon	Neuropeptide Y Receptor	Neurological Disease
Galnon is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with K_is of 11.7 and 34.1 μM respectively. Galnon exhibits anticonvulsant and anxiolytic effects .

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-18347AR

Conivaptan hydrochloride (Standard)	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-14184

Macitentan 5+ 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-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-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-10095

Olcegepant Maximum Cited Publications 34 Publications Verification 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-10095A

Olcegepant hydrochloride Maximum Cited Publications 34 Publications Verification 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-103536A

Galnon TFA	Neuropeptide Y Receptor	Neurological Disease
Galnon TFA is a selective and non-peptide agonist of galanin GAL1 and GAL2 receptor, with K_is of 11.7 and 34.1 μM respectively. Galnon TFA exhibits anticonvulsant and anxiolytic effects .

HY-129658A

TT-OAD2	GCGR	Metabolic Disease
TT-OAD2 is a non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist with an EC₅₀ of 5 nM. TT-OAD2 has the potential for diabetes treatment .

HY-123547

TLK19781	Others	Others
TLK19781 is a non-peptide small molecule insulin receptor activator that increases the content of insulin-stimulated GLUT4 on the cell membrane and enhances the activity of insulin-stimulated glucose transport in cell and animal models of insulin resistance.

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-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-124767

SR 142948A	Others	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-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-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-125976

ML233	Apelin Receptor (APJ)	Cardiovascular Disease
ML233 is a non-peptide based potent *apelin receptor* (APJ) agonist (EC₅₀*=3.7 μM). ML233 displays >21-fold selective over the closely related angiotensin 1 (AT1) receptor* (>79 μM) .

HY-12698

NNC 63-0532	Opioid Receptor	Neurological Disease
NNC63-0532 is a novel non-peptide nociceptin receptor (ORL1) agonist, with EC₅₀s of 305?nM. NNC63-0532 plays important roles in many disorders such as pain, drug addiction .

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-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-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-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)[1].

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-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-W370556

(Rac)-LM11A-31	Others	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-116066

YM471 free base	Others	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-112824

L-162313	Angiotensin Receptor	Cardiovascular Disease
L-162313 is a non-peptide angiotensin II AT1 and AT2 receptor agonist, with IC₅₀ values of 1.1 and 2.0 nM for AT1 and AT2 receptor, respectively. L-162313 can be used for the research of vasoconstriction, aldosterone release, and cardiovascular growth .

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-108482

CP-96,345	Cardiovascular Disease Classification of Application Fields Disease Research Fields	Neurokinin Receptor
CP-96,345 is a specific, highly potent, and orally active tachykinin and substance P receptor non-peptide inhibitor. CP-96,345 prevents the drop in blood pressure evoked by substance P and neurokinin A. CP-96,345 can be used for researching neurogenic inflammation .

HY-N2600R

Kuwanon H (Standard)	Structural Classification Flavonoids Flavones Source classification Phenols Polyphenols Plants Moraceae Morus alba Linn.	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)[1].

HY-15306S

Eltrombopag-13C4

1 Publications Verification

Eltrombopag- ¹³C₄ (SB-497115- ¹³C₄) is ^{13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .}

HY-13463BS

Avatrombopag-d8 hydrochloride

Avatrombopag-d₈ (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].

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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