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Nonpeptide

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By Targets:	Aminopeptidase (1) Angiotensin Receptor (9) Apelin Receptor (APJ) (1) Apoptosis (13) Bacterial (5) Bombesin Receptor (3) Bradykinin Receptor (11) Calcium Channel (1) Caspase (3) Cathepsin (1) CCR (7) CFTR (3) CGRP Receptor (3) Cholecystokinin Receptor (10) Complement System (1) CRFR (3) CXCR (6) Endothelin Receptor (13) ERK (1) GCGR (5) GHSR (3) GnRH Receptor (5) HIV (2) HIV Protease (2) IGF-1R (1) Integrin (9) 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 (8) PGE synthase (1) Potassium Channel (2) Prolyl Endopeptidase (PREP) (3) PROTACs (1) Protease Activated Receptor (PAR) (5) Proteasome (1) Reactive Oxygen Species (1) RIP kinase (1) RXFP Receptor (2) SARS-CoV (8) Somatostatin Receptor (4) Src (1) Thrombopoietin Receptor (10) Vasopressin Receptor (7) Virus Protease (1)
By Research Areas:	Cancer (34) Cardiovascular Disease (49) Endocrinology (49) Infection (18) Inflammation/Immunology (34) Metabolic Disease (26) Neurological Disease (73)
Click Chemistry:	Alkynes (5)

208

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P1095

Ivachtin Caspase-3 Inhibitor VII	Caspase	Cardiovascular Disease Neurological Disease
Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC₅₀ of 23 nM. Ivachtin has modest selectivity for the remaining caspases .

HY-10309

Sibrafiban RO 48-3657	Integrin	Cardiovascular Disease
Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-proagent of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation .

HY-121885

LMD-009 1 Publications Verification	CCR	Metabolic Disease Endocrinology
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC₅₀s from 11 to 87 nM .

HY-12436

NTRC-824	Neurotensin Receptor	Neurological Disease
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC₅₀ of 38 nM and a K_i of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (K_i >30 μM) .

HY-145278

RXFP3/4 agonist 2	RXFP Receptor	Neurological Disease
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC₅₀=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC₅₀ values in the range of 10-22 nM .

HY-50688

SB-265610 2 Publications Verification	CXCR	Inflammation/Immunology
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC₅₀s of 3.7 nM and 70 nM, respectively .

HY-145279

RXFP3 agonist 1	RXFP Receptor	Others
RXFP3 agonist 1 is a nonpeptide RXFP3 agonist (EC₅₀=6937 nM) .

HY-105235

Enadoline CI-977	Opioid Receptor	Neurological Disease
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-105235A

Enadoline hydrochloride CI-977 hydrochloride	Opioid Receptor	Neurological Disease
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-105346

WIN 51708	Neurokinin Receptor	Neurological Disease
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 .

HY-120096

BIBO3304 free base	Neuropeptide Y Receptor	Neurological Disease
BIBO3304 free base is a nonpeptide neuropeptide Y Y1 receptor antagonist. BIBO3304 free base displays subnanomolar affinity for both the human and the rat Y1 receptor, with IC₅₀ values of 0.38 nM and 0.72 nM, respectively. BIBO3304 free base significantly inhibits food intake induced by application of NPY or by fasting .

HY-136181

YNT-185 dihydrochloride	Orexin Receptor (OX Receptor)	Neurological Disease
YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC₅₀s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models .

HY-124733A

LIT-001	Oxytocin Receptor	Neurological Disease
LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC₅₀=55 nM; K_i=226 nM). LIT-001 improves social interaction in a mouse model of autism .

HY-110135A

NBI-31772 hydrate	IGF-1R	Neurological Disease
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (K_is=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects .

HY-124733

LIT-001 free base	Oxytocin Receptor	Neurological Disease
LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC₅₀=55 nM; K_i=226 nM). LIT-001 free base improves social interaction in a mouse model of autism .

HY-136181A

YNT-185	Orexin Receptor (OX Receptor)	Neurological Disease
YNT-185 is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC₅₀s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 ameliorates narcolepsy-cataplexy symptoms in mouse models .

HY-14128

NBI-34041 SB-723620	CRFR	Neurological Disease
NBI-34041 (SB-723620) is a selective and orally active nonpeptide CRF1 receptor antagonist with an IC₅₀ of 58.9 nM and a K_i of 4.0 nM for human CRF1 receptor. NBI-34041 has no inhibitory effect on the CRF2 receptor. NBI-34041 can be used for depression and anxiety disorders research.

HY-116567

OPC-51803	Vasopressin Receptor	Metabolic Disease
OPC-51803 is an orally active nonpeptide vasopressin V₂ receptor agonist. OPC-51803 can be used for the research of micturition disorders that result in frequent micturition, such as that from polyuria, nocturnal polyuria, and some kinds of urinary incontinence .

HY-12844

Ro 64-6198 1 Publications Verification	Opioid Receptor	Neurological Disease
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC₅₀ value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .

HY-14886

Fasitibant chloride MEN16132 free base	Bradykinin Receptor	Cardiovascular Disease Neurological Disease
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .

HY-108574

CP 339818 hydrochloride	Potassium Channel	Neurological Disease
CP 339818 hydrochloride is a nonpeptide and selective Kv1.3 (IC₅₀ value of ~200 nM) and Kv1.4 channels blocker. CP 339818 hydrochloride is a significantly less potent blocker of Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2. CP 339818 hydrochloride potently blocks the C-type inactivated conformation of Kv1.3 and suppresses T cell activation .

HY-14994

SCH79797 dihydrochloride 2 Publications Verification	Protease Activated Receptor (PAR) Apoptosis	Cardiovascular Disease
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC₅₀ of 70 nM and a K_i of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC₅₀ of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .

HY-14993

SCH79797 2 Publications Verification	Protease Activated Receptor (PAR) Apoptosis	Cardiovascular Disease
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC₅₀ of 70 nM and a K_i of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC₅₀ of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .

HY-168152

SARS-CoV-2 3CLpro-IN-26	SARS-CoV Virus Protease	Infection
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC₅₀ of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .

HY-100292

SL910102	Angiotensin Receptor	Cardiovascular Disease Endocrinology
SL910102 is a nonpeptide angiotensin AT₁ receptor antagonist.

HY-115272

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

HY-120148A

SM19712	Others	Others
SM19712 serves as an inhibitor of the nonpeptide endothelin converting enzyme.

HY-19732

BIBS 39	Angiotensin Receptor	Cardiovascular Disease Endocrinology
BIBS 39 is a new nonpeptide angiotensin II (AII) receptor antagonist.

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-101038A

ZK756326 dihydrochloride 1 Publications Verification	CCR	Endocrinology Cancer
ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

HY-11077

SR 146131	Cholecystokinin Receptor	Metabolic Disease Endocrinology
SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.

HY-15015A

OT-R antagonist 2 Oxytocin receptor antagonist 2	Oxytocin Receptor	Endocrinology
OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist.

HY-123744

PD-156707	Endothelin Receptor	Cardiovascular Disease
PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist .

HY-101038

ZK 756326	CCR	Endocrinology Cancer
ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

HY-19670

Befetupitant Ro67-5930	Neurokinin Receptor	Neurological Disease Endocrinology
Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.

HY-15778

AVE 0991 10+ Cited Publications	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC₅₀ of 21 nM .

HY-15015

OT-R antagonist 1 Oxytocin receptor antagonist 1	Oxytocin Receptor	Endocrinology
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.

HY-103363

SB-328437 1 Publications Verification	CCR	Inflammation/Immunology
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC₅₀ of 4.5 nM .

HY-103351

Cathepsin G Inhibitor I	Cathepsin	Inflammation/Immunology
Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G .

HY-19191

L-159282 MK 996	Angiotensin Receptor	Cardiovascular Disease Endocrinology
L-159282 is a highly potent, orally active, nonpeptide angiotensin II receptor antagonist, with anti-hypertensive activity.

HY-100269

Chymase-IN-1	Others	Inflammation/Immunology
Chymase-IN-1 is a potent, selective, orally active, nonpeptide inhibitor of human mast cell chymase with an IC₅₀ of 29 nM.

HY-121767

PD 123177	Angiotensin Receptor	Cardiovascular Disease
PD 123177 is a nonpeptide antagonist specific for angiotensin II (AII) subtype AT2 receptor in mammalian systems .

HY-15009

Fuscoside 1 Publications Verification OPC-21268	Vasopressin Receptor	Cardiovascular Disease Endocrinology
Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC₅₀ of 0.4 μM.

HY-101720

Fradafiban BIBU-52	Integrin	Cardiovascular Disease
Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a K_d value of 148 nM.

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-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-126106

(BrMT)2	Potassium Channel	Others
(BrMT)2 (compound 2) is a non-peptide snail toxin that slows down the activation of Kv1.1 channels .

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-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-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.

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-116700

Hinnuliquinone	Structural Classification Natural Products Nepenthes mirabilis (Lour.) Druce Source classification Plants Nepenthaceae	HIV Protease HIV
Hinnuliquinone is a C2-symmetric dimeric non-peptide fungal metabolite inhibitor of HIV-1 protease. Hinnuliquinone is a bis-indolyl-2,5-dihydroxybenzoquinone pigment, that can be isolated from Nodulisphorium hinnuleum .

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-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 .

HY-168152

SARS-CoV-2 3CLpro-IN-26		Alkynes
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC₅₀ of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .

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 .

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