Search Result

Targets Recommended:	Aldehyde Dehydrogenase (ALDH) Lactate Dehydrogenase Dihydroorotate Dehydrogenase Isocitrate Dehydrogenase (IDH) PDHK 15-PGDH

Results for "Aldehyde Dehydrogenase (ALDH) Agonists" in MCE Product Catalog:

By Targets:	Aldehyde Dehydrogenase (ALDH) (17) Dihydroorotate Dehydrogenase (27) Isocitrate Dehydrogenase (IDH) (11) Lactate Dehydrogenase (13) PDHK (8) 5-HT Receptor (137) AChE (3) ADC Linker (7) Adenosine Receptor (30) Adenylate Cyclase (1) Adiponectin Receptor (3) Adrenergic Receptor (129) Akt (2) Amyloid-β (2) Androgen Receptor (9) Angiotensin Receptor (17) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (11) Apoptosis (58) Aryl Hydrocarbon Receptor (10) ATP Citrate Lyase (1) Autophagy (78) Bacterial (21) Bcl-2 Family (2) Bombesin Receptor (4) Bradykinin Receptor (5) Calcium Channel (11) Cannabinoid Receptor (31) Caspase (1) CaSR (3) CCR (2) CDK (1) CGRP Receptor (4) Cholecystokinin Receptor (4) Complement System (8) COMT (1) COX (1) CRFR (11) CRISPR/Cas9 (1) CXCR (9) Cytochrome P450 (10) DNA/RNA Synthesis (26) Dopamine Receptor (80) Drug Metabolite (14) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) EBI2/GPR183 (2) Endogenous Metabolite (97) Endothelin Receptor (6) Enterovirus (2) Ephrin Receptor (1) Epigenetic Reader Domain (1) ERK (4) Estrogen Receptor/ERR (27) Fatty Acid Synthase (FASN) (1) Ferroptosis (13) Fungal (4) FXR (17) GABA Receptor (39) GHSR (12) Glucagon Receptor (28) Glucocorticoid Receptor (23) GlyT (1) GnRH Receptor (4) GPCR19 (8) GPR109A (4) GPR119 (10) GPR120 (8) GPR139 (2) GPR40 (20) GPR55 (1) GPR84 (3) Guanylate Cyclase (4) HBV (7) HCV (8) HCV Protease (2) HDAC (1) Hedgehog (1) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (25) Histone Methyltransferase (4) HIV (14) HSV (6) IFNAR (4) iGluR (29) IKK (1) Imidazoline Receptor (6) Influenza Virus (11) Insulin Receptor (2) Integrin (4) Interleukin Related (3) IRE1 (1) JAK (1) Leukotriene Receptor (1) LPL Receptor (24) LXR (16) mAChR (34) MCHR1 (GPR24) (4) MDM-2/p53 (4) Melanocortin Receptor (22) Melatonin Receptor (13) mGluR (37) MicroRNA (1) Mineralocorticoid Receptor (1) Mitochondrial Metabolism (3) Mitophagy (3) MMP (1) Monoamine Oxidase (1) Motilin Receptor (2) nAChR (48) Neurokinin Receptor (14) Neuropeptide Y Receptor (29) Neurotensin Receptor (4) NF-κB (8) NKCC (1) NO Synthase (2) Notch (1) Nucleoside Antimetabolite/Analog (2) Opioid Receptor (80) Orexin Receptor (OX Receptor) (11) Oxytocin Receptor (3) P2X Receptor (3) P2Y Receptor (9) PAK (2) Parasite (16) PARP (1) Phosphatase (3) Phosphodiesterase (PDE) (3) PKC (2) Potassium Channel (10) PPAR (64) Progesterone Receptor (7) Prostaglandin Receptor (32) PROTAC Linker (8) Protease-Activated Receptor (PAR) (22) Proteasome (1) Pyroptosis (1) RAR/RXR (31) Reactive Oxygen Species (10) RET (1) Reverse Transcriptase (2) ROR (29) SARS-CoV (6) Serotonin Transporter (4) Sigma Receptor (15) Sirtuin (3) Smo (6) Sodium Channel (5) Somatostatin Receptor (10) STAT (2) STING (15) TGF-beta/Smad (1) TGF-β Receptor (1) Thrombin (2) Thrombopoietin Receptor (7) Thyroid Hormone Receptor (10) TNF Receptor (1) Toll-like Receptor (TLR) (35) Trk Receptor (4) TRP Channel (33) TSH Receptor (4) Urotensin Receptor (4) Vasopressin Receptor (10) VD/VDR (4) VEGFR (1) Virus Protease (4) Wnt (5) β-catenin (3) γ-secretase (1)
By Research Areas:	Cancer (344) Cardiovascular Disease (184) Endocrinology (288) Infection (90) Inflammation/Immunology (310) Metabolic Disease (298) Neurological Disease (667)

By Targets:

Aldehyde Dehydrogenase (ALDH) (17)

Dihydroorotate Dehydrogenase (27)

Isocitrate Dehydrogenase (IDH) (11)

Lactate Dehydrogenase (13)

PDHK (8)

5-HT Receptor (137)

AChE (3)

ADC Linker (7)

Adenosine Receptor (30)

Adenylate Cyclase (1)

Adiponectin Receptor (3)

Adrenergic Receptor (129)

Akt (2)

Amyloid-β (2)

Androgen Receptor (9)

Angiotensin Receptor (17)

Angiotensin-converting Enzyme (ACE) (1)

Antibiotic (11)

Apoptosis (58)

Aryl Hydrocarbon Receptor (10)

ATP Citrate Lyase (1)

Autophagy (78)

Bacterial (21)

Bcl-2 Family (2)

Bombesin Receptor (4)

Bradykinin Receptor (5)

Calcium Channel (11)

Cannabinoid Receptor (31)

Caspase (1)

CaSR (3)

CCR (2)

CDK (1)

CGRP Receptor (4)

Cholecystokinin Receptor (4)

Complement System (8)

COMT (1)

COX (1)

CRFR (11)

CRISPR/Cas9 (1)

CXCR (9)

Cytochrome P450 (10)

DNA/RNA Synthesis (26)

Dopamine Receptor (80)

Drug Metabolite (14)

Drug-Linker Conjugates for ADC (1)

E1/E2/E3 Enzyme (1)

EBI2/GPR183 (2)

Endogenous Metabolite (97)

Endothelin Receptor (6)

Enterovirus (2)

Ephrin Receptor (1)

Epigenetic Reader Domain (1)

ERK (4)

Estrogen Receptor/ERR (27)

Fatty Acid Synthase (FASN) (1)

Ferroptosis (13)

Fungal (4)

FXR (17)

GABA Receptor (39)

GHSR (12)

Glucagon Receptor (28)

Glucocorticoid Receptor (23)

GlyT (1)

GnRH Receptor (4)

GPCR19 (8)

GPR109A (4)

GPR119 (10)

GPR120 (8)

GPR139 (2)

GPR40 (20)

GPR55 (1)

GPR84 (3)

Guanylate Cyclase (4)

HBV (7)

HCV (8)

HCV Protease (2)

HDAC (1)

Hedgehog (1)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (25)

Histone Methyltransferase (4)

HIV (14)

HSV (6)

IFNAR (4)

iGluR (29)

IKK (1)

Imidazoline Receptor (6)

Influenza Virus (11)

Insulin Receptor (2)

Integrin (4)

Interleukin Related (3)

IRE1 (1)

JAK (1)

Leukotriene Receptor (1)

LPL Receptor (24)

LXR (16)

mAChR (34)

MCHR1 (GPR24) (4)

MDM-2/p53 (4)

Melanocortin Receptor (22)

Melatonin Receptor (13)

mGluR (37)

MicroRNA (1)

Mineralocorticoid Receptor (1)

Mitochondrial Metabolism (3)

Mitophagy (3)

MMP (1)

Monoamine Oxidase (1)

Motilin Receptor (2)

nAChR (48)

Neurokinin Receptor (14)

Neuropeptide Y Receptor (29)

Neurotensin Receptor (4)

NF-κB (8)

NKCC (1)

NO Synthase (2)

Notch (1)

Nucleoside Antimetabolite/Analog (2)

Opioid Receptor (80)

Orexin Receptor (OX Receptor) (11)

Oxytocin Receptor (3)

P2X Receptor (3)

P2Y Receptor (9)

PAK (2)

Parasite (16)

PARP (1)

Phosphatase (3)

Phosphodiesterase (PDE) (3)

PKC (2)

Potassium Channel (10)

PPAR (64)

Progesterone Receptor (7)

Prostaglandin Receptor (32)

PROTAC Linker (8)

Protease-Activated Receptor (PAR) (22)

Proteasome (1)

Pyroptosis (1)

RAR/RXR (31)

Reactive Oxygen Species (10)

RET (1)

Reverse Transcriptase (2)

ROR (29)

SARS-CoV (6)

Serotonin Transporter (4)

Sigma Receptor (15)

Sirtuin (3)

Smo (6)

Sodium Channel (5)

Somatostatin Receptor (10)

STAT (2)

STING (15)

TGF-beta/Smad (1)

TGF-β Receptor (1)

Thrombin (2)

Thrombopoietin Receptor (7)

Thyroid Hormone Receptor (10)

TNF Receptor (1)

Toll-like Receptor (TLR) (35)

Trk Receptor (4)

TRP Channel (33)

TSH Receptor (4)

Urotensin Receptor (4)

Vasopressin Receptor (10)

VD/VDR (4)

VEGFR (1)

Virus Protease (4)

Wnt (5)

β-catenin (3)

γ-secretase (1)

By Research Areas:

Cancer (344)

Cardiovascular Disease (184)

Endocrinology (288)

Infection (90)

Inflammation/Immunology (310)

Metabolic Disease (298)

Neurological Disease (667)

1698

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

276

Peptides

185

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-135841

CM10	Aldehyde Dehydrogenase (ALDH)	Cancer Metabolic Disease
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC₅₀s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity.

HY-76006

3-Hydroxybenzaldehyde	Aldehyde Dehydrogenase (ALDH)	Cardiovascular Disease
3-Hydroxybenzaldehyde is a precursor compound for phenolic compounds, such as Protocatechualdehyde (HY-N0295). 3-Hydroxybenzaldehyde is a substrate of **aldehyde dehydrogenase (ALDH)** in rats and humans (ALDH2). 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo.

HY-19801

CVT-10216	Aldehyde Dehydrogenase (ALDH)	Neurological Disease
CVT-10216 is a highly selective, reversible **aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC₅₀** of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC₅₀ of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.

HY-W016645

4-Diethylaminobenzaldehyde	Aldehyde Dehydrogenase (ALDH)	Cancer
4-Diethylaminobenzaldehyde is a reversible **aldehyde dehydrogenases (ALDHs) inhibitor, with a K_i** of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC₅₀= 1.71μM).

HY-122577

EN40
Aldehyde Dehydrogenase (ALDH) Cancer

EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀ value of 2 uM

EN40	Aldehyde Dehydrogenase (ALDH)	Cancer
EN40 is a potent, selective **aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀** value of 2 uM

HY-18768

NCT-501	Aldehyde Dehydrogenase (ALDH)	Cancer
NCT-501 is a potent and selective theophylline-based inhibitor of **aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀** of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM).

HY-W012570

Decyl aldehyde
Endogenous Metabolite Infection

Decyl aldehyde is a simple ten-carbon aldehyde. Decyl aldehyde is a bacterial luciferase substrate.

Decyl aldehyde	Endogenous Metabolite	Infection
Decyl aldehyde is a simple ten-carbon aldehyde. Decyl aldehyde is a bacterial luciferase substrate.

HY-18768A

NCT-501 hydrochloride	Aldehyde Dehydrogenase (ALDH)	Cancer
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of **aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀** of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM).

HY-131633A

(+)-JQ-1-aldehyde	Epigenetic Reader Domain	Cancer
(+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.

HY-136594

BODIPY aminoacetaldehyde BAAA	Aldehyde Dehydrogenase (ALDH)	Cancer
BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.

HY-124011

m-PEG3-aldehyde
PROTAC Linker Cancer

m-PEG3-aldehyde is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
HY-138518

Azido-PEG3-aldehyde
PROTAC Linker Cancer

Azido-PEG3-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-140620

m-PEG4-aldehyde
PROTAC Linker Cancer

m-PEG4-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-133456

Biotin-PEG2-aldehyde
PROTAC Linker Cancer

Biotin-PEG2-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-W020014

Pyruvic aldehyde
Endogenous Metabolite Others

Pyruvic aldehyde is often used as a reagent in organic synthesis, as a flavoring agent, and in tanning.
HY-136051

Biotin-PEG3-aldehyde
ADC Linker Cancer

Biotin-PEG3-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
HY-136077

TCO-PEG3-aldehyde
ADC Linker Cancer

TCO-PEG3-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
HY-136074

Methyltetrazine-PEG4-aldehyde
ADC Linker Cancer

Methyltetrazine-PEG4-aldehyde is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

m-PEG3-aldehyde	PROTAC Linker	Cancer
m-PEG3-aldehyde is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

Azido-PEG3-aldehyde	PROTAC Linker	Cancer
Azido-PEG3-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

m-PEG4-aldehyde	PROTAC Linker	Cancer
m-PEG4-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG2-aldehyde	PROTAC Linker	Cancer
Biotin-PEG2-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Pyruvic aldehyde	Endogenous Metabolite	Others
Pyruvic aldehyde is often used as a reagent in organic synthesis, as a flavoring agent, and in tanning.

Biotin-PEG3-aldehyde	ADC Linker	Cancer
Biotin-PEG3-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

TCO-PEG3-aldehyde	ADC Linker	Cancer
TCO-PEG3-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Methyltetrazine-PEG4-aldehyde	ADC Linker	Cancer
Methyltetrazine-PEG4-aldehyde is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-112277

NCT-505	Aldehyde Dehydrogenase (ALDH)	Cancer
NCT-505 is a potent and selective **aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC₅₀ of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC₅₀**s, >57, 22.8, 20.1, >57 μM).

HY-136054

N3-PEG5-aldehyde
ADC Linker Cancer

N3-PEG5-aldehyde is a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

N3-PEG5-aldehyde	ADC Linker	Cancer
N3-PEG5-aldehyde is a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-B0240

Disulfiram Tetraethylthiuram disulfide; TETD	Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis	Metabolic Disease Cancer
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase *(ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD)* pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells^[1-4].

HY-135977

DBCO-SS-aldehyde
ADC Linker Cancer

DBCO-SS-aldehyde is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
HY-117041

m-PEG4-CH2-aldehyde
PROTAC Linker Cancer

m-PEG4-CH2-aldehyde is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.
HY-133457

Biotin-PEG2-C1-aldehyde
PROTAC Linker Cancer

Biotin-PEG2-C1-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-113165A

Isobutyryl-L-carnitine chloride
Endogenous Metabolite Metabolic Disease

Isobutyryl-L-carnitine chloride is a product of the acyl-CoA dehydrogenases.
HY-136076

TCO-PEG3-CH2-aldehyde
ADC Linker Cancer

TCO-PEG3-CH2-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
HY-W004305

Hexadecanal
PalmitAldehyde
Endogenous Metabolite Metabolic Disease

Hexadecanal (Palmitaldehyde) is a free fatty aldehyde present in animals.

DBCO-SS-aldehyde	ADC Linker	Cancer
DBCO-SS-aldehyde is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

m-PEG4-CH2-aldehyde	PROTAC Linker	Cancer
m-PEG4-CH2-aldehyde is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.

Biotin-PEG2-C1-aldehyde	PROTAC Linker	Cancer
Biotin-PEG2-C1-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Isobutyryl-L-carnitine chloride	Endogenous Metabolite	Metabolic Disease
Isobutyryl-L-carnitine chloride is a product of the acyl-CoA dehydrogenases.

TCO-PEG3-CH2-aldehyde	ADC Linker	Cancer
TCO-PEG3-CH2-aldehyde is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Hexadecanal PalmitAldehyde	Endogenous Metabolite	Metabolic Disease
Hexadecanal (Palmitaldehyde) is a free fatty aldehyde present in animals.

HY-138064

4-APC hydrobromide	Others	Others
4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.

HY-18936

Alda-1
Aldehyde Dehydrogenase (ALDH) Apoptosis Cancer

Alda-1 is a potent ALDH2 agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.
HY-136091

Aldehyde PEG23-thiol
ADC Linker Cancer

Aldehyde PEG23-thiol is a cleavable 23 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
HY-136140

Aldehyde-benzyl-PEG5-alkyne
PROTAC Linker Cancer

Aldehyde-benzyl-PEG5-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Alda-1	Aldehyde Dehydrogenase (ALDH) Apoptosis	Cancer
Alda-1 is a potent *ALDH2* agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.

Aldehyde PEG23-thiol	ADC Linker	Cancer
Aldehyde PEG23-thiol is a cleavable 23 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Aldehyde-benzyl-PEG5-alkyne	PROTAC Linker	Cancer
Aldehyde-benzyl-PEG5-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-N1177

Taraxerone	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
Taraxerone is isolated from Sedum sarmentosum. Taraxerone enhances effects on alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) activities with EC₅₀ values of 512.42 and 500.16 μM, respectively.

HY-133465

Tetrazine-Ph-PEG4-Ph-aldehyde
PROTAC Linker Cancer

Tetrazine-Ph-PEG4-Ph-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Tetrazine-Ph-PEG4-Ph-aldehyde	PROTAC Linker	Cancer
Tetrazine-Ph-PEG4-Ph-aldehyde is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-12465

Z-Ile-Leu-aldehyde Z-IL-CHO; GSI-XII; γ-Secretase inhibitor XII	Notch γ-secretase Apoptosis	Cancer
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of γ-secretase and notch.

HY-33914

4-Hydroxymethylpyrazole	Endogenous Metabolite	Others
4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876). Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase.

HY-N2597

Prunetin	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
Prunetin, an O-methylated isoflavone, possesses anti-inflammatory activity. Prunetin is a potent human aldehyde dehydrogenases inhibitor.

HY-Z0031

(R)-(-)-1,2-Propanediol	Others	Metabolic Disease
(R)-(-)-1,2-Propanediol is a (R)-enantiomer of 1,2-Propanediol that produced from glucose in Escherichia coli expressing NADH-linked glycerol dehydrogenase genes.

HY-B1877

Nitrofen
Others Cancer

Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.

Nitrofen	Others	Cancer
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.

HY-N0018

Daidzin Daidzoside; NPI-031D; Daidzein 7-O-glucoside	Mitochondrial Metabolism Reverse Transcriptase	Others
Daidzin is an isoflavone that has anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.

HY-W012926

Dihydrouracil 5,6-Dihydrouracil	Endogenous Metabolite	Metabolic Disease
Dihydrouracil (5,6-Dihydrouracil), a metabolite of Uracil, can be used as a marker for identification of dihydropyrimidine dehydrogenase (DPD)-deficient.

HY-135658

hDHODH-IN-1	Lactate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
hDHODH-IN-1 is a *human dihydroorotate dehydrogenase* (hDHODH)** inhibitor. hDHODH-IN-1 has anti-inflammatory effect.

HY-126241

RV01	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.

HY-13259

MG-132 Z-Leu-Leu-Leu-al; MG132	Proteasome Autophagy Apoptosis	Cancer
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC₅₀s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.

HY-135282

DHODH-IN-1	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
DHODH-IN-1 (compound 18d) is a potent *Dihydroorotate Dehydrogenase* (DHODH) inhibitor with an IC₅₀** of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway.

HY-114702

M77976	PDHK	Metabolic Disease
M77976 is a specific ATP-competitive inhibitor of *PDK4 (pyruvate dehydrogenase* kinase isoforms 4), with an IC₅₀** of 648 μM. M77976 is potential for the research of obesity and diabetes.

HY-135667

hDHODH-IN-7	Influenza Virus Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
DHODH-IN-9 (Compound 10k) is an azine-bearing analogue and is a human dihydroorotate dehydrogenase inhibitor. DHODH-IN-9 has antiviral effect with a pMIC₅₀ of 7.4.

HY-122737

*RORγt Inverse agonist* 8**	ROR	Inflammation/Immunology
RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC₅₀ of 19 nM for human RORγt-LBD.

HY-130797

TLR7/8 agonist 3
Toll-like Receptor (TLR) Cancer

TLR7/8 agonist 3 is a potent TLR7 and TLR8 agonist, extracted from patent WO2016057618 (compound of formula (II)).

HY-103665

*STING agonist-3*	STING	Cancer
STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING* agonist* with a pEC₅₀ and pIC₅₀ of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

HY-B0876

Fomepizole 4-Methylpyrazole	Cytochrome P450	Metabolic Disease
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.

HY-15394

(Rac)-Rotigotine hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Endocrinology Neurological Disease
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-P1333A

Dynorphin A TFA	Opioid Receptor	Neurological Disease
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).

HY-P1480

Neuropeptide Y (13-36), amide, human Neuropeptide Y (13-36), human	Neuropeptide Y Receptor	Neurological Disease Endocrinology
Neuropeptide Y (13-36), amide, human is a selective neuropeptide Y₂ receptor agonist.

HY-P1334A

DPDPE TFA
Opioid Receptor Neurological Disease

DPDPE TFA, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.

HY-113013

Hydroxypyruvic acid β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid	Endogenous Metabolite	Metabolic Disease
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.

HY-113466

4-Hydroxynonenal 4-HNE	Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite	Cancer Neurological Disease Cardiovascular Disease
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.

HY-113013A

Hydroxypyruvic acid lithium hydrate β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate	Endogenous Metabolite	Metabolic Disease
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.

HY-N2548

Turkesterone	Others	Cardiovascular Disease
Turkesterone, isolated from Ajuga turkestanica, is a potent ecdysteroid. Turkesterone acts as an ecdysteroid receptor (EcR) agonist in some insect systems.

HY-17462

Adrenosterone (+)-Adrenosterone	Androgen Receptor Endogenous Metabolite	Endocrinology
Adrenosterone ((+)-Adrenosterone) is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone also is a selective and competitive inhibitor of *hydroxysteroid (11-beta) dehydrogenase* 1 (HSD11β1)**.

HY-124697

*BMP signaling agonist* sb4**	TGF-β Receptor	Cancer
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC₅₀ value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.

HY-79494

Glyoxalic acid NSC 27785; Formylformic acid; Oxalaldehydic acid	Endogenous Metabolite	Others
Glyoxalic acid (NSC 27785) is an organic compound that is both an aldehyde and a carboxylic acid.

HY-12745A

Nalfurafine hydrochloride TRK-820 hydrochloride	Opioid Receptor	Neurological Disease
Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.

HY-12745

Nalfurafine TRK-820	Opioid Receptor	Neurological Disease
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.

HY-113165

Isobutyryl-L-carnitine
Endogenous Metabolite Metabolic Disease

Isobutyryl-L-carnitine is a product of the acyl-CoA dehydrogenases.

HY-10019

Varenicline CP 526555	nAChR	Neurological Disease
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.

HY-W007330

2-Bromoacetamide
Others Metabolic Disease

2-Bromoacetamide can inactivate alcohol dehydrogenase.
HY-W008393

(-)-Corey lactone diol
Others Others

(-)-Corey lactone diol is a reduced version of corey aldehyde. A building block in the chemical synthesis.
HY-W004307

Octadecanal
Endogenous Metabolite Others

Octadecanal is a long-chain aldehyde, present in both thigh and breast muscle.

HY-N0084

Betulinaldehyde Betulinic Aldehyde; Betunal	Bacterial	Infection Cancer
Betulinaldehyde(Betunal) belongs to pentacyclic triterpenoids and was reported to exhibit antimicrobial activities against bacteria and fungi, including S.

HY-113076

Thiamine pyrophosphate	Endogenous Metabolite	Metabolic Disease
Thiamine pyrophosphate is the coenzyme form of Vitamin B1 and is a required intermediate in the pyruvate dehydrogenase complex and the ketoglutarate dehydrogenase complex.

HY-I0637

Isovanillin 3-Hydroxy-4-methoxybenzAldehyde	Others	Metabolic Disease Neurological Disease
Isovanillin is an aldehyde oxidase inhibitor. Antispasmodic activities. Antidiarrheal activities.

HY-125996

NR1H4 activator 1	FXR	Inflammation/Immunology
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC₅₀ value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.

HY-W011417

Cinnabarinic acid	mGluR Apoptosis	Others
Cinnabarinic acid is a specific orthosteric agonist of mGlu₄ by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.

HY-14302

Salmeterol GR33343X	Adrenergic Receptor	Endocrinology Inflammation/Immunology
Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-17453

Salmeterol xinafoate GR 33343X xinafoate	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-18761

Cobalt phthalocyanine Cobalt(II) phthalocyanine; Cobaltous phthalocyanine; Phthalocyanine cobalt complex	Others	Others
Cobalt phthalocyanine is a catalyst of redox reaction, catalyzes aerobic regenerations of aldehydes and ketones from aldoximes and ketoximes has been developed.

HY-76224

3-Furaldehyde
Others Others

3-Furaldehyde is a member of furans and an aldehyde, and can be used to synthesize the neoclerodane diterpene Salvinorin A.

HY-135119

Salmeterol-D3	Adrenergic Receptor	Endocrinology Inflammation/Immunology
Salmeterol-D3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-12399

MKC9989
IRE1 Cancer

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC₅₀ of 0.23 to 44 μM.

HY-N7624

Methyl oleanonate 3-Oxoolean-12-en-28-oic acid methyl ester	PPAR	Cancer
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.

HY-15453

Devimistat CPI-613	Apoptosis	Cancer
Devimistat (CPI-613) is a lipoic acid analog that inhibits *pyruvate dehydrogenase* (PDH)** and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.

HY-133112

7-Desmethyl-3-hydroxyagomelatine 3-Hydroxy-7-desmethyl agomelatine	Melatonin Receptor 5-HT Receptor	Neurological Disease
7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist.

HY-101198

Clobenpropit dihydrobromide	Histamine Receptor Apoptosis	Cancer Neurological Disease
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.

HY-N0295

Protocatechualdehyde CatechAldehyde; Protocatechuic Aldehyde; Rancinamycin IV	Reactive Oxygen Species Bacterial	Cancer Infection
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent.

HY-P1201

Cyclosomatostatin	Somatostatin Receptor	Cancer
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.

HY-Y0790

Cuminaldehyde	Endogenous Metabolite	Cancer
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.

HY-B1833

Afloqualone HQ-495	GABA Receptor	Neurological Disease
Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous and sedative effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.

HY-101603

Manitimus
FK778
Others Inflammation/Immunology

Manitimus is an inhibitor of dehydroorotate dehydrogenase, and a potent immunosuppressive drug.

HY-Y0015

p-Dimethylaminobenzaldehyde 4-DimethylaminobenzAldehyde	Others	Others
p-Dimethylaminobenzaldehyde (4-Dimethylaminobenzaldehyde) is an organic compound containing amine and aldehyde moieties which is used in Ehrlich's reagent and Kovac's reagent to test for indoles.

HY-129545

DS-1001b	Isocitrate Dehydrogenase (IDH)	Cancer
DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.

HY-129527

GNE-9278	iGluR	Neurological Disease
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.

HY-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with K_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.

HY-P1201A

Cyclosomatostatin TFA	Somatostatin Receptor	Cancer
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.

HY-W012530

Phenylpyruvic acid
Endogenous Metabolite Others

Phenylpyruvic acid is used in the synthesis of 3-phenyllactic acid (PLA) by lactate dehydrogenase.

HY-W008129

H-D-cis-Hyp-OH	Endogenous Metabolite	Metabolic Disease
cis-4-Hydroxy-D-proline is a precursor of conformationally restricted PNA adenine monomer. cis-4-Hydroxy-D-proline can be used to study the specificity and kinetics of D-alanine dehydrogenase.

HY-N2498

Glomeratose A
Lactate Dehydrogenase Others

Glomeratose A is a lactate dehydrogenase inhibitor, isolated from Polygala tenuifolia.
HY-101966

NCT-503
Others Cancer

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC₅₀ of 2.5 µM.
HY-112645

BAY-2402234
Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer

BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.

HY-103476

Ro15-4513	GABA Receptor	Neurological Disease
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.

HY-B0083

Leflunomide HWA486; RS-34821; SU101	Others	Cancer
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.

HY-100020

BAY-1436032
Isocitrate Dehydrogenase (IDH) Cancer

BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

HY-W011094

Win 18446	Aldehyde Dehydrogenase (ALDH)	Endocrinology
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC₅₀ of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.

HY-17038A

Agomelatine hydrochloride S-20098 hydrochloride	Melatonin Receptor 5-HT Receptor	Neurological Disease
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-17038

Agomelatine S-20098	Melatonin Receptor 5-HT Receptor	Neurological Disease
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-P2161

TAK-683	Others	Cancer
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC₅₀=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC₅₀ values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.

HY-13673

Goserelin ICI 118630	GnRH Receptor Apoptosis	Cancer Endocrinology
Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.

HY-13673A

Goserelin acetate ICI-118630 acetate	GnRH Receptor Apoptosis	Endocrinology Cancer
Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.

HY-B1021

Vincamine	GPR40	Metabolic Disease Cardiovascular Disease
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40* agonist* and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.

HY-17038B

Agomelatine (L(+)-Tartaric acid) S-20098 L(+)-Tartaric acid	Melatonin Receptor 5-HT Receptor	Neurological Disease
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-14281

Trilostane
Win 24540
Others Endocrinology Cancer

Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.

HY-100991

FG 7142 ZK 39106; LSU-65	GABA Receptor	Neurological Disease
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (K_i=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC₅₀= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.

HY-100742B

(S)-GNE-140
Lactate Dehydrogenase Cancer

(S)-GNE-140 is the less active enantiomer of GNE-140 which can inhibit Lactate dehydrogenase A (LDHA).

HY-13986

Merimepodib VX-497; MMPD	HBV HCV	Infection
Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.

HY-77521

Dabigatran ethyl ester hydrochloride	Thrombin	Cardiovascular Disease
Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC₅₀ value of 0.8 μM and a thrombin inhibitor.

HY-W014787

Decanedioic acid	Endogenous Metabolite	Metabolic Disease
Decanedioic acid, a normal urinary acid, is found to be associated with carnitine-acylcarnitine translocase deficiency and medium chain acyl-CoA dehydrogenase deficiency.

HY-124062

TAS-114
Others Cancer

TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.

HY-133023

Indium(III) isopropoxide	Others	Others
Indium(III) Isopropoxide is an organo-metallic compound. Indium(III) Isopropoxide uesd as a hydrogen transfer catalyst for conversion of benzylic alcohols into aldehydes or ketones via Oppenauer oxidation. Indium(III) Isopropoxide also can be used as metal precursor.

HY-100681

GSK2837808A
Lactate Dehydrogenase Cancer

GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC₅₀s of 1.9 and 14 nM for LDHA and LDHB, respectively.

HY-135676

DHODH-IN-12	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
DHODH-IN-12 (Compound 12b) is a Leflunomide derivative and a weak *dihydroorotate dehydrogenase* (DHODH) inhibitor with a pK_a** of 5.07.

HY-103096

R162
Others Cancer

R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
HY-119459

Fluopyram
Fungal Infection

Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC₅₀ of 3.35 µg/mL.

HY-111095

D-(-)-Lactic acid (R)-2-Hydroxypropionic acid	Endogenous Metabolite	Metabolic Disease
D-(-)-Lactic acid is a normal intermediate in the fermentation (oxidation, metabolism) of sugar. D-(-)-Lactic acid is identified to be a competitive inhibitor of ProDH (proline dehydrogenase) in plants.

HY-135675

DHODH-IN-11	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak *dihydroorotate dehydrogenase* (DHODH) inhibitor with a pK_a** of 5.03.

HY-B0199

Mycophenolate Mofetil RS 61443; TM-MMF	Apoptosis	Cancer
Mycophenolate Mofetil is an immunosuppressant, a non-competitive, selective and reversible inhibitor of *inosine monophosphate dehydrogenase* (IMPDH) with IC₅₀**s of 39 nM and 27 nM, respectively.

HY-N6736

K-252c	PKC Bacterial Apoptosis	Cancer Infection
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC₅₀ of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.

HY-W001187

Tempo	DNA/RNA Synthesis Reactive Oxygen Species Mitochondrial Metabolism	Cancer
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects.

HY-111108

LDH-IN-1
Lactate Dehydrogenase Cancer

LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC₅₀s of 32 and 27 nM for LDHA and LDHB, respectively.

HY-113304

(S)-3,4-Dihydroxybutyric acid	Endogenous Metabolite	Metabolic Disease
(S)-3,4-Dihydroxybutyric acid is a normal human urinary metabolite that is excreted in increased concentration in patients with succinic semialdehyde dehydrogenase (SSADH) deficiency.

HY-W001941

D-Cystine
Others Others

D-Cystine is the D-enantiomer of L-Cystine. D-Cystine inhibits L-aspartate-β-semialdehyde dehydrogenase (ASADH) from Escherichia coli.

HY-113128

sn-Glycerol 3-phosphate	Endogenous Metabolite	Others
sn-Glycerol 3-phosphate is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.

HY-N7961

(E/Z)-Ginkgolic acid C17:2	Dihydroorotate Dehydrogenase	Others
(E/Z)-Ginkgolic acid C17:2, isolated from Ginkgo biloba, can bind with human *dihydroorotate dehydrogenase* (DHODH)** tightly.

HY-18055

BVT-14225
Others Metabolic Disease

BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 52 nM.

HY-113128A

sn-Glycerol 3-phosphate lithium	Endogenous Metabolite	Metabolic Disease
sn-Glycerol 3-phosphate lithium is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.

HY-18053

AZD 4017
Others Metabolic Disease

AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC₅₀ of 7 nM.

HY-113166

Dodecanoylcarnitine	Endogenous Metabolite	Metabolic Disease
Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.

HY-113128B

sn-Glycerol 3-phosphate biscyclohexylammonium salt	Endogenous Metabolite	Metabolic Disease
sn-Glycerol 3-phosphate biscyclohexylammonium salt is produced by cytosolic glycerol 3-phosphate dehydrogenase pathway through the reduction of dihydroxyacetone phosphate using NADH formed during glycolysis.

HY-16214

FX-11 LDHA Inhibitor FX11	Lactate Dehydrogenase Apoptosis	Cancer
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC₅₀ of 23.3 μM for HeLa cell and a K_i value of 8 μM.

HY-17469

Gimeracil Gimestat	Others	Cancer
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of *DPYD (dihydropyrimidine dehydrogenase, DPD)*.

HY-108325

Brequinar DUP785; NSC 368390	Dihydroorotate Dehydrogenase Virus Protease DNA/RNA Synthesis	Cancer Infection Inflammation/Immunology
Brequinar (DUP785) is a potent inhibitor of *dihydroorotate dehydrogenase* (DHODH) with an IC₅₀ of 5.2 nM for human DHODH**. Brequinar has potent activities against a broad spectrum of viruses.

HY-B2004

Thifluzamide	Fungal	Infection
Thifluzamide, a broad-spectrum succinate dehydrogenase inhibitor (SDHI) fungicide, has been widely used in the controlling of a variety of fungal diseases in rice fields.

HY-N7114A

Chloramphenicol succinate sodium	Bacterial Antibiotic	Metabolic Disease Infection
Chloramphenicol succinate sodium is a prodrug of Chloramphenicol, with Haemotoxicity. Chloramphenicol succinate is a competitive substrate and inhibitor of succinate dehydrogenase (SDH) that is the possible reason for its toxicity.

HY-135570

hDHODH-IN-3	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus	Infection
hDHODH-IN-3 (compound 21d) is a *human dihydroorotate dehydrogenase* (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC₅₀** value of 8.6.

HY-12688

Succinyl phosphonate	Endogenous Metabolite Reactive Oxygen Species	Neurological Disease
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.

HY-135664

hDHODH-IN-5	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
DHODH-IN-7 is a human *dihydroorotate dehydrogenase* (DHODH) inhibitor, with an IC₅₀** of 0.91 μM. DHODH-IN-7 induces differentiation in acute myeloid leukemia.

HY-W040073

Nifurtimox	Parasite Lactate Dehydrogenase	Cancer Infection
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

HY-N2337

11beta-Hydroxyprogesterone 11β-Hydroxyprogesterone	Endogenous Metabolite	Cardiovascular Disease
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED₅₀ of 10 nM.

HY-129630

Tetrahydrocortisol	Endogenous Metabolite	Metabolic Disease
Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity.

HY-12688A

Succinyl phosphonate trisodium salt	Endogenous Metabolite Reactive Oxygen Species	Cancer Metabolic Disease Neurological Disease
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.

HY-18717

Mutant IDH1-IN-2	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.

HY-100742

GNE-140 racemate	Lactate Dehydrogenase	Cancer
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent *lactate dehydrogenase* A (LDHA)** inhibitor.

HY-137463

AG-636	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
AG-636 is a potent, reversible, selective and orally active *dihydroorotate dehydrogenase* (DHODH) inhibitor with an IC₅₀** of 17 nM. AG-636 has strong anticancer effects.

HY-128578

KPLH1130	PDHK	Metabolic Disease Inflammation/Immunology
KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.

HY-126256

PRMT5-IN-1	Histone Methyltransferase	Cancer
PRMT5 IN-1, a hemiaminal, is a covalent protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.

HY-135654

hDHODH-IN-2	Lactate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
hDHODH-IN-2 is an analogue of the active metabolite of Leflunomide. hDHODH-IN-2 is a *human dihydroorotate dehydrogenase* (hDHODH)** inhibitor. hDHODH-IN-1 has anti-inflammatory activity.

HY-107977

IDH1 Inhibitor 3
Isocitrate Dehydrogenase (IDH) Cancer

IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC₅₀ of 45 nM for IDH1^R132H.

HY-W017522

Adipic acid	Endogenous Metabolite	Metabolic Disease
Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.

HY-135648

PfDHODH-IN-1	Parasite Lactate Dehydrogenase DNA/RNA Synthesis	Infection
PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity.

HY-W012875

3-Nitropropanoic acid β-Nitropropionic acid; Bovinocidin	Bacterial Apoptosis	Infection Metabolic Disease
3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM.

HY-120924

BRD9185	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
BRD9185 is a *Dihydroorotate dehydrogenase* (DHODH) inhibitor, with an EC₅₀** of 16 nM against multidrug-resistant blood-stage parasites in vitro and is curative after just three doses in a P. berghei mouse model.

HY-113212

Ursocholic acid	Endogenous Metabolite	Metabolic Disease
Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.

HY-136498

T-705RMP	Drug Metabolite	Infection
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC₅₀ of 601 μM.

HY-N3115

Palbinone	Others	Inflammation/Immunology
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits *3α-hydroxysteroid dehydrogenase* (3α-HSD), with an IC₅₀** of 46 nM. Anti-inflammatory activity.

HY-101943

LY 345899	Others	Cancer
LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC₅₀ values of 96 nM and 663 nM, respectively and a K_i of 18 nM for MTHFD1.

HY-117240

NCT-502	Others	Cancer
NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC₅₀ of 3.7 μM against PHGDH.

HY-16082

AZD7545	PDHK	Metabolic Disease
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC₅₀s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.

HY-138097

α-NETA	Aldehyde Dehydrogenase (ALDH) AChE Apoptosis	Cancer
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity.

HY-113108

(R)-3-Hydroxyisobutyric acid	Endogenous Metabolite	Metabolic Disease
(R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.

HY-108012

ME1111	Fungal	Infection
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research.

HY-128787

hDHODH-IN-4	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus	Infection
hDHODH-IN-4 is a potent human *dihydroorotate dehydrogenase* (DHODH) inhibitor, with a pIC₅₀ of 7.8 for human recombinant DHODH. hDHODH-IN-4 inhibits measles virus replication, with a pMIC₅₀** of 8.8.

HY-100742A

(R)-GNE-140	Lactate Dehydrogenase	Cancer
(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC₅₀s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

HY-101930

BMS-816336	Others	Metabolic Disease
BMS-816336 is a novel, potent and orally bioavailable inhibitor against *human 11β-hydroxysteroid dehydrogenase* type 1 (11β-HSD1) enzyme with an IC₅₀** of 3.0 nM.

HY-19540

GSK864	Isocitrate Dehydrogenase (IDH)	Cancer
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC₅₀ values of 8.8, 15.2 and 16.6 nM.

HY-W051723

(R)-3-Hydroxybutanoic acid (R)-(-)-3-Hydroxybutanoic acid; (R)-3-Hydroxybutyric acid	Endogenous Metabolite	Others
(R)-3-Hydroxybutanoic acid is a metabolite, and converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid has applications as a nutrition source and as a precursor for vitamins, antibiotics and pheromones.

HY-W078844

PfDHODH-IN-2	Dihydroorotate Dehydrogenase Parasite	Infection
PfDHODH-IN-2, a dihydrothiophenone derivative (Compound 11), is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC₅₀ of 1.11 µM. PfDHODH-IN-2 acts as an antimalarial agent and can be used for the research of malaria.

HY-10533

Eniluracil 5-Ethynyluracil; GW776C85	Others	Cancer
Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of *dihydropyrimidine dehydrogenase* (DPD)**, increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.

HY-12492

VER-246608	PDHK	Cancer
VER-246608 is a potent and ATP-competitive inhibitor of *pyruvate dehydrogenase* kinase (PDK) with IC₅₀s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4**, respectively.

HY-100184

DSM265	Dihydroorotate Dehydrogenase Parasite	Infection
DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC₅₀ of 4.3 nM.

HY-114009

AKR1C1-IN-1
Others Neurological Disease

AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a K_i value of 4 nM for AKR1C1.

HY-135678

DHODH-IN-14	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
DHODH-IN-14 (Compound 7l) is a hydroxyfurazan analog of A771726. DHODH-IN-14 is a *dihydroorotate dehydrogenase* (DHODH) inhibitor with an IC₅₀ of 0.49 μM for rat liver DHODH**. DHODH-IN-14 can be used for rheumatoid arthritis.

HY-135677

DHODH-IN-13	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
DHODH-IN-13 (Compound 7a) is a hydroxyfurazan analog of A771726. DHODH-IN-13 is a *dihydroorotate dehydrogenase* (DHODH) inhibitor with an IC₅₀ of 4.3 μM for rat liver DHODH**. DHODH-IN-13 can be used for rheumatoid arthritis.

HY-135679

DHODH-IN-15	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Inflammation/Immunology
DHODH-IN-15 (Compound 7b) is a hydroxyfurazan analog of A771726. DHODH-IN-15 is a *dihydroorotate dehydrogenase* (DHODH) inhibitor with an IC₅₀ of 11 μM for rat liver DHODH**. DHODH-IN-15 can be used for rheumatoid arthritis.

HY-135619

DHODH-IN-4	Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection Inflammation/Immunology
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum *dihydroorotate dehydrogenase* (DHODH) inhibitor, with IC₅₀** values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity.

HY-Y0445A

Sodium dichloroacetate	PDHK Reactive Oxygen Species NKCC Apoptosis	Cancer
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.

HY-135618

DHODH-IN-3	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC₅₀ value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a K_i^app of 32 nM. DHODH-IN-3 has the potential for malaria treatment.

HY-101232

Tiotidine ICI 125211	Histamine Receptor	Cardiovascular Disease
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA₂=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.

HY-123962

G6PD activator AG1	Others	Metabolic Disease
G6PD activator AG1 is a potent and selective *glucose-6-phosphate dehydrogenase* (G6PD) activator with an EC₅₀** of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.

HY-B1729

Phenoxyethanol	Bacterial	Infection
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.

HY-100688

ML390	Dihydroorotate Dehydrogenase	Cancer
ML390 is a potent *dihydroorotate dehydrogenase* (DHODH)** inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models.

HY-109619

D4-abiraterone Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite	Androgen Receptor Cytochrome P450	Cancer
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.

HY-N2177

3-Dehydrotrametenolic acid	Lactate Dehydrogenase Apoptosis	Cancer
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a *lactate dehydrogenase* (LDH)** inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity.

HY-N7393

Isomalt Palatinitol	Lactate Dehydrogenase	Metabolic Disease
Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes *lactate dehydrogenase* (LDH)** moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes.

HY-W040307

Saccharopine L-Saccharopine	Endogenous Metabolite	Metabolic Disease
Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis.

HY-W015851

(R)-3-Hydroxybutanoic acid sodium (R)-(-)-3-Hydroxybutanoic acid sodium; (R)-3-Hydroxybutyric acid sodium	Endogenous Metabolite	Neurological Disease
(R)-3-Hydroxybutanoic acid sodium ((R)-3-Hydroxybutyric acid) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium has applications as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones.

HY-114459

Mutant IDH1-IN-4	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-4 (compound 434) is an inhibitor of *mutant Isocitrate dehydrogenase* 1 (IDH 1), with IC₅₀** values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.

HY-126254

BI-4924	Others	Cancer
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC₅₀=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC₅₀ of 2200 nM at 72 h.

HY-103394

TC HSD 21	Others	Cancer
TC HSD 21 is a potent *17β-hydroxysteroid dehydrogenase* type 3 (17β-HSD3) inhibitor with an IC₅₀** of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.

HY-135666

DHODH-IN-8	Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC₅₀s of 0.13 μM and 47.4 μM, and K_is of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity.

HY-133898

Danavorexton
Orexin Receptor (OX Receptor) Others

Danavorexton is an orexin receptor agonist.
HY-14234

Glucocorticoid receptor agonist
Glucocorticoid Receptor Metabolic Disease Endocrinology

Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.

HY-12762

QS11	Others	Cancer
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC₅₀ of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.

HY-123943

*STING agonist-4*	STING	Cancer
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC₅₀) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function.

HY-13423

Tenovin-1	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a *dihydroorotate dehydrogenase* (DHODH)** inhibitor.

HY-130251

DS18561882	Others	Cancer
DS18561882 is a highly potent, isozyme-selective *methylenetetrahydrofolate dehydrogenase* 2 (MTHFD2) inhibitor with an IC₅₀ value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC₅₀**=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.

HY-N0157

Orotic acid 6-Carboxyuracil; Vitamin B13	Nucleoside Antimetabolite/Analog Endogenous Metabolite	Metabolic Disease
Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats.

HY-N0157A

Orotic acid zinc	Nucleoside Antimetabolite/Analog Endogenous Metabolite	Metabolic Disease
Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats.

HY-131145

Brombuterol hydrochloride Bromobuterol hydrochloride	Adrenergic Receptor	Inflammation/Immunology
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist.

HY-112921B

*diABZI STING agonist-1 trihydrochloride*	STING	Inflammation/Immunology Cancer
diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

HY-112921A

*diABZI STING agonist-1*	STING	Inflammation/Immunology
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

HY-100699

Clenproperol
Adrenergic Receptor Endocrinology

Clenproperol is a β2-adrenergic agonist.
HY-118539

NSC12404
LPL Receptor Others

NSC12404 is a weak and specific LPA₂ receptor agonist.

HY-131974

*Glucocorticoid receptor agonist-1*	Glucocorticoid Receptor	Inflammation/Immunology
Glucocorticoid receptor agonist-1 is a potent glucocorticoid receptor agonist with an IC₅₀ of 2.8 nM extracted from patent WO2017210471A1, compound 41.

HY-126321

*RORγt agonist* 1**	ROR	Cancer
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC₅₀ of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.

HY-113377

L-Glyceric acid	Endogenous Metabolite	Metabolic Disease
L-Glyceric acid is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid excretion to distinguish PH1 from PH2.

HY-113377A

L-Glyceric acid sodium	Endogenous Metabolite	Metabolic Disease
L-Glyceric acid sodium is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid sodium can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid sodium excretion to distinguish PH1 from PH2.

HY-114400A

TRPV4 agonist-1
Inflammation/Immunology

TRPV4 agonist-1 is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC₅₀ of 60 nM in the hTRPV4 Ca²⁺ assay.

HY-B2245

Estradiol dipropionate	Estrogen Receptor/ERR Progesterone Receptor	Endocrinology
Estradiol dipropionate is a combined estrogen-progesterone, acts as an estrogen and progesterone agonist.

HY-107399

CD3254
RAR/RXR Cancer Metabolic Disease

CD3254 a potent and selective retinoid-X-receptor (RXR) agonist.
HY-17354A

(R)-Baclofen hydrochloride
STX 209 hydrochloride
GABA Receptor Neurological Disease

(R)-Baclofen hydrochloride (STX 209 hydrochloride) is a selective GABAB receptor agonist.
HY-17354

(R)-Baclofen
STX209
GABA Receptor Neurological Disease

(R)-Baclofen(STX209) is a selective GABAB receptor agonist.
HY-P0236A

Neurokinin A(4-10) TFA
Neurokinin Receptor Neurological Disease Endocrinology

Neurokinin A (4-10) TFA is a tachykinin NK₂ receptor agonist.
HY-110304

NPEC-caged-LY379268
mGluR Neurological Disease

NPEC-caged-LY379268 is a type II mGluR agonist.
HY-136435

Mapenterol hydrochloride
Adrenergic Receptor Endocrinology

Mapenterol hydrochloride is a type of β2-adrenoceptor agonist.

HY-10545

Taribavirin	HBV HCV	Infection
Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.

HY-18767

Ivosidenib AG-120	Isocitrate Dehydrogenase (IDH)	Cancer Metabolic Disease
Ivosidenib (AG-120) is an orally active inhibitor of *isocitrate dehydrogenase* 1 mutant (mIDH1) enzyme**, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.

HY-129239

ASLAN003	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Apoptosis	Cancer
ASLAN003 is an orally active and potent *Dihydroorotate Dehydrogenase* (DHODH) inhibitor with an IC₅₀ of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis** and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.

HY-10545A

Taribavirin hydrochloride	HBV HCV	Infection
Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.

HY-101930B

(R)-BMS-816336	Others	Metabolic Disease
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and *cynomolgus monkey 11β-hydroxysteroid dehydrogenase* type 1 (11β-HSD1) enzyme with IC₅₀**s of 14.5 nM, 50.3 nM and 16 nM, respectively .

HY-112921

*diABZI STING agonist-1 (Tautomerism)*	STING	Inflammation/Immunology
diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

HY-111358

TLR7 agonist 1
Toll-like Receptor (TLR) Infection

TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC₅₀ of 90 nM.

HY-114400

*TRPV4 agonist-1 free base*	TRP Channel	Inflammation/Immunology
TRPV4 agonist-1 free base is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC₅₀ of 60 nM in the hTRPV4 Ca²⁺ assay.

HY-128855

Talsaclidine	mAChR	Neurological Disease
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.

HY-19574

FPR Agonist 43
Others Inflammation/Immunology

FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.
HY-135400

Glyco-Obeticholic acid
FXR Inflammation/Immunology

Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.

HY-126293

*Apelin agonist* 1**	Others	Cardiovascular Disease
Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0.

HY-N0108

Physcion Parietin; Rheochrysidin	Bacterial	Cancer Infection Inflammation/Immunology
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC₅₀ and a K_d of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.

HY-13239

LY2979165
mGluR Neurological Disease

LY2979165 is the alanine prodrug of 2812223, a selective and potent orthosteric mGlu2 receptor agonist.
HY-N9333

Wistin
PPAR Cancer Metabolic Disease

Wistin, isolated from Caragana sinica roots, is a PPARα and PPARγ agonist.
HY-112597

Pparδ agonist
PPAR Metabolic Disease

PPARδ agonist is a PPARδ agonist extracted from patent US20180071304, compound example 10.
HY-131105S

Cimbuterol-D9
Adrenergic Receptor Cardiovascular Disease

Cimbuterol-D9 is the deuterium labeled Cimbuterol. Cimbuterol is aβ-adrenergic agonist.
HY-100120

Pparδ agonist 2
PPAR Metabolic Disease

Pparδ agonist 2 is a PPARδ agonist extracted from patent WO 2016057656 A1.
HY-P1738

[Sar9] Substance P
Neurokinin Receptor Neurological Disease Endocrinology

[Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist.

HY-109131

Foscarbidopa Carbidopa 4′-monophosphate	Dopamine Receptor	Neurological Disease
Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist.

HY-102053

Apimostinel
NRX-1074; AGN-241660
iGluR Neurological Disease

Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist.

HY-135399

Tauro-Obeticholic acid	FXR	Inflammation/Immunology
Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.

HY-135954A

PDK4-IN-1 hydrochloride	PDHK Apoptosis	Cancer Metabolic Disease Inflammation/Immunology
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active *pyruvate dehydrogenase* kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis**. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.

HY-101813

Laflunimus HR325	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Prostaglandin Receptor	Inflammation/Immunology
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of *dihydroorotate dehydrogenase* (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC₅₀ values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1** and -2 inhibitor.

HY-W010342

6-Aminonicotinamide	Others	Cancer
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP⁺-dependent enzyme *glucose-6-phosphate dehydrogenase* (G6PD) inhibitor (K_i**=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.

HY-135954

PDK4-IN-1	PDHK Apoptosis	Cancer Metabolic Disease Inflammation/Immunology
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active *pyruvate dehydrogenase* kinase 4 (PDK4) inhibitor with an IC₅₀ value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis**. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.

HY-124593

PTC299	VEGFR Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Cancer
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of *dihydroorotate dehydrogenase* (DHODH)**. PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.

HY-18056

PF-915275	Others	Metabolic Disease
PF-915275 is a potent, selective and orally active *human 11β-hydroxysteroid dehydrogenase* type 1 (11βHSD1) inhibitor with a K_i of 2.3 nM and an EC₅₀ of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC₅₀** of 20 and 100 nM, respectively.

HY-111353

GPR120 Agonist 2
GPR120 Metabolic Disease

GPR120 Agonist 2 is a GPR120 agonist extracted from patent US 20110313003 A1, example 209.
HY-19673A

KUL-7211 racemate
Adrenergic Receptor Endocrinology

KUL-7211 racemate is the racemate of KUL-7211. KUL-7211 is a selective β-adrenoceptor agonist.

HY-107688A

UB-165 fumarate	nAChR	Neurological Disease
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for nicotine binding in rat brain.

HY-135982

*GPR81 agonist* 1**	Others	Metabolic Disease
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC₅₀s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.

HY-131104S

Brombuterol D9 Bromobuterol D9	Adrenergic Receptor	Inflammation/Immunology
Brombuterol D9 (Bromobuterol D9) is a deuterium labeled Brombuterol. Brombuterol is a β-adrenergic receptor agonist.

HY-111748

RORγt Inverse agonist 2
ROR Inflammation/Immunology

RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC₅₀ of 119 nM.
HY-103039

TLR7 agonist 2
Toll-like Receptor (TLR) Inflammation/Immunology

TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

HY-136449

Bromchlorbuterol hydrochloride	Adrenergic Receptor	Inflammation/Immunology
Bromchlorbuterol hydrochloride is an active β-adrenergic agonist (β-agonist) and can be used for the research of pulmonary disease and asthma.

HY-100699S

Clenproperol-D7
Adrenergic Receptor Endocrinology

Clenproperol-D7 is the deuterium labeled Clenproperol. Clenproperol is a β2-adrenergic agonist.
HY-P1144

Oxyntomodulin
Glucagon Receptor Metabolic Disease

Oxyntomodulin, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.
HY-U00395

GPR40 Agonist 2
GPR40 Metabolic Disease

GPR40 Agonist 2 is a GPR40 agonist that can be used in the research of diabetes, extracted from patent WO2009054479A1.

HY-131104AS

Brombuterol D9 hydrochloride Bromobuterol D9 hydrochloride	Adrenergic Receptor	Inflammation/Immunology
Brombuterol D9 hydrochloride (Bromobuterol D9 hydrochloride) is a deuterium labeled Brombuterol hydrochloride. Brombuterol hydrochloride is a β-adrenergic receptor agonist.

HY-100087

Budesonide impurity C	Glucocorticoid Receptor	Cancer Inflammation/Immunology
Budesonide impurity C is an impurity of Budesonide. Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist.

HY-10020

Varenicline Hydrochloride CP 526555 hydrochloride	nAChR	Neurological Disease
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a K_i value of 0.12 nM.

HY-100012

CBR-5884	Others	Cancer
CBR-5884 is an active, selective inhibitor of *phosphoglycerate dehydrogenase* (PHGDH) with an IC₅₀ of 33 μM. CBR-5884 inhibits de novo serine synthesis** in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.

HY-18173

AZD8329	Others	Metabolic Disease
AZD8329 is a potent *11β-Hydroxysteroid dehydrogenase* type 1 (11β-HSD1) inhibitor with an IC₅₀** of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.

HY-111359

GPR40 agonist 1
GPR40 Metabolic Disease

GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC₅₀ of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
HY-103083

GPR40 agonist 4
GPR40 Metabolic Disease

GPR40 agonist 4 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC₅₀ of 7.54.
HY-P1144A

Oxyntomodulin TFA
Glucagon Receptor Metabolic Disease

Oxyntomodulin TFA, a 37-amino acid peptide hormone, is a glucagon-like peptide 1 (GLP-1) receptor agonist.

HY-101039A

AR-M 1000390 hydrochloride	Opioid Receptor	Neurological Disease
AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC₅₀ of 7.2±0.9 nM for δ agonist potency.

HY-112679

GLP-1 receptor agonist 2
Glucagon Receptor Others

GLP-1 receptor agonist 2 is a glucagon-like peptide-1 receptor (GLP-1R) agonist.
HY-13288

Org 27569
Cannabinoid Receptor Neurological Disease

Org 27569 is a potent CB1 receptor allosteric modulator, which increases agonist binding, yet blocks agonist-induced CB1 signaling.

HY-108415

Cloprostenol sodium salt ICI 80996 sodium salt	Prostaglandin Receptor	Endocrinology
Cloprostenol sodium salt (ICI 80996 sodium salt) is a potent synthetic prostaglandin analogue, acts as a luteolytic agent, and is a PGF2α receptor agonist.

HY-19522

Seladelpar
MBX-8025
PPAR Metabolic Disease

Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC₅₀ 2 nM), and specific PPAR-δ agonist.
HY-U00340

PPAR agonist 1
PPAR Metabolic Disease

PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.

HY-111583

*RXFP3/4 agonist* 1**	Others	Metabolic Disease
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC₅₀s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.

HY-19711

*STING agonist-1* G10	STING Virus Protease	Infection
STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC₉₀ of 24.57 μM.

HY-128353

*ROR agonist-1*	ROR	Inflammation/Immunology
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary T_H 17 cells with a pIC₅₀ of 7.5.

HY-17405

Alarelin Acetate
Alarelin
GnRH Receptor Endocrinology

Alarelin acetate is a synthetic GnRH agonist.
HY-100810

Isoguvacine hydrochloride
GABA Receptor Neurological Disease

Isoguvacine hydrochloride is a GABA receptor agonist.

HY-13653

(-)-Epigallocatechin Gallate EGCG; Epigallocatechol Gallate	Autophagy Reactive Oxygen Species HIV Ferroptosis Mitochondrial Metabolism Endogenous Metabolite	Cancer
(-)-Epigallocatechin Gallate is a tea flavonoid with potent antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects. (-)-Epigallocatechin Gallate (EGCG) is a *glutamate dehydrogenase* 1/2 (GDH1/2, GLUD1/2) inhibitor. Epigallocatechin-3-gallate induces oxidative phosphorylation (OXPHOS**) by activating cytochrome c oxidase.

HY-15510B

Tenovin-6 Hydrochloride	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits *dihydroorotate dehydrogenase* (DHODH)**.

HY-114226

Olutasidenib FT-2102	Isocitrate Dehydrogenase (IDH)	Cancer Inflammation/Immunology
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of *mutant Isocitrate dehydrogenase* 1 (IDH1), with IC₅₀** values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .

HY-114855

BT2	Bcl-2 Family	Metabolic Disease
BT2 is a BCKDC kinase (BDK) inhibitor with an IC₅₀ of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a K_i value of 59 μM.

HY-15510

Tenovin-6	MDM-2/p53 Dihydroorotate Dehydrogenase Sirtuin Autophagy	Cancer
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC₅₀s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits *dihydroorotate dehydrogenase* (DHODH)**.

HY-12405

CGP-42112
CGP42112A
Angiotensin Receptor Neurological Disease Endocrinology

CGP-42112 (CGP-42112A) is a potent Angiotensin-II subtype 2 receptor(AT2 R) agonist.
HY-112185

GLP-1 receptor agonist 1
Glucagon Receptor Metabolic Disease

GLP-1 receptor agonist 1 is a GLP-1 receptor agonist extracted from patent WO2018056453A1, Compound 67.

HY-108711

*GPR120 Agonist* 1**	GPR120	Metabolic Disease
GPR120 Agonist 1 is a potent and selective GPR120 agonist, and possesses promising antidiabetic effect and good safety profile to be a development candidate.

HY-136608

5-AAM-2-CP
nAChR Neurological Disease

5-AAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist.
HY-136609

5-AMAM-2-CP
nAChR Neurological Disease

5-AMAM-2-CP is a major metabolite of Acetamiprid. Acetamiprid is a neonicotinoid insecticide used worldwide and is a nAChR agonist.

HY-100469

*LXRβ agonist-2*	LXR	Cardiovascular Disease
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC₅₀ of 7 nM, displays 28.5-fold selectivity over LXRα (EC₅₀=200 nM) and used in the treatment of atherosclerosis.

HY-B1161

Methoprene ZR-515	Others	Infection
Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist.

HY-12835

S1P1 Agonist III
LPL Receptor Inflammation/Immunology

S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.
HY-42068

(-)-Aspartic acid
(R)-Aspartic acid; D-(-)-Aspartic acid
Endogenous Metabolite iGluR Neurological Disease

(-)-Aspartic acid is an endogenous NMDA receptor agonist.

HY-B1829A

Dexamethasone phosphate disodium Dexamethasone 21-phosphate disodium salt	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Dexamethasone phosphate disodium is a glucocorticoid receptor agonist.

HY-101717

Indanidine
Adrenergic Receptor Cardiovascular Disease Endocrinology

Indanidine is an alpha-adrenergic agonist.
HY-U00281

S16961
S169611
nAChR Neurological Disease

S16961 is a nicotinic receptor agonist.
HY-U00227

U91356
Dopamine Receptor Neurological Disease

U91356 is a dopamine receptor agonist.

HY-13660

Mocravimod hydrochloride KRP-203	LPL Receptor	Inflammation/Immunology
Mocravimod hydrochloride (KRP-203), an immunosuppressant, is a potent and orally active S1PR1 (sphingosine 1-phosphate receptor type 1) agonist.

HY-100234A

DREADD agonist 21 dihydrochloride
mAChR Neurological Disease

DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC₅₀=1.7 nM).

HY-109136

Runcaciguat	Guanylate Cyclase	Cardiovascular Disease
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.

HY-100234

DREADD agonist 21
mAChR Neurological Disease

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC₅₀=1.7 nM).

HY-W002116

Methyl syringate	TRP Channel	Inflammation/Immunology
Methyl syringate, a chemical marker of asphodel monofloral honey, is an efficient phenolic mediator for bacterial and fungal laccases. Methyl syringate is a TRPA1 agonist.

HY-B0968A

Trimetazidine	Autophagy	Cardiovascular Disease
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC₅₀ of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a *3-hydroxyacyl-CoA dehydrogenase* (HADHA)** inhibitor.

HY-B0968

Trimetazidine dihydrochloride	Autophagy	Cardiovascular Disease
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC₅₀ of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a *3-hydroxyacyl-CoA dehydrogenase* (HADHA)** inhibitor.

HY-101265

*S1p receptor agonist* 1**	LPL Receptor	Inflammation/Immunology
S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC₅₀=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.

HY-130243

*RORγt Inverse agonist* 6**	ROR	Inflammation/Immunology
RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

HY-114310

*VDR agonist* 1**	VD/VDR Apoptosis	Cancer
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC₅₀ of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.

HY-108566

U-46619 9,11-Methanoepoxy PGH2	Prostaglandin Receptor	Cardiovascular Disease
U-46619 (9,11-Methanoepoxy PGH2) is a stable analogue of thromboxane A2 (TXA2) and acts as a potent TXA2 agonist.

HY-B1540

Beclometasone
Beclomethasone
Glucocorticoid Receptor Inflammation/Immunology Endocrinology

Beclometasone (Beclomethasone) is a prototype glucocorticoid receptor agonist.
HY-P1000

Sfllrnpndkyepf
Thrombin Cardiovascular Disease

Sfllrnpndkyepf is a synthetic thrombin receptor agonist peptide.
HY-19065

Ru-32514
GABA Receptor Neurological Disease

Ru-32514 is an agonist of benzodiazepine receptor.
HY-P0187

Senktide
Neurokinin Receptor Neurological Disease Endocrinology

Senktide is a tachykinin NK₃ receptor agonist.

HY-100380

*TPO agonist* 1**	Thrombopoietin Receptor	Cardiovascular Disease
TPO agonist 1 is a thrombopoietin (TPO) agonist extracted from patent WO2008134338A1, compound TPO mimetic. It would be useful as promoters of thrombopoiesis and megakaryocytopoiesis to treat thrombocytopenia.

HY-18776

A2AR-agonist-1
Adenosine Receptor Neurological Disease

A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.

HY-U00396

*MC-4R Agonist* 1**	Melanocortin Receptor	Metabolic Disease Endocrinology
MC-4R Agonist 1 is an agonist of human melanocortin-4 receptor (MC-4R), used in the research of obesity, diabetes, and sexual dysfunction.

HY-P2518

Protease-Activated Receptor-1, PAR-1 Agonist	Protease-Activated Receptor (PAR)	Inflammation/Immunology
Protease-Activated Receptor-1, PAR-1 Agonist is a thrombin-specific, protease-activated receptor 1 (PAR-1)-specific agonist peptide.

HY-114411

*ERRγ Inverse Agonist* 1**	Estrogen Receptor/ERR	Cancer
ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC₅₀ of 40 nM.

HY-129657

*GLP-1 receptor agonist* 4**	Glucagon Receptor	Metabolic Disease
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC₅₀ of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.

HY-10559

Nelotanserin APD125	5-HT Receptor	Cancer Neurological Disease
Nelotanserin is a potent 5-HT_2A inverse agonist, a moderately potent 5-HT_2C partial inverse agonist and a weak 5-HT_2B inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

HY-P1504

β-Melanocyte Stimulating Hormone (MSH), human Beta-MSH (1-22) (human)	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

HY-B0716S

Urapidil D6	5-HT Receptor Adrenergic Receptor	Endocrinology Neurological Disease
Urapidil D6 is a deuterium labeled Urapidil. Urapidil is an α1-adrenoreceptor antagonist and a 5-HT_1A receptor agonist.

HY-10013

Taranabant MK-0364	Cannabinoid Receptor	Metabolic Disease
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding K_i of 0.13 nM for the human CB1R in vitro.

HY-U00205

Dopexamine hydrochloride
FPL60278AR
Adrenergic Receptor Cardiovascular Disease Endocrinology

Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
HY-50108

GW 4064
FXR Autophagy Metabolic Disease Cancer

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.
HY-P2278

PEN (human)
Others

PEN (human) is an endogenous peptide GPR83 agonist.
HY-U00066

Cicloprolol hydrochloride
Adrenergic Receptor Cardiovascular Disease Endocrinology

Cicloprolol is a partial β 1-adrenoceptor agonist .
HY-A0173

Progabide
SL 76002
GABA Receptor Neurological Disease

Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.
HY-17416A

Guanfacine
Adrenergic Receptor Neurological Disease Endocrinology

Guanfacine is a selective α2A receptor agonist.

HY-A0129

Histamine phosphate Histamine diphosphate	Histamine Receptor	Neurological Disease Endocrinology Cancer
Histamine (phosphate) diphosphate is a potent agonist of histamine receptors and vasodilator.

HY-N1415

β-Caryophyllene (-)-(E)-Caryophyllene; (−)-β-caryophyllene; (−)-trans-Caryophyllene	Cannabinoid Receptor Endogenous Metabolite	Cancer Infection Neurological Disease
β-Caryophyllene is a CB2 receptor agonist.

HY-U00391

β3-AR agonist 2
Adrenergic Receptor Metabolic Disease Endocrinology

β₃-AR agonist 2 is a potent and selective β₃-adrenergic receptor (β₃-AR) agonist with an EC₅₀ of 8 nM.

HY-107901

*Pparδ agonist* 1**	PPAR	Metabolic Disease Cardiovascular Disease
Pparδ agonist 1 is a PPAR-δ agonist, with an EC₅₀ of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.

HY-P1504A

β-Melanocyte Stimulating Hormone (MSH), human TFA Beta-MSH (1-22) (human) TFA	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

HY-15705

*GPR35 agonist* 2**	Others	Metabolic Disease Inflammation/Immunology
GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC₅₀s of 26 and 3.2 nM in the β-arrestin and Ca²⁺ release assay, respectively.

HY-130118

*MRGPRX1 agonist* 1**	Others	Neurological Disease
MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC₅₀ of 50 nM, and is inactive on MRGPRC11. Analgesic effect.

HY-14304

Zinterol MJ 9184	Adrenergic Receptor	Cardiovascular Disease
Zinterol (MJ 9184) is a potent and selective β2-adrenoceptor agonist. Zinterol increases I_Ca in a concentration-dependent manner with an EC₅₀ of 2.2 nM.

HY-B0418A

Loperamide hydrochloride R-18553 hydrochloride	Opioid Receptor Autophagy	Metabolic Disease Neurological Disease
Loperamide (hydrochloride) (R-18553 (hydrochloride)) is an opioid receptor agonist. Loperamide hydrochloride is a selective and competitive human intestinal carboxylesterases (hiCE) inhibitor. Loperamide hydrochloride has anti-diarrheal effect.

HY-131338

*RORγt inverse agonist* 13**	ROR	Inflammation/Immunology
RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC₅₀ of 63.8 nM.

HY-14340

WAY-181187 SAX-187	5-HT Receptor	Neurological Disease
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a K_i of 2.2 nM and an EC₅₀ of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.

HY-G0021

N-Desmethylclozapine Norclozapine; Desmethylclozapine; Normethylclozapine	mAChR Opioid Receptor Drug Metabolite Virus Protease	Infection
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC₅₀=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.

HY-N0808

Camphor (±)-Camphor	TRP Channel Influenza Virus	Cancer Infection Inflammation/Immunology
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities. Camphor is a TRPV3 agonist.

HY-A0008

Talipexole dihydrochloride B-HT 920 dihydrochloride	Adrenergic Receptor Dopamine Receptor 5-HT Receptor	Neurological Disease Endocrinology
Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.

HY-B0316

Avobenzone	Estrogen Receptor/ERR Apoptosis	Others
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.

HY-P0108

Angiotensin II 5-valine
Valine angiotensin II; 5-L-Valine angiotensin II
Angiotensin Receptor Cancer Endocrinology

Angiotensin II 5-valine is an agonist of angiotensin receptor.
HY-B2215

Dimemorfan phosphate
Sigma Receptor Inflammation/Immunology Neurological Disease

Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
HY-B0489

Arecoline hydrobromide
Arecoline bromide
mAChR Neurological Disease

Arecoline hydrobromide (Arecoline bromide) is a muscarinic acetylcholine receptor agonist.
HY-14917

Capadenoson
BAY 68-4986
Adenosine Receptor Cardiovascular Disease

Capadenoson is a selective agonist of adenosine-A1 receptor.
HY-19998

Taprenepag isopropyl
PF-04217329
Prostaglandin Receptor Inflammation/Immunology Endocrinology

Taprenepag isopropyl is a highly selective EP₂ receptor agonist.
HY-16722

Fosdagrocorat
PF-04171327
Glucocorticoid Receptor Inflammation/Immunology Endocrinology

Fosdagrocorat (PF-04171327) is a dissociated glucocorticoid receptor agonist.
HY-17633

Fonadelpar
NPS-005; SJP-0035
PPAR Neurological Disease

Fonadelpar is a PPARδ agonist, used in the research of neuroparalytic keratopathy.
HY-U00230

CDD0102
CDD0102A
mAChR Neurological Disease

CDD0102 is a potent M₁ Muscarinic receptor agonist.
HY-N2309

Kainic acid
Others Neurological Disease

Kainic acid is a potent agonist at excitatory amino acid receptor subtypes in the CNS.
HY-107480

YK11
Androgen Receptor Metabolic Disease

YK11 is a partial agonist of androgen receptor, with osteogenic activity.
HY-14799

Palovarotene
R 667; Ro 3300074
RAR/RXR Autophagy Others

Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
HY-14864A

(S)-Mapracorat
(S)-ZK-245186; (S)-BOL-303242X
Glucocorticoid Receptor Endocrinology

(S)-Mapracorat is a selective and less active glucocorticoid receptor agonist.
HY-P0236

Neurokinin A(4-10)
Neurokinin Receptor Neurological Disease Endocrinology

Neurokinin A (4-10) is a tachykinin NK₂ receptor agonist.
HY-B0380A

Trimebutine maleate
Opioid Receptor Metabolic Disease

Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects.
HY-B0380

Trimebutine
Opioid Receptor Metabolic Disease

Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.
HY-14864

Mapracorat
ZK-245186; BOL-303242X
Glucocorticoid Receptor Endocrinology

Mapracorat is a novel non-steroidal selective glucocorticoid receptor agonist.
HY-108449

WS-12
TRP Channel Metabolic Disease Cancer

WS-12 is an agonist of TRPM8 with an EC₅₀ of 39 nM.
HY-101585

Imoxiterol
RP 58802B
Adrenergic Receptor Neurological Disease Endocrinology

Imoxiterol (RP 58802B) is a β-adrenergic agonist.
HY-P1013

Deltorphin 2
[D-Ala2]-Deltorphin II
Opioid Receptor Neurological Disease

Deltorphin 2 is a selective peptide agonist for the δ opioid receptor.

HY-100113

*AT2 receptor agonist* C21**	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AT2 receptor agonist C21 is a druglike selective angiotensin II AT2 receptor agonist with K_i values of 0.4 nM and >10 µM for the AT2 receptor and AT1 receptor, respectively.

HY-14773S

(Rac)-Mirabegron D5 (Rac)-YM178 D5	Adenosine Receptor	Metabolic Disease
(Rac)-Mirabegron D5 ((Rac)-YM178 D5) is a deuterium labeled (Rac)-Mirabegron. (Rac)-Mirabegron is the racemate of Mirabegron. Mirabegron is a selective β₃-adrenoceptor agonist.

HY-128922

Dexamethasone palmitate DXP	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Dexamethasone palmitate (DXP) is a prodrug of Dexamethasone, which is a glucocorticoid receptor agonist. Dexamethasone palmitate (DXP) has a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Anti-inflammatory agent.

HY-108472

Loxoribine 7-Allyl-8-oxoguanosine; RWJ 21757	Toll-like Receptor (TLR) Influenza Virus	Cancer Infection
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist.

HY-P1313A

PAR 4 (1-6) (TFA) GYPGQV TFA	Protease-Activated Receptor (PAR)	Others
PAR 4 (1-6) TFA (GYPGQV TFA), a hexapeptide, is a fragment of protease-activated receptor 4 (PAR₄). PAR 4 (1-6) TFA acts as a PAR₄-specific agonist.

HY-16713A

(S)-(-)-5-Fluorowillardiine hydrochloride (5S)-Fluorowillardiine hydrochloride; (S)-5-Fluorowillardiine hydrochloride	iGluR	Neurological Disease
(S)-(-)-5-Fluorowillardiine hydrochloride is a potent and specific AMPAR agonist.

HY-U00216

NNC45-0781
Estrogen Receptor/ERR Metabolic Disease

NNC45-0781 is a tissue-selective estrogen partial-agonist.
HY-13201

CGS 21680
Adenosine Receptor Neurological Disease

CGS 21680 is a selective adenosine A2A receptor agonist, with a K_i of 27 nM.
HY-100532

CD437
AHPN
RAR/RXR Autophagy Cancer

CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
HY-16718

Dagrocorat
PF-00251802
Glucocorticoid Receptor Inflammation/Immunology Endocrinology

Dagrocorat (PF-00251802) is a novel and dissociated glucocorticoid receptor agonist.
HY-103173

5'-N-Ethylcarboxamidoadenosine
NECA
Adenosine Receptor Cancer Metabolic Disease

5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
HY-11076

GI 181771
Cholecystokinin Receptor Metabolic Disease Endocrinology

GI 181771 is a cholecystokinin 1 receptor agonist investigated for the treatment of obesity.
HY-P0080

Novokinin
Angiotensin Receptor Metabolic Disease

Novokinin is a peptide agonist of the angiotensin AT2 receptor.
HY-16713

(S)-(-)-5-Fluorowillardiine
(5S)-Fluorowillardiine; (S)-5-Fluorowillardiine
iGluR Neurological Disease

(S)-(-)-5-Fluorowillardiine is a potent and specific AMPAR agonist.
HY-B0189

Mosapride
TAK-370; AS-4370
5-HT Receptor Neurological Disease

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
HY-33353

GSK-4716
Estrogen Receptor/ERR Cancer

GSK-4716 is a selective ERRβ/γ agonist.
HY-111132

JT010
TRP Channel Cancer

JT010 is a potent agonist of TRPA1 with an EC₅₀ of 0.65 nM.
HY-B0570

Decamethonium Bromide
nAChR Neurological Disease

Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
HY-U00226

UP202-56
Adenosine Receptor Inflammation/Immunology

UP202-56 is an adenosine analogue, which is an adenosinergic agonist.
HY-13201A

CGS 21680 Hydrochloride
Adenosine Receptor Neurological Disease

CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a K_i of 27 nM.
HY-U00293

ZK-90055 hydrochloride
Adrenergic Receptor Inflammation/Immunology Endocrinology

ZK-90055 hydrochloride is a β2 adrenergic receptor agonist.
HY-B0475

Xylometazoline hydrochloride
Adrenergic Receptor Cardiovascular Disease Endocrinology

Xylometazoline hydrochloride is an α-adrenoceptor agonist commonly used as nasal decongestant.
HY-16748

Nelonicline
ABT-126
nAChR Neurological Disease

Nelonicline (ABT-126) is a selective neuronal nicotinic receptor agonist.
HY-U00038

ENS-163 phosphate
ENS 213-163; Sandoz ENS 163 phosphate; Thiopilocarpine phosphate
mAChR Neurological Disease

ENS-163 phosphate is a selective muscarinic M1 receptor agonist.
HY-12451

FICZ
6-Formylindolo[3,2-b]carbazole
Aryl Hydrocarbon Receptor Others

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a K_d of 70 pM.
HY-P1481

β-Casomorphin, human
Human β-casomorphin 7
Opioid Receptor Metabolic Disease

is an opioid peptide, acts as an agonist of opioid receptor.

HY-101033

*GPR35 agonist* 1**	Others	Cancer Endocrinology
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC₅₀ of 5.8 nM, displays good druggability.

HY-N2411

Geissoschizine methyl ether	5-HT Receptor	Neurological Disease
Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is potent 5-HT_1A receptor agonist.

HY-19320

Orexin 2 Receptor Agonist	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.

HY-109527

*5-HT7 agonist* 1**	5-HT Receptor	Neurological Disease
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC₅₀ of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.

HY-108258A

PSN 375963 hydrochloride	GPR119	Endocrinology
PSN 375963 hydrochloride is a potent GPR119 agonist, with EC₅₀s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).

HY-41076

*Ca2+ channel agonist* 1**	Calcium Channel CDK	Neurological Disease
Ca²⁺ channel agonist 1 is an agonist of N-type Ca²⁺ channel and an inhibitor of Cdk2, with EC₅₀s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.

HY-P0080A

Novokinin TFA
Angiotensin Receptor Metabolic Disease

Novokinin TFA is a peptide agonist of the angiotensin AT2 receptor.

HY-13736A

Quinagolide hydrochloride CV205-502 hydrochloride	Dopamine Receptor	Neurological Disease
Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.

HY-P1337

Dynorphin B (1-13)
Opioid Receptor Neurological Disease

Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.
HY-14299

Indacaterol
Adrenergic Receptor Neurological Disease Endocrinology

Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.
HY-19661

Tecadenoson
CVT-510
Adenosine Receptor Neurological Disease Cardiovascular Disease

Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
HY-113035

Angiotensin III
Endogenous Metabolite Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin III is an angiotensin 1 (AT1) and AT2 receptor agonist.
HY-P1470

[Leu5]-Enkephalin, amide
Leu-Enkephalin amide
Opioid Receptor Neurological Disease

[Leu5]-Enkephalin, amide is a δ opioid receptor agonist.
HY-P1336

Deltorphin I
Deltorphin 1; Deltorphin C
Opioid Receptor Neurological Disease

Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
HY-14299A

Indacaterol maleate
QAB149
Adrenergic Receptor Endocrinology

Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.

HY-17355A

Dexpramipexole dihydrochloride (R)-Pramipexole dihydrochloride; R-(+)-Pramipexole dihydrochloride; KNS-760704 dihydrochloride	Dopamine Receptor	Neurological Disease
Dexpramipexole dihydrochloride ((R)-Pramipexole dihydrochloride) is a neuroprotective agent and weak non-ergoline dopamine agonist.

HY-101274

BAR501
GPCR19 Cardiovascular Disease

BAR501 is a potent and selective agonist of GPBAR1 with an EC₅₀ of 1 μM.
HY-B0188

Mianserin
Mianserine
Histamine Receptor Neurological Disease Endocrinology

Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
HY-100273

AGN 194078
RAR/RXR Autophagy Cancer

AGN 194078 is a selective RARα agonist with a K_d and EC₅₀ of 3 and 112 nM, respectively.
HY-B0189A

Mosapride citrate
TAK-370 citrate; AS-4370 citrate
5-HT Receptor Neurological Disease

Mosapride citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

HY-P1532

Pancreatic Polypeptide, rat Rat pancreatic polypeptide	Neuropeptide Y Receptor	Metabolic Disease Endocrinology
Pancreatic Polypeptide, rat is an agonist of NPY receptor, with high affinity at NPYR4.

HY-W015326

3-Hydroxymandelic Acid
Endogenous Metabolite Others

3-Hydroxymandelic Acid, a metabolite of Phenylephrine, Phenylephrine is a α-receptor agonist.
HY-111068

KD-3010
PPAR Metabolic Disease

KD-3010 is a potent, orally active, and selective PPARδ agonist.
HY-17622

Tavilermide
MIM-D3
Trk Receptor Inflammation/Immunology

Tavilermide is a selective, partial agonist of TrkA, or a nerve growth factor (NGF) mimetic.
HY-21098A

PD-168077 maleate
Dopamine Receptor Neurological Disease

PD-168077 maleate is a selective dopamine D₄ receptor agonist, with a K_i of 9 nM.
HY-12664

AF64394
Others Others

AF64394 is a GPR3 inverse agonist, with a pIC₅₀ of 7.3.
HY-101973

XL041
BMS-852927
LXR Cardiovascular Disease

XL041 (BMS-852927) is an LXRβ-selective agonist.

HY-B0374A

Moxonidine hydrochloride BDF5895 hydrochloride	Imidazoline Receptor	Neurological Disease
Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.

HY-U00233

FG8119
NNC13-8119
GABA Receptor Neurological Disease

FG8119 is a novel benzodiazepine agonist extracted from patent US 4745112 A.

HY-135572

*TLX agonist* 1**	Others	Cancer Neurological Disease
TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC₅₀=1μM; K_d= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.

HY-14958A

Pardoprunox hydrochloride SLV-308 hydrochloride; DU-126891 hydrochloride	5-HT Receptor Adrenergic Receptor Dopamine Receptor	Neurological Disease Endocrinology
Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC₅₀s of 8, 9.2, and 6.3, respectively.

HY-14958

Pardoprunox SLV-308; DU-126891	5-HT Receptor Adrenergic Receptor Dopamine Receptor	Neurological Disease Endocrinology
Pardoprunox (SLV-308) is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC₅₀s of 8, 9.2, and 6.3, respectively.

HY-P1123

MEDICA16	ATP Citrate Lyase GPR40 GPR120	Metabolic Disease
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120.

HY-19434A

cis-ACPD	iGluR mGluR	Neurological Disease
cis-ACPD is a potent agonist of NMDA receptor, with an IC₅₀ of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC₅₀s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.

HY-P1198

Hemokinin 1, human	Neurokinin Receptor	Neurological Disease
Hemokinin 1, human is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human can produces an opioid-independent analgesia.

HY-112606

ML-290	Others	Others
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC₅₀ of 94 nM. ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.

HY-17366A

Clozapine N-oxide dihydrochloride	mAChR Dopamine Receptor Drug Metabolite	Neurological Disease
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist.

HY-17366

Clozapine N-oxide	mAChR Dopamine Receptor Drug Metabolite	Neurological Disease
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist.

HY-114146

CID 1375606
Others Metabolic Disease Neurological Disease

CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
HY-100124

Bamaluzole
GABA Receptor Neurological Disease

Bamaluzole is a GABA receptor agonist extracted from patent WO 2012064642 A1.
HY-P1087

Adrenorphin
Metorphamide
Opioid Receptor Cancer

Adrenorphin is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with K_i of 12 nM.
HY-B0452

Ritodrine hydrochloride
DU21220 hydrochloride
Adrenergic Receptor Endocrinology

Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
HY-101038A

ZK756326 dihydrochloride
CCR Cancer Endocrinology

ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

HY-B0091A

Adapalene sodium salt CD 271 sodium salt	RAR/RXR Autophagy	Inflammation/Immunology
Adapalene sodium salt(CD 271; Differin), a synthetic retinoid, is a Retinoic acid receptor agonist (RAR).

HY-109111

Azelaprag
Others Others

Azelaprag (Example 263.0) is an apelin receptor agonist drug candidate.
HY-U00400

PF-592379
Dopamine Receptor Neurological Disease

PF-592379 is a potent dopamine D₃ receptor agonist with an EC₅₀ of 21 nM.
HY-11077

SR 146131
Cholecystokinin Receptor Metabolic Disease Endocrinology

SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
HY-113035A

Angiotensin III TFA
Endogenous Metabolite Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin III (TFA) is an angiotensin 1 (AT1) and AT2 receptor agonist.
HY-B0091

Adapalene
CD271
RAR/RXR Autophagy Apoptosis Inflammation/Immunology Cancer

Adapalene(CD-271; Differin), a synthetic retinoid, is a retinoic acid receptor agonist (RAR).
HY-14734B

Anamorelin Fumarate
ONO-7643 Fumarate; RC1291 Fumarate
GHSR Cancer Endocrinology

Anamorelin Fumarate is a novel ghrelin receptor agonist with EC₅₀ value of 0.74 nM in the FLIPR assay.

HY-P1578

Galanin (1-16), mouse, porcine, rat	Neuropeptide Y Receptor	Neurological Disease Endocrinology
Galanin (1-16), mouse, porcine, rat is an agonist of the hippocampal galanin receptor, with a K_d of 3 nM.

HY-100327

MK-6913
Tetrahydrofluoroene 52
Estrogen Receptor/ERR Metabolic Disease

MK-6913 (Tetrahydrofluoroene 52) is a potent and selective estrogen receptor β agonist.
HY-10448

Capsaicin
(E)-Capsaicin
TRP Channel Autophagy Cancer

Capsaicin is a TRPV1 agonist with an EC₅₀ of 0.29 μM in HEK293 cells.
HY-79593

MRE-269
ACT-333679
Prostaglandin Receptor Cardiovascular Disease Endocrinology

MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
HY-B0409A

Clonidine hydrochloride
Adrenergic Receptor Cardiovascular Disease Endocrinology

Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.
HY-101582

ZT 52656A hydrochloride
Opioid Receptor Neurological Disease

ZT 52656A is a selective kappa opioid agonist, used for the prevention or alleviation of pain in the eye.
HY-19250

U-101017
PNU 101017
GABA Receptor Neurological Disease

U-101017 is a partial agonist of benzodiazepine receptor and GABAA receptor, with anxiolytic effects.
HY-103704

LY2562175
FXR Autophagy Metabolic Disease

LY2562175 is a potent and selective FXR agonist, with an EC₅₀ of 193 nM.
HY-107216

G-1
Estrogen Receptor/ERR Cancer

G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a K_i of 11 nM.
HY-N2371

27-Hydroxycholesterol
Estrogen Receptor/ERR LXR Endogenous Metabolite Cancer

27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.

HY-B0648

Medroxyprogesterone 17α-Hydroxy-6α-methylprogesterone; U8840	Progesterone Receptor	Endocrinology
Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.

HY-12499

(S)-Willardiine
(-)-Willardiine
iGluR Neurological Disease

(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.
HY-19468

ERB-196
WAY-202196
Estrogen Receptor/ERR Inflammation/Immunology Neurological Disease

ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.
HY-P1337A

Dynorphin B (1-13) (TFA)
Opioid Receptor Neurological Disease

Dynorphin B (1-13) TFA acts as an agonist on opioid κ-receptor.

HY-P0252

α-Melanocyte-Stimulating Hormone (MSH), amide	Melanocortin Receptor	Metabolic Disease
α-Melanocyte-Stimulating Hormone (MSH), amide is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist.

HY-P1192

GR-73632	Neurokinin Receptor	Neurological Disease Endocrinology
GR-73632 is a novel tachykinin neurokinin 1 (NK-1) receptor agonist. GR-73632 acts directly on the peripheral terminals of primary sensory neurons through NK1 receptor which convey itch signals.

HY-128573

*RORγt Inverse agonist* 3**	ROR	Neurological Disease
RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC₅₀s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.

HY-P3137

TRV056	Angiotensin Receptor	Cardiovascular Disease
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.

HY-P3136

TRV055	Angiotensin Receptor	Cardiovascular Disease
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.

HY-114464

11-Beta-hydroxyandrostenedione 4-Androsten-11β-ol-3,17-dione	Endogenous Metabolite	Endocrinology
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a *11β-hydroxysteroid dehydrogenase* (11βHSD) isozymes** inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.

HY-131312

Mutant IDH1-IN-6	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-6 is a potent, selective and orally active *mutant isocitrate dehydrogenase* (IDH) inhibitor with IC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes**, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.

HY-14773

Mirabegron
YM178
Adrenergic Receptor Neurological Disease Endocrinology

Mirabegron is a selective β₃-adrenoceptor agonist with EC₅₀ of 22.4 nM.
HY-100676

GRI977143
LPL Receptor Caspase Cancer Inflammation/Immunology

GRI977143 is a specific LPA₂ receptor agonist, with an EC₅₀ of 3.3 μM .

HY-W014666

Xanthurenic acid	Endogenous Metabolite mGluR Apoptosis	Metabolic Disease Neurological Disease
Xanthurenic acid is a putative endogenous Group II metabotropic glutamate receptor agonist, on sensory transmission in the thalamus.

HY-109197

Vonafexor
EYP001
FXR HBV Infection

Vonafexor (EYP001) is a selective FXR agonist with anti-HBV effects.
HY-101639A

CP-409092 hydrochloride
GABA Receptor Neurological Disease

CP-409092 hydrochloride is a partial agonist of GABA_A receptor, with anti-anxiety activity.
HY-102075A

TMP778
ROR Inflammation/Immunology

TMP778 is a potent and selevtive RORγt inverse agonist, with an IC₅₀ of 7 nM in FRET assay.
HY-100336

AC260584
mAChR Neurological Disease

AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC₅₀ of 7.6.
HY-10475

AM580
CD336; NSC608001; Ro 40-6055
RAR/RXR Autophagy Cancer

AM580 is a selective RARα agonist with IC₅₀ and EC₅₀ of 8 nM and 0.36 nM, respectively.

HY-15108

Purmorphamine Shh Signaling Antagonist VI	Smo Autophagy	Neurological Disease Cancer
Purmorphamine (Shh Signaling Antagonist VI) is a smoothened/Smo receptor agonist with an EC₅₀ of 1 μM.

HY-101384A

Ro 10-5824 dihydrochloride
Dopamine Receptor Others

Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with K_i of 5.2 nM.
HY-P1331

BAM-22P
Bovine adrenal medulla-22P
Opioid Receptor Neurological Disease

BAM-22P, a highly potent opioid peptide, is a potent opioid agonist.
HY-109032

Firuglipel
GPR119 Metabolic Disease

Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
HY-100140

Pipequaline
PK-8165
GABA Receptor Neurological Disease

Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity.
HY-41700

D-Alanine
(R)-Alanine; Ba 2776; D-α-Alanine
Endogenous Metabolite Others

D-Alanine is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC₅₀ of 9 mM for GlyR.

HY-107319

Almitrine mesylate Almitrine bismesylate; Almitrine bismethanesulfonate; Almitrine dimesylate	Potassium Channel	Neurological Disease Cardiovascular Disease
Almitrine mesylate, a peripheral chemoreceptor agonist, inhibits selectively the Ca²⁺-dependent K⁺ channel.

HY-12749

Midodrine
(±)-Midodrin
Others Neurological Disease

Midodrine is an α1-receptor agonist, for the treatment of dysautonomia and orthostatic hypotension.

HY-B1403

Dienestrol	Estrogen Receptor/ERR	Endocrinology Cancer
Dienestrol is a synthetic, non-steroidal estrogen, is an estrogen receptor agonist, for the treatment of menopausal and postmenopausal symptoms.

HY-101299

(+)-Dihydrexidine hydrochloride (+)-DAR-0100 (hydrochloride)	Dopamine Receptor	Neurological Disease
(+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC₅₀ of 72± 21 nM.

HY-16972

SR9243
LXR Cancer

SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
HY-N6629

3'-Methoxyflavonol
Others Neurological Disease

3'-Methoxyflavonol is a selective agonist of neuromedin U 2 receptor (NMU2R).

HY-104026

L-Kynurenine	Aryl Hydrocarbon Receptor Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.

HY-100291

SX-3228
GABA Receptor Neurological Disease

SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC₅₀ of 17 nM.

HY-P1578A

Galanin (1-16), mouse, porcine, rat TFA	Neuropeptide Y Receptor	Neurological Disease Endocrinology
Galanin (1-16), mouse, porcine, rat (TFA) is an agonist of the hippocampal galanin receptor, with a K_d of 3 nM.

HY-101987

BW 245C
Prostaglandin Receptor Cardiovascular Disease Endocrinology

BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
HY-13101

MCOPPB triHydrochloride
MCOPPB 3HCl
Opioid Receptor Neurological Disease

MCOPPB 3Hcl is a nociceptin receptor agonist with pKi of 10.07; weaker activity at other opioid receptors.
HY-P0226

TFLLR-NH2
Protease-Activated Receptor (PAR) Cardiovascular Disease

TFLLR-NH2 is a selective PAR1 agonist with an EC₅₀ of 1.9 μM.

HY-19883

Lusutrombopag S-888711	Thrombopoietin Receptor	Inflammation/Immunology
Lusutrombopag is an orally bioavailable thrombopoietin (TPO) receptor agonist, used for treatment of chronic liver disease.

HY-N0178

Diosmin
Aryl Hydrocarbon Receptor Cancer Cardiovascular Disease

Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
HY-A0040

Talipexole
B-HT 920
Dopamine Receptor Neurological Disease

Talipexole (B-HT920) is a dopamine agonist that has been proposed as an antiparkinsonian agent.
HY-P1515

Angiotensin II (3-8), human
Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin II (3-8), human is a less effective agonist at the angiotensin AT₁ receptor.
HY-101639

CP-409092
GABA Receptor Neurological Disease

CP-409092 is a partial agonist of GABA_A receptor, with anti-anxiety activity.
HY-13788B

LY 344864 hydrochloride
5-HT Receptor Neurological Disease

LY 344864 hydrochloride is a selective 5-HT1F agonist with a K_i of 6 nM.
HY-10002

Calcitriol
1,25-Dihydroxyvitamin D3
VD/VDR Endogenous Metabolite Cancer

Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.

HY-P1198A

Hemokinin 1, human TFA	Neurokinin Receptor	Neurological Disease
Hemokinin 1, human TFA is a selective tachykinin neurokinin 1 (NK1) receptor full agonist. Hemokinin 1, human TFA is a full agonist at NK2 and NK3 receptor. Hemokinin 1, human TFA can produces an opioid-independent analgesia.

HY-14304A

Zinterol hydrochloride MJ 9184 hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist. Zinterol hydrochloride increases I_Ca in a concentration-dependent manner with an EC₅₀ of 2.2 nM. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits.

HY-P0078

TRAP-6 PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6	Protease-Activated Receptor (PAR)	Inflammation/Immunology
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.

HY-N0166

Gramine Donaxine	Adiponectin Receptor Adrenergic Receptor Reverse Transcriptase	Cancer Infection Metabolic Disease Endocrinology
Gramine (Donaxine) is a natural alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC₅₀s of 3.2 and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine (Donaxine) has anti-tumor, anti-viral and anti-inflammatory properties.

HY-100775

Setogepram sodium salt PBI-4050 sodium salt	GPR40 GPR84	Metabolic Disease Inflammation/Immunology
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram sodium salt decreases renal, liver and pancreatic fibrosis. Setogepram sodium salt exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

HY-B0436

Salbutamol hemisulfate Albuterol hemisulfate; AH-3365 hemisulfate	Adrenergic Receptor Autophagy	Inflammation/Immunology Endocrinology Cancer
Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting β2 adrenergic receptor agonist Target: β2 Adrenergic Receptor Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD.

HY-14229

TGR5 Receptor Agonist CCDC	GPCR19	Metabolic Disease
TGR5 Receptor Agonist (CCDC), a potent TGR5(GPCR19) agonist, shows improved potency in the U2-OS cell assay (pEC₅₀=6.8) and in melanophore cells (pEC₅₀=7.5).

HY-B0188A

Mianserin hydrochloride Org GB 94	Histamine Receptor	Neurological Disease Endocrinology
Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.

HY-100140A

Pipequaline hydrochloride PK-8165 (hydrochloride)	GABA Receptor	Neurological Disease
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity.

HY-14785

Befiradol
NLX-112; F13640
5-HT Receptor Neurological Disease

Befiradol (NLX-112) is a selective 5-HT1A receptor agonist.
HY-W014325

TRPM8 antagonist WS-3
TRP Channel Cancer Metabolic Disease

TRPM8 antagonist WS-3 is an agonist of TRPM8 with an EC₅₀ of 3.7 μM.

HY-101864

Blarcamesine hydrochloride AVex-73 hydrochloride; AE-37 hydrochloride	Sigma Receptor	Neurological Disease
Blarcamesine hydrochloride (AVex-73 hydrochloride) is a Sigma-1 Receptor agonist with an IC₅₀ of 860 nM.

HY-19334

L755507
Adrenergic Receptor CRISPR/Cas9 Cancer Endocrinology

L755507 is a potent, selective agonist of β₃-AR with an IC₅₀ of 35 nM.

HY-14785A

Befiradol hydrochloride NLX-112 hydrochloride; F 13640 hydrochloride	5-HT Receptor	Neurological Disease
Befiradol hydrochloride (NLX-112 hydrochloride) is a selective 5-HT_1A receptor agonist.

HY-P0079

Neuromedin N Neuromedin N (rat, mouse, porcine, canine)	Dopamine Receptor	Neurological Disease
Neuromedin N is a potent modulator of dopamine D2 receptor agonist binding in rat neostriatal membranes.

HY-114116

ML-109
TSH Receptor Metabolic Disease Endocrinology

ML-109 is a potent and full thyroid stimulating hormone receptor (TSHR) agonist, with an EC₅₀ of 40 nM.
HY-10838

GW 501516
GW 1516; GSK-516
PPAR Autophagy Metabolic Disease Cancer

GW 501516 (GW 1516) is a PPARδ agonist with an EC₅₀ of 1.1 nM.
HY-P0297

Protease-Activated Receptor-4
Protease-Activated Receptor (PAR) Others

Protease-Activated Receptor-4 is the agonist of proteinase-activated receptor-4 (PAR4).

HY-15306

Eltrombopag SB-497115	Thrombopoietin Receptor	Cardiovascular Disease Cancer
Eltrombopag (SB-497115) is a thrombopoietin (TPO) receptor agonist developed for certain conditions that lead to thrombocytopenia.

HY-P1477

Adrenocorticotropic Hormone (ACTH) (1-39), rat ACTH (1-39) (mouse, rat)	Melanocortin Receptor	Metabolic Disease Endocrinology
Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.

HY-12749A

Midodrine hydrochloride (±)-Midodrine hydrochloride	Others	Neurological Disease
Midodrine hydrochloride ((±)-Midodrine hydrochloride) is an α1-receptor agonist, for the treatment of dysautonomia and orthostatic hypotension.

HY-N3216

Nagilactone B
LXR Cardiovascular Disease

Nagilactone B, extracted from the root bark of Podocarpus nagi, is a liver X receptor (LXR) agonist.
HY-16465

IRL-1620
Endothelin Receptor Neurological Disease Endocrinology

IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.
HY-12721

Clonidine
Adrenergic Receptor Neurological Disease

Clonidine is an alpha 2-adrenergic agonist which is used extensively in anesthesia research.
HY-18939

N6-Cyclohexyladenosine
CHA
Adenosine Receptor Neurological Disease

N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).

HY-14648A

Dexamethasone acetate Dexamethasone 21-acetate; Hexadecadrol acetate	Glucocorticoid Receptor Autophagy Mitophagy Bacterial	Inflammation/Immunology Endocrinology Cancer
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. Dexamethasone acetate has the potential for ophthalmic infections treatment.

HY-107418

Tropifexor
LJN452
FXR Autophagy Cardiovascular Disease

Tropifexor (LJN452) is a highly potent agonist of FXR with an EC₅₀ of 0.2 nM.
HY-P1515A

Angiotensin II (3-8), human TFA
Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin II (3-8), human (TFA) is a less effective agonist at the angiotensin AT₁ receptor.

HY-10922A

Camicinal hydrochloride GSK962040 hydrochloride	Motilin Receptor	Metabolic Disease
Camicinal hydrochloride (GSK962040 hydrochloride) is a small molecule, selective motilin receptor agonist with pEC₅₀ of 7.9.

HY-P2321

TRAP-6 amide
Protease-Activated Receptor (PAR) Inflammation/Immunology

TRAP-6 amide is a PAR-1 thrombin receptor agonist peptide.
HY-101271

WAY-200070
Estrogen Receptor/ERR Neurological Disease

WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC₅₀ of 2.3 nM.

HY-P0088

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous κ opioid receptor agonist and is antinociceptive at physiological concentrations.

HY-100166

AP521
5-HT Receptor Neurological Disease

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM.
HY-10480

Fasiglifam
TAK-875
GPR40 Metabolic Disease

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC₅₀ of 72 nM.
HY-111454

SR17018
Opioid Receptor Neurological Disease

SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC₅₀ of 97 nM.
HY-15677

INT-777
S-EMCA
GPCR19 Endocrinology

INT-777 is a potent TGR5 agonist with an EC₅₀ of 0.82 μM.
HY-13421

SR1001
ROR Inflammation/Immunology

SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively.
HY-16086

Balaglitazone
DRF 2593; NN 2344
PPAR Metabolic Disease

Balaglitazone is a selective partial PPARγ agonist with an EC₅₀ of 1.351 μM for human PPARγ.
HY-101492

GPR120-IN-1
GPR120 Metabolic Disease

GPR120-IN-1 is a selective Gpr120 agonist with a logEC₅₀ of −7.62.
HY-P0226A

TFLLR-NH2(TFA)
Protease-Activated Receptor (PAR) Others

TFLLR-NH2 (TFA) is a selective PAR1 agonist with an EC₅₀ of 1.9 μM.

HY-15388

Tazarotene AGN 190168	RAR/RXR Autophagy	Inflammation/Immunology Cancer
Tazarotene (AGN 190168) is a selective retinoic acid receptor (RAR) agonist for the treatment of plaque psoriasis and acne vulgaris.

HY-B0374

Moxonidine
BDF5895
Imidazoline Receptor Neurological Disease

Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent.

HY-B0769

Phenylephrine (R)-(-)-Phenylephrine; L-Phenylephrine	Adrenergic Receptor	Cardiovascular Disease Endocrinology
(R)-(-)-Phenylephrine is a selective α₁-adrenoceptor agonist primarily used as a decongestant.

HY-10922

Camicinal
GSK962040
Motilin Receptor Metabolic Disease

Camicinal (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.

HY-120879

PF2562	Dopamine Receptor	Neurological Disease
PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a K_i of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC₅₀ of 568 nM in HTRF assay.

HY-136258

*nAChR agonist* CMPI hydrochloride**	nAChR	Neurological Disease
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)₃(β2)₂ nAChR to ACh (10 µM) with an EC₅₀ of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.

HY-133011

*nAChR agonist* 1**	nAChR	Neurological Disease
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC₅₀ of 0.32 µM in a Ca²⁺ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.

HY-115400

1V209 TLR7 agonist T7	Toll-like Receptor (TLR)	Cancer
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.

HY-101630

Deramciclane EGIS-3886	5-HT Receptor	Neurological Disease
Deramciclane has a high affinity for 5-HT_2A and 5-HT_2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist.

HY-P1145

Glucagon-like peptide 1 (1-37), human
HuGLP-1
Glucagon Receptor Metabolic Disease

Glucagon-like peptide 1 (1-37), human is a highly potent agonist of the GLP-1 receptor.
HY-70037

Cinacalcet
AMG 073
CaSR Cardiovascular Disease

Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-107542

Oleoylethanolamide N-Oleoylethanolamide; Oleamide MEA; Oleic acid monoethanolamide	Endogenous Metabolite PPAR	Metabolic Disease Cardiovascular Disease
Oleoylethanolamide is a high affinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.

HY-112627

CAY 10465	Aryl Hydrocarbon Receptor	Cardiovascular Disease
CAY 10465 is a selective and high-affinity AhR agonist, with a K_i of 0.2 nM, and shows no effect on estrogen receptor (K_i >100000 nM).

HY-111786

LHC-165
Toll-like Receptor (TLR) Cancer

LHC-165 is a TLR7 agonist. Has potential to treat solid tumors.
HY-102016

SB756050
GPCR19 Metabolic Disease

SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
HY-101540

NMI 8739
Dopamine Receptor Neurological Disease

NMI 8739 is a dopamine D₂ autoreceptor agonist, which is an amine conjugate of the DHA carrier and the neurotransmitter dopamine.
HY-B0716

Urapidil
5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology

Urapidil is an α1 adrenoreceptor antagonist and a 5-HT_1A receptor agonist.

HY-14870

Selexipag NS-304; ACT-293987	Prostaglandin Receptor	Cardiovascular Disease Endocrinology
Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI₂) receptor (IP receptor).

HY-108003

MM 07
Others Cardiovascular Disease

MM 07 is a biased apelin receptor agonist, with a K_D of 300 nM in CHO-K1 cells and a K_D of 172 nM in human heart.

HY-76772A

(+)-Cevimeline hydrochloride hemihydrate (+)-SNI-2011; (+)-AF102B hydrochloride hemihydrate	mAChR	Neurological Disease
(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.

HY-15885

LY2119620
mAChR Neurological Disease

LY2119620 is a high-affinity muscarinic M₂/M₄ receptor agonist.
HY-B0206

Rizatriptan benzoate
MK 462
5-HT Receptor Neurological Disease

Rizatriptan Benzoate(Maxalt) is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.
HY-14734

Anamorelin
RC-1291; ONO-7643
GHSR Cancer Endocrinology

Anamorelin (RC-1291) is a potent ghrelin receptor agonist with EC₅₀ value of 0.74 nM in the FLIPR assay.
HY-107395

BMS 753
RAR/RXR Inflammation/Immunology

BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, with a K_i of 2 nM.
HY-15291

MBX-2982
GPR119 Metabolic Disease

MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
HY-19919

BMS-779788
EXEL04286652; XL-652; BMS-788
LXR Metabolic Disease

BMS-779788 is a LXR partial agonist with IC₅₀ values of 68 nM for LXRα and 14 nM for LXRβ.
HY-14171

Bexarotene
LGD1069
RAR/RXR Autophagy Cancer

Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
HY-103098

EMDT oxalate
5-HT Receptor Neurological Disease

EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects.
HY-100347A

SRI-011381 hydrochloride
TGF-beta/Smad Neurological Disease

SRI-011381 hydrochloride is an oral bioavailabile TGF-beta signaling agonist, exhibits neuroprotective effect.
HY-15566

APD597
JNJ-38431055
GPR119 Metabolic Disease

APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
HY-108414

(R)-Equol
(+)-Equol
Estrogen Receptor/ERR Cancer

(R)-Equol is an agonist of both ERα and ERβ with K_is of 27.4 and 15.4 nM, respectively.
HY-18723

Yoda 1
Others Cardiovascular Disease

Yoda 1 is a Piezo1 agonist. Yoda 1 activates purified Piezo1 channels.

HY-14734A

Anamorelin hydrochloride RC-1291 hydrochloride; ONO-7643 hydrochloride	GHSR	Cancer Endocrinology
Anamorelin (RC-1291) hydrochloride is a potent ghrelin receptor agonist with EC₅₀ value of 0.74 nM in the FLIPR assay.

HY-19942A

TD-5471 hydrochloride
Adrenergic Receptor Metabolic Disease Endocrinology

TD-5471 hydrochloride is a potent and selective full agonist of the human β₂-adrenoceptor.

HY-101822

Naminterol	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Naminterol is a phenethanolamine derivative, is a β₂ adrenoceptor agonist with bronchodilatory properties. Naminterol is used for treatment of asthma.

HY-19308

RWJ-51204
GABA Receptor Neurological Disease

RWJ-51204 is a partial agonist of GABA(A) receptor, with K_i of 0.2-2 nM to the benzodiazepine site on GABA(A) receptors.
HY-16737

Elafibranor
GFT505
PPAR Metabolic Disease

Elafibranor (GFT505) is a PPARα/δ agonist with EC₅₀s of 45 and 175 nM, respectively.

HY-19434

trans-ACPD Trans-(±)-ACP	mGluR	Metabolic Disease
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.

HY-P1334

DPDPE
Opioid Receptor Neurological Disease

DPDPE, an opioid peptide, is a selective δ-opioid receptor (DOR) agonist with anticonvulsant effects.

HY-17551

NMDA N-Methyl-D-aspartic acid	iGluR Endogenous Metabolite	Neurological Disease
NMDA is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor.

HY-131103

Phenylethanolamine A	Adrenergic Receptor	Metabolic Disease Inflammation/Immunology
Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process.

HY-P2321A

TRAP-6 amide TFA
Protease-Activated Receptor (PAR) Inflammation/Immunology

TRAP-6 amide TFA is a PAR-1 thrombin receptor agonist peptide.
HY-103107

LY334370
5-HT Receptor Neurological Disease

LY334370 is a selective 5-HT_1F receptor agonist with a K_i of 1.6 nM.

HY-76772B

(-)-Cevimeline hydrochloride hemihydrate (-)-SNI-2011; (-)-AF102B hydrochloride hemihydrate	mAChR	Neurological Disease
(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011), a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.

HY-P1477A

Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA ACTH (1-39) (mouse, rat) TFA	Melanocortin Receptor	Metabolic Disease Endocrinology
Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA) is a potent melanocortin 2 (MC2) receptor agonist.

HY-16998

SR2211
ROR Inflammation/Immunology

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a K_i of 105 nM and an IC₅₀ of ~320 nM.
HY-30006

1-Aminocyclobutanecarboxylic acid
iGluR Neurological Disease

1-Aminocyclobutanecarboxylic acid is a NMDA receptor partial agonist acting at the glycine site, NR1.

HY-P1309

*PAR-4 Agonist* Peptide, amide** PAR-4-AP; AY-NH2	Protease-Activated Receptor (PAR)	Inflammation/Immunology
PAR-4 Agonist Peptide, amide (PAR-4-AP; AY-NH2) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.

HY-129656

*GLP-1 receptor agonist* 3**	Glucagon Receptor	Metabolic Disease
GLP-1 receptor agonist 3 is a GLP-1 receptor agonist extracted from patent WO2018109607A1, Example 4A-1, has EC₅₀s of 1.1 nM and 13 nM in Clone H6 and Clone C6 cell lines assay, respectively.

HY-10233

Gaboxadol hydrochloride Lu 02-030 hydrochloride; THIP hydrochloride	GABA Receptor	Neurological Disease
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 µM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 µM) and a superagonist efficacy at α4β3δ (ED₅₀=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic and has hypnotic activities.

HY-15430A

Encenicline hydrochloride EVP-6124 hydrochloride	nAChR	Neurological Disease
Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

HY-106094

CY 208-243
Dopamine Receptor Neurological Disease

CY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity.

HY-B0084

Dienogest STS 557	Progesterone Receptor Autophagy Apoptosis	Endocrinology Cancer
Dienogest(STS-557) is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis.

HY-136586

Loperamide phenyl
Opioid Receptor Metabolic Disease Neurological Disease

Loperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist.

HY-P1533

CRF, bovine Corticotropin Releasing Factor bovine	CRFR	Inflammation/Immunology Endocrinology
CRF, bovine is a potent agonist of CRF receptor, and displaces [¹²⁵I-Tyr]ovine CRF with a K_i of 3.52 nM.

HY-B1583

(Z)-Capsaicin Zucapsaicin; Civamide; cis-Capsaicin	TRP Channel HSV	Neurological Disease
(Z)-Capsaicin is the cis isomer of capsaicin, acts as an orally active TRPV1 agonist, and is used in the research of neuropathic pain.

HY-17457

Levalbuterol tartrate Levosalbutamol tartrate	Adrenergic Receptor	Neurological Disease Endocrinology
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.

HY-P1031

[bAla8]-Neurokinin A(4-10)
MEN 10210
Neurokinin Receptor Endocrinology

[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.
HY-B0735

Fenoldopam
SKF 82526
Dopamine Receptor Cardiovascular Disease

Fenoldopam(SKF 82526) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.

HY-112322

Carbacyclin Carbaprostacyclin; Carba-PGI2	Prostaglandin Receptor	Cardiovascular Disease Endocrinology
Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.

HY-100728

BMT-145027
mGluR Neurological Disease

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC₅₀ of 47 nM.

HY-19945

DAA-1106	GABA Receptor	Neurological Disease
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.

HY-12111

BMS-564929
Androgen Receptor Endocrinology

BMS-564929 is an androgen receptor (AR) agonist, binds to androgen receptor (AR) with a K_i of 2.11±0.16 nM.

HY-B0566

Guanabenz Acetate BR-750; Wy8678 acetate	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanabenz (Acetate) (BR-750) is an alpha-2 selective adrenergic agonist used as an antihypertensive agent.

HY-100673

LM22A-4
Trk Receptor Neurological Disease

LM22A-4 is a specific agonist of tyrosine kinase receptor B, used for neurological disease research.
HY-P1145A

Glucagon-like peptide 1 (1-37), human TFA
HuGLP-1 TFA
Glucagon Receptor Metabolic Disease

Glucagon-like peptide 1 (1-37), human (TFA) is a highly potent agonist of the GLP-1 receptor.
HY-101331

Phenylbiguanide
N-Phenylbiguanide; PBG; 1-Phenylbiguanide
5-HT Receptor Neurological Disease

Phenylbiguanide is a 5-HT₃ receptor selective agonist with an EC₅₀ of 3.0±0.1 μM.

HY-114025

H4 Receptor antagonist 1	Histamine Receptor	Neurological Disease Endocrinology
H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC₅₀ of 19 nM.

HY-70037A

Cinacalcet hydrochloride AMG-073 hydrochloride	CaSR	Cardiovascular Disease
Cinacalcet hydrochloride (AMG-073 hydrochloride) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease treatment.

HY-17355B

Dexpramipexole (R)-Pramipexole; R-(+)-Pramipexole; KNS-760704	Dopamine Receptor	Neurological Disease
Dexpramipexole(KNS-760704), also known as R-(+)-Pramipexole, is a neuroprotective agent and weak non-ergoline dopamine agonist.

HY-U00206

D2343
Adrenergic Receptor Endocrinology

D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
HY-111271

L 888607
Prostaglandin Receptor Inflammation/Immunology Endocrinology

L 888607 is a potent, and selective CRTH2 (also known as DP₂) agonist with a K_i of 0.8 nM.
HY-15430

Encenicline
EVP-6124
nAChR Neurological Disease

Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
HY-12584

PF-5190457
PF-05190457
GHSR Metabolic Disease Endocrinology

PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pK_i of 8.36.

HY-B0735A

Fenoldopam mesylate Fenoldopam methanesulfonate; SKF-82526 mesylate	Dopamine Receptor	Cardiovascular Disease
Fenoldopam(SKF 82526) mesylate is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist.

HY-B0726

Pilocarpine Hydrochloride
mAChR Neurological Disease

Pilocarpine Hydrochloride is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
HY-50935

Troglitazone
CS-045
PPAR Autophagy Apoptosis Ferroptosis Cancer

Troglitazone is a PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.
HY-130115

IACS-8803
STING Cancer

IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy.

HY-B1832

Prednisone acetate Prednisone 21-acetate	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Prednisone acetate (Prednisone 21-acetate), the acetate salt form of prednisolone, is a glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties.

HY-P1339

Orexin B, human Human orexin B	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human is an endogenous agonist at Orexin receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-101273

BAR502
GPCR19 FXR Autophagy Inflammation/Immunology Neurological Disease

BAR502 is a dual FXR and GPBAR1 agonist with IC₅₀ values of 2 μM and 0.4 μM, respectively.

HY-P1545

ACTH (1-17) α1-17-ACTH	Melanocortin Receptor	Cancer Neurological Disease Endocrinology
ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a K_i of 0.21 nM.

HY-111498

RGX-104
LXR Cancer Inflammation/Immunology

RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
HY-16162

D-3263
TRP Channel Cancer

D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
HY-B1752A

Quinpirole Hydrochloride
(-)-LY 171555
Dopamine Receptor Neurological Disease

Quinpirole Hydrochloride ((-)-LY 171555) is a high-affinity agonist of dopamine D2/D3 receptor.

HY-P1577

Dermorphin Analog	Opioid Receptor	Inflammation/Immunology
Dermorphin Analog is an analog of Dermorphin. Dermorphin is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin.

HY-W015878

5-Aminovaleric acid	Endogenous Metabolite	Metabolic Disease Neurological Disease
5-Aminovaleric acid is believed to act as a methylene homologue of gamma-aminobutyric acid (GABA) and functions as a weak GABA agonist.

HY-B0468

Isoprenaline hydrochloride Isoproterenol hydrochloride	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
Isoprenaline hydrochloride is a non-selective β-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.

HY-100775A

Setogepram PBI-4050	GPR40 GPR84	Metabolic Disease Inflammation/Immunology
Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.

HY-100942

5-Carboxamidotryptamine maleate 5-CT maleate	5-HT Receptor	Neurological Disease
5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT₅ and 5-HT₇ receptors agonist.

HY-19511

GSK2018682	LPL Receptor	Inflammation/Immunology
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC₅₀s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.

HY-14546

Aripiprazole
OPC-14597
5-HT Receptor Neurological Disease

Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.

HY-14261

Vilazodone Hydrochloride EMD 68843 Hydrochloride; SB659746A Hydrochloride	5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT_1A receptor partial agonist.

HY-130116

IACS-8779
STING Cancer

IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy.

HY-103225

S-8510 phosphate SB-737552 phosphate	GABA Receptor	Neurological Disease
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-114165

DJ-V-159
Androgen Receptor Metabolic Disease

DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
HY-P0059

Teriparatide
Human parathyroid hormone-(1-34); hPTH (1-34)
Others Cancer

Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC₅₀ of 2 nM in HEK293 cells.
HY-100328

CB2R-IN-1
Cannabinoid Receptor Neurological Disease

CB2R-IN-1 is a potent cannabinoid CB₂ receptor inverse agonist with a K_i of 0.9 nM.
HY-18100A

PRE-084 hydrochloride
Sigma Receptor Neurological Disease

PRE-084 hydrochloride is a high affinity, selective σ1 agonist, has an IC50 of 44 nM in the sigma receptor assay.
HY-B1006

Pilocarpine nitrate
mAChR Neurological Disease

Pilocarpine nitrate is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
HY-101950

KIN1148
Influenza Virus Infection

KIN1148, a small-molecule IRF3 agonist, is a novel influenza vaccine adjuvant found to enhance flu vaccine efficacy.

HY-B0194A

Tizanidine hydrochloride	Adrenergic Receptor	Cancer Neurological Disease Endocrinology
Tizanidine hydrochloride is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

HY-101420

VUF10460
Histamine Receptor Inflammation/Immunology Endocrinology

VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pK_i of 7.46.
HY-103187

HEMADO
Adenosine Receptor Cancer Inflammation/Immunology

HEMADO is a potent and selective adenosine A₃ receptor agonist with a K_i of 1.1 nM at the human A₃ subtype.

HY-17030

Acamprosate calcium Calcium N-acetylhomotaurinate	GABA Receptor	Neurological Disease
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.

HY-12199

Pitolisant Tiprolisant	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-B0197A

Naratriptan hydrochloride GR-85548A hydrochloride	5-HT Receptor	Neurological Disease
Naratriptan hydrochloride is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.

HY-P1339A

Orexin B, human TFA Human orexin B TFA	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, human (TFA) is an endogenous agonist at Orexin receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-12520A

SKF 38393 hydrochloride (±)-SKF-38393 hydrochloride; SKF-38393A	Dopamine Receptor	Neurological Disease
SKF 38393 hydrochloride is a selective agonist of the dopamine D1 receptor (D1DR) with an IC₅₀ of 110 nM.

HY-16162A

D-3263 hydrochloride
TRP Channel Cancer

D-3263 hydrochloride is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.

HY-B0577

Latanoprost PHXA41	Prostaglandin Receptor	Others
Latanoprost (PHXA41) is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).

HY-109096

Nidufexor LMB763	FXR Autophagy	Inflammation/Immunology
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).

HY-12199B

Pitolisant hydrochloride Ciproxidine; BF 2649	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-A0014

Ramelteon TAK-375	Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon is a highly potent and selective melatonin receptor agonist with K_i values of 14 and 112 pM for human melatonin1 and melatonin2.

HY-B0194

Tizanidine	Adrenergic Receptor	Neurological Disease Endocrinology Cancer
Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

HY-101386

PZM21
Opioid Receptor Neurological Disease

PZM21 is a potent and selective μ opioid receptor agonist with an EC₅₀ of 1.8 nM.

HY-15601

Vesatolimod GS-9620	Toll-like Receptor (TLR) Apoptosis HBV HCV HIV	Inflammation/Immunology
Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC₅₀ of 291 nM.

HY-P1467

[Met5]-Enkephalin, amide 5-Methionine-enkephalin amide	Opioid Receptor	Neurological Disease
[Met5]-Enkephalin, amide is an agonist for δ opioid receptors as well as putative ζ ζ opioid receptors.

HY-15778

AVE 0991
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-P1545A

ACTH (1-17) (TFA) α1-17-ACTH TFA	Melanocortin Receptor	Cancer Neurological Disease Endocrinology
ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a K_i of 0.21 nM.

HY-P0098

[D-Ala2]leucine-enkephalin
Opioid Receptor Cancer

[D-Ala2]leucine-enkephalin, a delta opioid agonist, is a degradation resistant long-acting Leu-enkephalin.

HY-P2273

Calcitonin (human)	CGRP Receptor	Metabolic Disease
Calcitonin human is an endogenous calcitonin receptor agonist.Calcitonin human lowers systemic blood calcium levels and inhibits bone resorption.

HY-B0197

Naratriptan GR-85548A	5-HT Receptor	Neurological Disease
Naratriptan is a selective 5-HT1 receptor subtype agonist and is a triptan drug that is used for the treatment of migraine headaches.

HY-112152

GSK726701A
Prostaglandin Receptor Inflammation/Immunology Neurological Disease Endocrinology

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC₅₀ of 7.4.

HY-101609

Lesopitron dihydrochloride E4424	5-HT Receptor	Neurological Disease
Lesopitron dihydrochloride is a full and selective 5-HT_1A receptor agonist with IC₅₀ of 125 nM in rat hippocampal membranes.

HY-14149

Cisapride
R 51619; (±)-Cisaprid
5-HT Receptor Neurological Disease

Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.

HY-P1349

Orexin B, rat, mouse Rat orexin B; Orexin B (mouse)	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, rat, mouse is an endogenous agonist at Orexin receptor with K_is of 420 and 36 nM for OX1 and OX2, respectively.

HY-16465A

IRL-1620 TFA
Endothelin Receptor Neurological Disease Endocrinology

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.

HY-B0197AS

Naratriptan D3 Hydrochloride GR-85548A D3	5-HT Receptor	Neurological Disease
Naratriptan D3 Hydrochloride is the deuterium labeled Naratriptan, which is a selective 5-HT1 receptor subtype agonist.

HY-B0354A

Urapidil hydrochloride
5-HT Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology

Urapidil HCl is an α1-adrenoceptor antagonist and 5-HT1A receptor agonist.

HY-50911

Turofexorate isopropyl FXR-450; XL335; WAY-362450	FXR Autophagy	Metabolic Disease Cancer
Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC₅₀ of 4 nM.

HY-15306A

Eltrombopag Olamine Eltrombopag diethanolamine salt; SB-497115GR	Thrombopoietin Receptor	Cardiovascular Disease Cancer
Eltrombopag Olamine (Eltrombopag diethanolamine salt) is a thrombopoietin-receptor agonist used to treat low blood platelet counts with chronic immune thrombocytopenia.

HY-13788C

LY 344864 racemate
5-HT Receptor Neurological Disease

LY 344864 racemate is a 5-HT_1F receptor agonist extracted from patent US 5708187 A.
HY-133528

OptoBI-1
TRP Channel Neurological Disease

OptoBI-1 is a photochromic TRPC3 agonist, which asts as a photopharmacological tool to control of neuronal firing.
HY-19774

GNE-0946
ROR Inflammation/Immunology

GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC₅₀ value of 4 nM for HEK-293 cell.

HY-112289

IDH889	Isocitrate Dehydrogenase (IDH)	Cancer
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of *isocitrate dehydrogenase* 1 (IDH1)*. IDH889 has potent selectivity for IDH1 R132 mutations, with IC₅₀s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1^R132H, IDH1^R132C and IDH1^wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC₅₀ of 0.014 μM.

HY-136429

Ethylhydrocupreine Optochin	Bacterial Parasite	Infection
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against *S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC₅₀* of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.

HY-133552

*RORγt Inverse agonist* 10**	ROR	Inflammation/Immunology
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC₅₀ of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R

HY-136429A

Ethylhydrocupreine hydrochloride Optochin hydrochloride	Bacterial Parasite	Infection
Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against *S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC₅₀* of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.

HY-N0175

Cytisinicline Cytisine; Sophorine; Baptitoxine	nAChR	Metabolic Disease
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.

HY-P1467A

[Met5]-Enkephalin, amide TFA 5-Methionine-enkephalin amide (TFA)	Opioid Receptor	Neurological Disease
[Met5]-Enkephalin, amide TFA is an agonist for δ opioid receptors as well as putative ζ ζ opioid receptors.

HY-107675

Desformylflustrabromine hydrochloride Deformylflustrabromine hydrochloride; dFBr hydrochloride	nAChR	Neurological Disease
Desformylflustrabromine hydrochloride is a selective agonist of α₄β₂ neuronal nicotinic acetylcholine receptor (nAChR) with a pEC₅₀ of 6.48.

HY-15401

WAY 163909
5-HT Receptor Cancer

WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a K_i of 10.5±1.1 nM.
HY-16728

Rapastinel
GLYX-13
iGluR Neurological Disease

Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.

HY-P1164

Urotensin II (114-124), human	Urotensin Receptor	Cardiovascular Disease
Urotensin II (114-124), human, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.

HY-17034B

Medetomidine hydrochloride MPV785	Adrenergic Receptor	Neurological Disease Endocrinology
Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.

HY-B0459

Scopine 6,7-Epoxytropine	Adrenergic Receptor	Neurological Disease Endocrinology
Scopine is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.

HY-100907

(±)-Acetylcarnitine chloride Acetyl dl-carnitine chloride	Others	Neurological Disease
(±)-Acetylcarnitine chloride (Acetyl dl-carnitine chloride) is a weak cholinergic agonist with cholinergic properties. (±)-Acetylcarnitine chloride is an important intermediate in lipid metabolism.

HY-101586

Alvameline
Lu 25-109
mAChR Neurological Disease

Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
HY-14351

AC-264613
Protease-Activated Receptor (PAR) Inflammation/Immunology

AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC₅₀ of 7.5.

HY-12199A

Pitolisant oxalate Tiprolisant oxalate	Histamine Receptor	Neurological Disease Endocrinology
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-16916

NS1643
Potassium Channel Autophagy Others

NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K(+) channels with an EC₅₀ of 10.5 μM.
HY-101649

Imiglitazar
TAK-559
PPAR Cardiovascular Disease

Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC₅₀ values of 67 and 31 nM.

HY-P1588

Scyliorhinin II	Neurokinin Receptor	Neurological Disease Endocrinology
Scyliorhinin II is a selective neurokinin-3 receptor agonist, with a K_i of 2.5 nM for neurokinin-3 receptor in rat cerebral cortex.

HY-13510

Cutamesine dihydrochloride SA4503 dihydrochloride; AGY94806 dihydrochloride	Sigma Receptor	Neurological Disease
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes.

HY-N0382

Galangin Norizalpinin; 3,5,7-Trihydroxyflavone	Cytochrome P450 Autophagy	Cancer
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.

HY-13715

Norepinephrine Levarterenol; L-Noradrenaline	Endogenous Metabolite Adrenergic Receptor Autophagy	Endocrinology Cardiovascular Disease
Norepinephrine (Levarterenol; L-Noradrenaline) is a β₁-selective adrenergic receptor agonist with EC₅₀ of 5.37 μM.

HY-13788

LY 344864
5-HT Receptor Neurological Disease

LY 344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
HY-13788A

LY 344864 S-enantiomer
5-HT Receptor Others

LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist.

HY-P1261

Parstatin(mouse)	Protease-Activated Receptor (PAR)	Inflammation/Immunology Cardiovascular Disease
Parstatin(mouse), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.

HY-103410

Carmoxirole hydrochloride EMD 45609 hydrochloride	Dopamine Receptor	Cardiovascular Disease
Carmoxirole hydrochloride (EMD 45609 hydrochloride) is a selective, peripherally acting dopamine D2 receptor agonist and exhibits antihypertensive activities in vivo.

HY-P0244

Dermorphin
Opioid Receptor Neurological Disease

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.
HY-100856

PCO371
Thyroid Hormone Receptor Endocrinology

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.
HY-B0383A

Almotriptan
5-HT Receptor Neurological Disease

Almotriptan is a 5-HT1B/1D-receptor agonist used to treat migraine.

HY-14953

Imepitoin AWD 131-138	GABA Receptor	Neurological Disease
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.

HY-14652

Tamibarotene
Am 80
RAR/RXR Autophagy Apoptosis Cancer

Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
HY-101419

CYM-5541
ML249
LPL Receptor Cardiovascular Disease

CYM-5541 (ML249) is an selective and allosteric S1P₃ receptor agonist with an EC₅₀ between 72 and 132 nM.
HY-12237

SKF 38393 hydrobromide
Dopamine Receptor Neurological Disease

SKF 38393 hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC₅₀ of 110 nM.
HY-14426

L-655708
GABA Receptor Neurological Disease

L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (K_i=0.45 nM).

HY-P2279

Parathyroid hormone (1-34) (rat)	Thyroid Hormone Receptor	Endocrinology Metabolic Disease
Parathyroid hormone (1-34) (rat) is a parathyroid hormone (PTH) receptor agonist, increasing serum PTH levels and bone mass in rats.

HY-101787

FTBMT
Others Neurological Disease

FTBMT is a selective GPR52 agonist with an EC₅₀ of 75 nM. FTBMT has antipsychotic and procognitive properties.
HY-U00014

AVE-8134
PPAR Metabolic Disease

AVE-8134 is a potent PPARα agonist, with EC₅₀ values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.

HY-14831

Arhalofenate MBX 102; JNJ 39659100	PPAR	Metabolic Disease
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

HY-19317

ITE	Aryl Hydrocarbon Receptor	Inflammation/Immunology Cancer
ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a K_i of 3 nM. ITE also has immunosuppressive activity.

HY-15243

Capromorelin Tartrate CP 424391-18	GHSR	Neurological Disease Endocrinology
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

HY-13715A

Norepinephrine hydrochloride Levarterenol hydrochloride; L-Noradrenaline hydrochloride	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology
Norepinephrine hydrochloride (Levarterenol hydrochloride) is a β₁-selective adrenergic receptor agonist with EC₅₀ of 5.37 μM.

HY-P1262

Parstatin(human)	Protease-Activated Receptor (PAR)	Inflammation/Immunology Cardiovascular Disease
Parstatin(human), a cell-penetrating PAR-1 thrombin receptor agonist peptide, is a potent inhibitor of angiogenesis.

HY-N2311

Ibotenic acid (RS)-Ibotenic acid; DL-Ibotenic acid	iGluR	Neurological Disease
Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Q_m) receptor sites.

HY-B0802

Terbutaline sulfate Terbutaline hemisulfate	Adrenergic Receptor Bacterial Antibiotic	Infection Endocrinology Inflammation/Immunology
Terbutaline sulfate is a β2-adrenergic receptor agonist; a fast-acting bronchodilator and a tocolytic to delay premature labor.

HY-14562

TBPB
mAChR Neurological Disease

TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
HY-14413

SR3335
ML 176
ROR Metabolic Disease

SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a K_i of 220 nM.

HY-101300

Cirazoline hydrochloride LD 3098 hydrochloride	Adenosine Receptor	Neurological Disease
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (K_i=120 nM) and only a partial agonist at α1B-AR (K_i= 960 nM) and α1D-AR (K_i=660 nM).

HY-P1309A

*PAR-4 Agonist* Peptide, amide TFA** PAR-4-AP TFA; AY-NH2 TFA	Protease-Activated Receptor (PAR)	Inflammation/Immunology
PAR-4 Agonist Peptide, amide TFA (PAR-4-AP TFA; AY-NH2 TFA) is a proteinase-activated receptor-4 (PAR-4) agonist, which has no effect on either PAR-1 or PAR-2 and whose effects are blocked by a PAR-4 antagonist.

HY-A0007

Rotigotine Hydrochloride N-0923 Hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-131961

Triciferol	VD/VDR HDAC	Cancer
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC₅₀=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.

HY-A0182A

Felypressin acetate PLV-2 acetate	Vasopressin Receptor	Cardiovascular Disease
Felypressin acetate (PLV-2 acetate) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin acetate is widely used in dental procedures.

HY-B0545

Probenecid	TRP Channel Bacterial HIV	Metabolic Disease
Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

HY-100171

PRX933 hydrochloride GW876167 hydrochloride; BVT-933 hydrochloride	5-HT Receptor	Cardiovascular Disease
PRX933 hydrochloride is a 5-HT_2c receptor agonist extracted from patent WO 2014140631 A1.

HY-N0783

Eupatilin	PPAR Autophagy	Inflammation/Immunology Neurological Disease Cancer
Eupatilin, a lipophilic flavonoid isolated from Artemisia species, is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.

HY-100443B

(-)-PX20606 trans isomer (-)-PX-102 trans isomer; (-)-PX-104	FXR Autophagy	Metabolic Disease
(-)-PX20606 trans isomer is a FXR agonist with EC₅₀s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.

HY-19365

AB-MECA
Adenosine Receptor Neurological Disease

AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.

HY-P1164A

Urotensin II (114-124), human TFA	Urotensin Receptor	Cardiovascular Disease
Urotensin II (114-124), human TFA, an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.

HY-P0177

123C4
Ephrin Receptor Metabolic Disease

123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a K_i value of 0.65 μM.
HY-P0244A

Dermorphin TFA
Opioid Receptor Neurological Disease

Dermorphin TFA is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain.

HY-17501

Bambuterol (±)-Bambuterol; KWD-2183	Adrenergic Receptor	Endocrinology
Bambuterol ((±)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.

HY-P1127

Galanin (1-30), human	Neuropeptide Y Receptor	Neurological Disease Endocrinology
Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with K_is of both 1 nM.

HY-10629

LXR-623
WAY 252623
LXR Metabolic Disease Cancer

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC₅₀s of 24 nM and 179 nM, respectively.

HY-17584

Linaclotide	Guanylate Cyclase	Others
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.

HY-110164

AdipoRon hydrochloride	Adiponectin Receptor	Metabolic Disease
AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM, respectively.

HY-P1012

[Sar9,Met(O2)11]-Substance P
Neurokinin Receptor Neurological Disease Endocrinology

[Sar9,Met(O2)11]-Substance P is a tachykinin NK₁ receptor selective agonist.
HY-128604

XY101
ROR Cancer

XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC₅₀ of 30 nM and a K_d of 380 nM.
HY-111200

Vabicaserin hydrochloride
SCA 136
5-HT Receptor Neurological Disease

Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT_2C) receptor-selective agonist with an EC₅₀ of 8 nM.
HY-108526

AC-55649
RAR/RXR Autophagy Others

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC₅₀ of 6.9.

HY-17501A

Bambuterol hydrochloride (±)-Bambuterol hydrochloride; KWD-2183 hydrochloride	Adrenergic Receptor	Endocrinology
Bambuterol hydrochloride ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.

HY-109104

Telratolimod
MEDI9197; 3M-052
Toll-like Receptor (TLR) Cancer

Telratolimod (MEDI9197) is a potent toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.
HY-16685

AGN 205327
RAR/RXR Autophagy Cancer

AGN 205327 is a potent synthetic RARs agonist with EC50 of 3766/734/32 nM for RARα/β/γ respectively; no inhibition on RXR.

HY-15536A

Cebranopadol ((1α,4α)stereoisomer) GRT6005 (1α,4α)stereoisomer	Opioid Receptor	Neurological Disease
Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.

HY-101777

TC-O 9311
GPR139 Neurological Disease

TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC₅₀ of 39 nM.
HY-P0210

DAMGO
Opioid Receptor Cancer

DAMGO is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

HY-10487

JDTic dihydrochloride	Opioid Receptor	Neurological Disease
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

HY-13338S

Mabuterol-D9
Adrenergic Receptor Inflammation/Immunology Cardiovascular Disease

Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor.

HY-12216

Resmetirom MGL-3196; VIA-3196	Thyroid Hormone Receptor	Cardiovascular Disease Endocrinology
Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC₅₀ value of 0.21 μM.

HY-U00371

AR-08	Adrenergic Receptor	Neurological Disease Endocrinology
AR-08 is an agonist of α2-adrenergic receptor, used for the treatment of attention deficit hyperactivety disorder (ADHD).

HY-A0182

Felypressin PLV-2	Vasopressin Receptor	Cardiovascular Disease
Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.

HY-P0090

Calcitonin (salmon) Salmon calcitonin	CGRP Receptor	Cancer
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.

HY-B0659

Brimonidine
UK 14304; AGN190342
Adrenergic Receptor Endocrinology

Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
HY-19863

F-15599
NLX-101
5-HT Receptor Neurological Disease

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.
HY-101192

GSK682753A
EBI2/GPR183 Inflammation/Immunology

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC₅₀ of 53.6 nM.
HY-B0383

Almotriptan malate
PNU180638
5-HT Receptor Neurological Disease

Almotriptan Malate is a 5-HT1B/1D-receptor agonist used to treat migraine.
HY-P0014

Liraglutide
Glucagon Receptor Metabolic Disease

Liraglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist used clinically to treat type 2 diabetes mellitus.

HY-16504

Treprostinil sodium UT-15	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
Treprostinil sodium is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

HY-18687

APNEA
N6-[2-(4-Aminophenyl)ethyl]adenosine
Adenosine Receptor Neurological Disease

APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist.

HY-126047B

(R)-(+)-Anatabine	NF-κB Amyloid-β nAChR	Inflammation/Immunology Neurological Disease
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

HY-111406

Omidenepag isopropyl	Prostaglandin Receptor	Inflammation/Immunology
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug.

HY-121744

PS10	PDHK	Inflammation/Immunology
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC₅₀ of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (K_d= 239 nM) than for Hsp90 (K_d= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase

HY-111269

AZD8848	Toll-like Receptor (TLR)	Inflammation/Immunology
AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.

HY-111098

GSK1702934A
TRP Channel Cardiovascular Disease

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

HY-15848

AdipoRon	Adiponectin Receptor	Metabolic Disease
AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with K_ds of 1.8 and 3.1 μM, respectively.

HY-13773

Motolimod
VTX-2337; VTX-378
Toll-like Receptor (TLR) Cancer

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC₅₀ of approximately 100 nM.

HY-P0298

[Des-Arg9]-Bradykinin	Bradykinin Receptor	Inflammation/Immunology Endocrinology
[Des-Arg9]-Bradykinin is a Bradykinin (B₁) receptor agonist that displays selectivity for B₁ over B₂ receptors.

HY-13443

Exendin-4
Exenatide
Glucagon Receptor Metabolic Disease

Exendin-4 (Exenatide), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC₅₀ of 3.22 nM.

HY-B1893

Fluorometholone	Glucocorticoid Receptor	Inflammation/Immunology
Fluorometholone, a synthetic glucocorticoid, is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic properties. Fluorometholone can be used for the research of dry eye.

HY-102075B

TMP780	ROR	Inflammation/Immunology
TMP780 is an inverse agonist of RORγt with an IC₅₀ of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.

HY-P1012A

[Sar9,Met(O2)11]-Substance P TFA
Neurokinin Receptor Neurological Disease Endocrinology

[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK₁ receptor selective agonist.

HY-14601

Pioglitazone hydrochloride U 72107A; AD 4833	PPAR Ferroptosis	Cancer Metabolic Disease
Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC₅₀s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

HY-15443

AM251	Cannabinoid Receptor	Neurological Disease
AM251 is a selective cannabinoid 1 (CB1) receptor antagonist with an IC₅₀ of 8 nM, also acts as a potent GPR55 agonist with an EC₅₀ of 39 nM.

HY-19134

EMD 56551
5-HT Receptor Neurological Disease

EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.

HY-B0606

Diquafosol tetrasodium INS365	P2Y Receptor	Inflammation/Immunology
Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface, as a topical treatment of dry eye disease.

HY-14557

Pimavanserin
ACP-103
5-HT Receptor Neurological Disease

Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-B0418AS

Loperamide D6 hydrochloride R-18553 D6 hydrochloride	Opioid Receptor Autophagy	Metabolic Disease Neurological Disease
Loperamide D6 hydrochloride (R-18553 D6 hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea.

HY-19946

Eptapirone F 11440	5-HT Receptor	Neurological Disease
Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.

HY-P0210B

DAMGO (TFA)
Opioid Receptor Cancer

DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a K_d of 3.46 nM for native μ-OPR.

HY-109044

Tapinarof WBI-1001; Benvitimod; GSK2894512	Aryl Hydrocarbon Receptor	Inflammation/Immunology
Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC₅₀ of 13 nM. Tapinarof resolves skin inflammation in mice.

HY-P0298A

[Des-Arg9]-Bradykinin acetate	Bradykinin Receptor	Inflammation/Immunology Endocrinology
[Des-Arg9]-Bradykinin acetate is a Bradykinin B₁ receptor agonist that displays selectivity for B₁ over B₂ receptors.

HY-14342

MK-5046
Bombesin Receptor Others

MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).

HY-13967

AMG 837	GPR40	Metabolic Disease
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

HY-14898

AGN 210676 Simenepag	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
AGN 210676 is a selective prostaglandin EP₂ agonist extracted from patent US20070203222A1, Compound example 23, has an EC₅₀ of 5 nM.

HY-P1533A

CRF, bovine TFA Corticotropin Releasing Factor bovine TFA	CRFR	Inflammation/Immunology Endocrinology
CRF, bovine (TFA) is a potent agonist of CRF receptor, and displaces [¹²⁵I-Tyr]ovine CRF with a K_i of 3.52 nM.

HY-16728B

Rapastinel Trifluoroacetate GLYX-13 Trifluoroacetate	iGluR	Neurological Disease
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.

HY-101442

SR9238
LXR Metabolic Disease

SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC₅₀s of 214 nM and 43 nM for LXRα and LXRβ, respectively.

HY-13967A

AMG 837 sodium salt	GPR40	Metabolic Disease
AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

HY-14792

Inolitazone Efatutazone; CS-7017; RS5444	PPAR	Cancer
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

HY-B0823

Acetamiprid	nAChR	Neurological Disease
Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.

HY-14887

Fedovapagon	Vasopressin Receptor	Metabolic Disease
Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC₅₀ of 24 nM, which is being developed for the treatment of nocturia.

HY-10021

Varenicline Tartrate CP 526555-18	nAChR	Neurological Disease
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.

HY-101640

TPA 023
GABA Receptor Neurological Disease

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with K_i of 0.19-0.41 nM.

HY-13443A

Exendin-4 acetate Exenatide acetate	Glucagon Receptor	Metabolic Disease
Exendin-4 acetate (Exenatide acetate), a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC₅₀ of 3.22 nM.

HY-U00215

Ro 41-3290	GABA Receptor	Neurological Disease
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor. Ro 41-3290 is an investigational hypnotic.

HY-13467

AM-1638
GPR40 Metabolic Disease

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC₅₀ of 0.16 μM.

HY-B0121

Sumatriptan succinate GR 43175	5-HT Receptor	Neurological Disease
Sumatriptan succinate (GR 43175) is a serotonin1 (5-HT1) receptor agonist, which is effective in the acute treatment of migraine headache.

HY-75502

Rotigotine N-0437; N-0923	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-N0322

Cholesterol	Estrogen Receptor/ERR Endogenous Metabolite	Metabolic Disease
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.

HY-B0031S

Quetiapine D4 fumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine D4 fumarate is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.

HY-14792B

Inolitazone dihydrochloride Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride	PPAR	Cancer
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

HY-114269

(-)-(S)-B-973B
nAChR Neurological Disease

(-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.

HY-A0007S

Rotigotine D7 Hydrochloride N-0923 D7 Hydrochloride	Dopamine Receptor	Neurological Disease
Rotigotine (N-0923) D7 Hydrochloride is the deuterium labeled Rotigotine(N-0923), which is a dopamine D2 and D3 receptor agonist.

HY-16988A

SR9011 hydrochloride
Autophagy Cancer

SR9011 hydrochloride is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-A0190

Ceruletide Caerulein; Cerulein; FI-6934	Cholecystokinin Receptor	Metabolic Disease Cardiovascular Disease Endocrinology
Ceruletide is a decapeptide and a potent cholecystokinin receptor agonist. Ceruletide is a safe and effective cholecystokinetic agent with a direct spasmogenic effect on the gallbladder muscle and bile ducts.

HY-N6709

Zeranol α-Zearalanol	Estrogen Receptor/ERR	Endocrinology
Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.

HY-111775

LJ570
PPAR Metabolic Disease

LJ570 is a PPARα/PPARγ dual agonist with EC₅₀s of 1.05 and 0.12 μM, respectively.

HY-13044

ADL-5859	Opioid Receptor	Neurological Disease
ADL5859 is a δ-opioid receptor agonist with Ki of 0.8 nM, selectivity against opioid receptor κ, μ, and weak inhibitory activity at the hERG channel.

HY-17568

Nonivamide Pelargonic acid vanillylamide; Nonanoic acid vanillylamide; Pseudocapsaicin	TRP Channel	Neurological Disease
Nonivamide is a agonist, which exhibits 4d-EC₅₀ value of 5.1 mg/L in static toxicity tests.

HY-B1347

Clorprenaline hydrochloride	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Clorprenaline hydrochloride is a β₂-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.

HY-B0106A

Etiracetam UCB 6474	Calcium Channel	Neurological Disease
Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059).

HY-111110

Olorinab APD 371	Cannabinoid Receptor	Neurological Disease
Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB₂) agonist, with an EC₅₀ of 6.2 nM for hCB₂.

HY-124540B

(Rac)-ABT-202 dihydrochloride	nAChR	Neurological Disease
(Rac)-ABT-202 dihydrochloride is a racemate of ABT-202. ABT-202 is an agonist of nicotinic acetylcholine receptors (nAChRs) and can be used as an analgesic.

HY-19995

GSK137647A
GSK 137647
GPR120 Metabolic Disease

GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
HY-100013C

2-PCCA hydrochloride
Others Neurological Disease

2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC₅₀ of 116 nM in HEK293 cells.

HY-N0169

Hyodeoxycholic acid HDCA	Endogenous Metabolite GPCR19	Metabolic Disease
Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC₅₀ of 31.6 µM in CHO cells.

HY-13715B

Norepinephrine bitartrate monohydrate Levarterenol bitartrate monohydrate; L-Noradrenaline bitartrate monohydrate	Adrenergic Receptor Autophagy	Cardiovascular Disease Endocrinology
Norepinephrine bitartrate monohydrate (Levarterenol bitartrate monohydrate; L-Noradrenaline bitartrate monohydrate) is a β₁-selective adrenergic receptor agonist with EC₅₀ of 5.37 μM.

HY-100032

PD 117519
CI947
Adenosine Receptor Neurological Disease

PD 117519 (CI947) is an A_2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
HY-101929

CU-CPT17e
Toll-like Receptor (TLR) Cancer Inflammation/Immunology

CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.

HY-50844

Ibutamoren Mesylate 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-16989

SR9009
Autophagy Cancer

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
HY-B0659A

Brimonidine tartrate
UK 14304 tartrate; AGN190342 tartrate
Adrenergic Receptor Endocrinology

Brimonidine tartrate (UK 14304 tartrate) is a full α2-adrenergic receptor (α2-AR) agonist.

HY-Y0966

Glycine	Endogenous Metabolite iGluR	Neurological Disease
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.

HY-14557A

Pimavanserin tartrate ACP-103 tartrate	5-HT Receptor	Neurological Disease
Pimavanserin tartrate (ACP-103) is a potent 5-HT 2A receptor inverse agonist with pIC₅₀ and pK_i of 8.73 and 9.3, respectively.

HY-16988

SR9011
Autophagy Cancer

SR9011 is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-U00123

Guanoxabenz Hydroxyguanabenz	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanoxabenz is an α2 adrenergic receptor agonist, with a K_i of 4000 nM and the fully activated form 40 nM for an α2A adrenoceptor.

HY-14817

Indeglitazar
PPM 204
PPAR Metabolic Disease

Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.

HY-135601

Cinacalcet metabolite M4	Drug Metabolite	Cardiovascular Disease
Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease.

HY-101869

MK-0343
MRK-409
GABA Receptor Neurological Disease

MK0343 (MRK-409) is an orally bioavailable GABA_A receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic.

HY-P1481A

β-Casomorphin, human TFA Human β-casomorphin 7 TFA	Opioid Receptor	Metabolic Disease Neurological Disease
β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor.

HY-14167

GW842166X	Cannabinoid Receptor	Inflammation/Immunology Neurological Disease
GW842166X is a potent and selective cannabinoid receptor 2 (CB2) agonist with IC₅₀ values of 63 and 91 nM for human and rat CB2, respectively.

HY-P1322

[D-Trp34]-Neuropeptide Y	Neuropeptide Y Receptor	Neurological Disease
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y₅ receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y₁, Y₂, Y₄, and y₆ receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats.

HY-P1314

2-Furoyl-LIGRLO-amide	Protease-Activated Receptor (PAR)	Inflammation/Immunology
2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD₂ value of 7.0..

HY-P1869

Neuropeptide EI, rat	MCHR1 (GPR24) Melanocortin Receptor	Neurological Disease Endocrinology
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms.

HY-N0377

Liquiritigenin 4',7-Dihydroxyflavanone	Estrogen Receptor/ERR	Cancer Inflammation/Immunology Neurological Disease
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC₅₀ of 36.5 nM for activation of the ERE tk-Luc.

HY-P1170

N-terminally acetylated Leu-enkephalin Ac-L-Tyr-Gly-Gly-L-Phe-D-Leu-COOH	Opioid Receptor	Neurological Disease
N-terminally acetylated Leu-enkephalin is the N-terminally acetylated form of Leu-enkephalin. Leu-enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

HY-P0119A

Lixisenatide acetate	Glucagon Receptor	Metabolic Disease
Lixisenatide acetate is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).

HY-100881

TUG-891
GPR120 Metabolic Disease

TUG-891 is a potent and selective agonist for the long chain free fatty acid (LCFA) receptor 4 (FFA4/GPR120).

HY-100441

Treprostinil LRX-15	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
Treprostinil (LRX-15) is a potent DP1 and EP2 agonist with EC₅₀ values of 0.6±0.1 and 6.2±1.2 nM, respectively.

HY-B0459A

Scopine hydrochloride 6,7-Epoxytropine hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
Scopine hydrochloride (6,7-Epoxytropine hydrochloride) is the metabolite of anisodine, which is a α1-adrenergic receptor agonist and used in the treatment of acute circulatory shock.

HY-B0163

Detomidine	Adrenergic Receptor	Neurological Disease Endocrinology
Detomidine, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine produces dose-dependent sedative and analgesic effects.

HY-P0119

Lixisenatide
Glucagon Receptor Metabolic Disease

Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes mellitus (T2DM).

HY-P1308

SLIGRL-NH2 Protease-Activated Receptor-2 Activating Peptide	Protease-Activated Receptor (PAR)	Inflammation/Immunology
SLIGRL-NH2 (Protease-Activated Receptor-2 Activating Peptide) is an agonist of Protease-Activated Receptor-2 (PAR-2).

HY-B0100

Etomidate R 16659	GABA Receptor	Neurological Disease
Etomidate (R 16659) is a potent GABA_A receptor agonist. Etomidate is a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.

HY-101238

Agmatine sulfate	Imidazoline Receptor NO Synthase Endogenous Metabolite	Neurological Disease Cancer
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.

HY-P2519

Protease-Activated Receptor-3 (PAR-3) (1-6), human	Protease-Activated Receptor (PAR)	Inflammation/Immunology
Protease-Activated Receptor-3 (PAR-3) (1-6), human is a proteinase-activated receptor (PAR-3) agonist peptide.

HY-114380

Radioprotectin-1	LPL Receptor	Others
Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA₂), with an EC₅₀ value of 25 nM for murine LPA₂ subtype.

HY-N0361

Dihydrocapsaicin	TRP Channel	Metabolic Disease
Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.

HY-50919

Paricalcitol	VD/VDR	Metabolic Disease
Paricalcitol, a vitamin D analogue, is a vitamin D receptor agonist, used for the prevention and treatment of secondary hyperparathyroidism (excessive secretion of parathyroid hormone) associated with chronic renal failure.

HY-14839

Evatanepag CP-533536 free acid	Prostaglandin Receptor	Cardiovascular Disease Endocrinology
Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.

HY-B1478

Dimaprit dihydrochloride	Histamine Receptor NO Synthase	Endocrinology
Dimaprit dihydrochloride is a selective histamine H2 receptor agonist, it also inhibits nNOS with an IC₅₀ of 49 μM. Dimaprit dihydrochloride can stimulate gastric acid secretion.

HY-101907

ASP7663
TRP Channel Neurological Disease

ASP7663 is an orally active and selective TRPA1 agonist. ASP7663 exerts both anti-constipation and anti-abdominal pain actions.
HY-N7707

Sandacanol
Apoptosis Cancer

Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.

HY-119433

Asoprisnil J867	Progesterone Receptor	Endocrinology
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.

HY-118930

MK-0493	Melanocortin Receptor	Endocrinology Metabolic Disease
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.

HY-B0556

Tetrahydrozoline Tetryzoline	Adrenergic Receptor	Cardiovascular Disease
Tetrahydrozoline (Tetryzoline), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline is widely used for the research of nasal congestion and conjunctival congestion.

HY-P0165

Taspoglutide ITM077; R1583; BIM51077	Glucagon Receptor	Metabolic Disease
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC₅₀ value of 0.06 nM.

HY-16642A

LY2828360	Cannabinoid Receptor	Neurological Disease
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB₂) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

HY-130115A

IACS-8803 disodium
STING Cancer

IACS-8803 disodium is a highly potent cyclic dinucleotide STING agonist. IACS-8803 disodium has a robust systemic antitumor efficacy.

HY-B0556A

Tetrahydrozoline hydrochloride Tetryzoline hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride), a derivative of imidazoline, is an α-adrenergic agonist that causes vasoconstriction. Tetrahydrozoline hydrochloride is widely used for the research of nasal congestion and conjunctival congestion.

HY-103662

GW-870086	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
GW-870086 is a potent anti-inflammatory agent, acting as a glucocorticoid receptor agonist, with a pIC₅₀ of 10.1 in A549 cells expressing NF-κB.

HY-U00373

Revexepride	5-HT Receptor Cytochrome P450	Neurological Disease
Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.

HY-17038S

Agomelatine D6 S-20098 D6	Melatonin Receptor 5-HT Receptor	Neurological Disease
Agomelatine D6 (S-20098 D6) is deuterium labeled Agomelatine. Agomelatine is a specific agonist of MT1 and MT2 receptors .

HY-12761

A-836339
Cannabinoid Receptor Neurological Disease

A-836339 is a cannabinoid CB2 receptor-selective agonist; exhibits high potencies at CB(2) and selectivity over CB(1) receptors.
HY-16684

AGN 195183
RAR/RXR Autophagy Cancer

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.

HY-P1030

Hemokinin 1 (mouse)	Neurokinin Receptor	Endocrinology
Hemokinin 1 (mouse) is a selective agonist of neurokinin-1 receptor, with K_i of 0.175 nM and 560 nM for human NK1 receptor and human NK2 receptor, respectively.

HY-14824

Sofiniclin ABT 894	nAChR	Neurological Disease
Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD).

HY-15382

FTY720 (S)-Phosphate (S)-FTY720P; (S)-FTY720 phosphate	LPL Receptor	Inflammation/Immunology
FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.

HY-B0163A

Detomidine hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
Detomidine hydrochloride, an imidazole derivative, is a potent α2-adrenergic agonist. Detomidine hydrochloride produces dose-dependent sedative and analgesic effects.

HY-108532

AC-261066
RAR/RXR Cancer

AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC₅₀ of 8.0.

HY-B1111

Amitraz BTS-27419	Adrenergic Receptor Monoamine Oxidase Parasite	Infection Endocrinology
Amitraz is a non-systemic acaricide and insecticide, with alpha-adrenergic agonist activity, interaction with octopamine receptors of the central nervous system and inhibition of monoamine oxidases and prostaglandin synthesis.

HY-B1037

Salbutamol Albuterol; AH-3365	Adrenergic Receptor	Neurological Disease Endocrinology
Salbutamol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease (COPD).

HY-100490B

Rilmenidine phosphate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cancer Cardiovascular Disease
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-100490

Rilmenidine	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cancer Cardiovascular Disease
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

HY-110160

Pozanicline dihydrochloride ABT-089 dihydrochloride	nAChR	Neurological Disease
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K_i of 16.7 nM for binding to [³H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K_i of 17 nM while binding to α7 nAChR is insignificant.

HY-P1322A

[D-Trp34]-Neuropeptide Y TFA	Neuropeptide Y Receptor	Neurological Disease
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y₅ receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y₁, Y₂, Y₄, and y₆ receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats.

HY-N0049

Nuciferine	5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine is an antagonist at 5-HT_2A (IC₅₀=478 nM), 5-HT_2C (IC₅₀=131 nM), and 5-HT_2B (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-B0979

Lobeline hydrochloride α-Lobeline hydrochloride; L-Lobeline hydrochloride	nAChR	Neurological Disease
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.

HY-10013B

Taranabant ((1R,2R)stereoisomer) MK0364 (1R,2R)stereoisomer	Cannabinoid Receptor	Others
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.

HY-13556A

Arzoxifene hydrochloride LY 353381 HCl; SERM 3	Estrogen Receptor/ERR	Cancer
Arzoxifene hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.

HY-128113

AG-09/1
Others Inflammation/Immunology

AG-09/1 is a specific formyl peptide receptor 1 (FPR1) agonist. N-formyl peptide receptors (FPR) are important in host defense.

HY-12705A

Bromocriptine mesylate CB-154	Dopamine Receptor Autophagy	Neurological Disease Cancer
Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, which binds D2 dopamine receptor with pK_i of 8.05±0.2.

HY-12381

ML224
NCGC00242364; ANTAG3
TSH Receptor Endocrinology

ML224(NCGC00242364; ANTAG3) is a selective TSHR inverse agonist; inhibits TSH-stimulated cAMP production with an IC50 = 2.3 μM.

HY-B0100A

Etomidate hydrochloride R16659 hydrochloride	GABA Receptor	Neurological Disease
Etomidate hydrochloride (R 16659 hydrochloride) is a potent GABA_A receptor agonist. Etomidate hydrochlorideis a neurological drug and effective parenteral medication and has the potential for management of endogenous hypercortisolaemia.

HY-14417A

(1R,2S)-VU0155041
mGluR Neurological Disease

(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC₅₀ of 2.35 μM.

HY-B0524A

Betahistine dihydrochloride	Histamine Receptor	Endocrinology Inflammation/Immunology Neurological Disease
Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).

HY-B1473

Serotonin hydrochloride 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride	5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a K_i of 44 μM.

HY-U00183

Epanolol Visacor; ICI141292	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Epanolol (Visacor; ICI141292) is a potent β-adrenoceptor partial agonist with a greater affinity for β1- than β2-adrenoceptors.

HY-131103S

Phenylethanolamine A-D3	Adrenergic Receptor	Metabolic Disease Inflammation/Immunology
Phenylethanolamine A-D3 is a deuterium labeled Phenylethanolamine A. Phenylethanolamine A acts as a β-adrenergic agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process.

HY-B1052

Lofexidine hydrochloride Baq-168; MDL-14042	Adrenergic Receptor	Neurological Disease Endocrinology
Lofexidine (hydrochloride) is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.

HY-138626

ACH-000143	Melatonin Receptor	Metabolic Disease
ACH-000143 is a potent and orally active melatonin receptor agonist, with EC₅₀ values of 0.06 nM and 0.32 nM for MT1 and MT2, respectively.

HY-N2253

Neoruscogenin	ROR	Infection Neurological Disease
Neoruscogenin, a member of the steroidal sapogenin family, is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).

HY-P2519A

Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA	Protease-Activated Receptor (PAR)	Inflammation/Immunology
Protease-Activated Receptor-3 (PAR-3) (1-6), human TFA is a proteinase-activated receptor (PAR-3) agonist peptide.

HY-105634A

Nomegestrol acetate	Progesterone Receptor	Endocrinology
Nomegestrol acetate is a potent, highly selective progestogen, which is characterized as a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors, including the androgen and glucocorticoid receptors.

HY-B1052A

Lofexidine	Adrenergic Receptor	Neurological Disease Endocrinology
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.

HY-14261S

Vilazodone D8	5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.

HY-103698A

TLR7/8 agonist 1 dihydrochloride
Toll-like Receptor (TLR) Inflammation/Immunology

TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.

HY-P1314A

2-Furoyl-LIGRLO-amide TFA	Protease-Activated Receptor (PAR)	Inflammation/Immunology
2-Furoyl-LIGRLO-amide TFA is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD₂ value of 7.0..

HY-111492

DIM-C-pPhOCH3
Others Cancer

DIM-C-pPhOCH₃ is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.

HY-103207

Amibegron hydrochloride SR 58611A	Adrenergic Receptor	Neurological Disease Endocrinology
Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC₅₀ of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.

HY-D0237

Betahistine mesylate	Histamine Receptor	Inflammation/Immunology
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).

HY-12434

INT-767
FXR GPCR19 Autophagy Cancer

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC₅₀s of 30 and 630 nM, respectively.

HY-111498A

RGX-104 free Acid	LXR	Cancer Inflammation/Immunology
RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

HY-B0524

Betahistine	Histamine Receptor	Cancer Inflammation/Immunology
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).

HY-P0288

[Leu5]-Enkephalin Leu-enkephalin; Leucine enkephalin; Leucyl-enkephalin	Opioid Receptor Endogenous Metabolite	Neurological Disease
[Leu5]-Enkephalin is a pentapeptide with morphine like properties. [Leu5]-Enkephalin is a five amino acid endogenous peptide that acts as an agonist at opioid receptors.

HY-14218

Ditolylguanidine
1,3-Di-o-tolylguanidine; DTG
Sigma Receptor Neurological Disease

Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor).

HY-15027

5-Aminosalicylic Acid Mesalamine; 5-ASA; Mesalazine	PPAR PAK NF-κB Endogenous Metabolite	Inflammation/Immunology Cancer
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

HY-125946

Latanoprost lactone diol	Prostaglandin Receptor	Inflammation/Immunology
Latanoprost lactone diol is an intermediate in the synthesis of Latanoprost. Latanoprost is a prostaglandin F2α analogue and an agonist for the FP prostanoid receptor, and lowers intraocular-pressure (IOP).

HY-100490A

Rilmenidine hemifumarate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cancer Cardiovascular Disease
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .

HY-10626

T0901317	LXR FXR ROR Apoptosis	Cancer Metabolic Disease Cardiovascular Disease
T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

HY-104042

Vorasidenib AG-881	Isocitrate Dehydrogenase (IDH)	Cancer
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual *mutant isocitrate dehydrogenases* 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC₅₀** ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.

HY-13291

WIN 55,212-2 Mesylate (R)-(+)-WIN 55212	Cannabinoid Receptor	Neurological Disease
WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with K_is of 62.3 and 3.3 nM for human recombinant CB1 and CB2 receptors, respectively.

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-101454

SR0987	ROR	Cancer Inflammation/Immunology
SR0987, a SR1078 analog, is a RORγt agonist, with an EC₅₀ of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.

HY-B0031S1

Quetiapine D4 hemifumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine D4 hemifumarate is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.

HY-P1160

Bay 55-9837	Glucagon Receptor	Metabolic Disease
Bay 55-9837 is a potent and highly selective agonist of VPAC2, with a K_d of 0.65 nM. Bay 55-9837 may be a useful therapy for the research of type 2 diabetes.

HY-P0185

Endomorphin 1	Opioid Receptor	Neurological Disease
Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

HY-103252

Monomethyl fumarate	GPR109A Drug Metabolite	Inflammation/Immunology Neurological Disease
Monomethyl fumarate, an active metabolite of Dimethyl fumarate (DMF), is a potent GPR109A agonist. Monomethyl fumarate has the potential for multiple neuroprotective pathways and other models of retinal disease.

HY-100443A

PX20606 trans racemate PX-102 trans racemate	FXR Autophagy	Metabolic Disease
PX20606 trans racemate (PX-102 trans racemate) is a FXR agonist with EC₅₀s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.

HY-10013A

Taranabant racemate MK-0364 racemate	Cannabinoid Receptor	Neurological Disease
Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1.

HY-10627A

GW3965 hydrochloride	LXR	Cardiovascular Disease Cancer
GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

HY-130012

CO23	Thyroid Hormone Receptor	Metabolic Disease Endocrinology
CO23 is a selective thyroid hormone receptor (TR) α agonist and used for growth and development regulation. CO23 was able to be transported through the blood-brain barrier.

HY-10627

GW3965
LXR Cardiovascular Disease

GW3965 is a potent, selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

HY-14414

GSK4112 SR6452	Autophagy	Metabolic Disease
GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

HY-19770

GSK2981278
ROR Inflammation/Immunology

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.

HY-P0186

Endomorphin 2	Opioid Receptor	Neurological Disease
Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

HY-U00435

Neoseptin 3
Toll-like Receptor (TLR) Cancer

Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation factor 2 (mTLR4/MD-2) agonist with an EC₅₀ of 18.5 μM.

HY-15606

Tanaproget NSP-989	Progesterone Receptor	Endocrinology
Tanaproget (NSP-989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.

HY-N0132A

Synephrine hydrochloride Oxedrine hydrochloride	Adrenergic Receptor Endogenous Metabolite	Neurological Disease Endocrinology
Synephrine hydrochloride (Oxedrine hydrochloride) is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium, it has sympathomimetic and structural similarities to ephedra and ephedrine alkaloids.

HY-U00450

4-O-Methyl honokiol	PPAR NF-κB	Cancer Inflammation/Immunology
4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.

HY-N0132

Synephrine Oxedrine	Adrenergic Receptor Endogenous Metabolite	Neurological Disease Endocrinology
Synephrine (Oxedrine) is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium, it has sympathomimetic and structural similarities to ephedra and ephedrine alkaloids.

HY-19381

WAY-151932 VNA-932; WAY-VNA 932	Vasopressin Receptor	Metabolic Disease Endocrinology
WAY-151932 is a vasopressin V₂-receptor agonist with IC₅₀ of 80.3 nM and 778 nM in human-V₂ binding and V_1a binding assay.

HY-111343

ONC212
Apoptosis Cancer Endocrinology

ONC212, a fluorinated-ONC201 analogue, is a promising anti-cancer agent and also a selective agonist of GPR132. ONC212 also induces apoptosis.

HY-A0279A

Pristinamycin IA Mikamycin B; Mikamycin IA	Bacterial	Others
Pristinamycin IA (Mikamycin B;Mikamycin IA), a biologically active decapeptide isolated from the skin of the Australian frog Hyla caerulea, is a potent cholecystokinetic agent, and acts as a cholecystokinin receptor agonist.

HY-124498

Oxantel CP-14445	nAChR Parasite	Infection
Oxantel (CP-14445), a m-oxyphenol derivative of Pyrantel (HY-12641), is a N-subtype AChR agonist. Oxantel is an anthelmintic, with excellent trichuricidal properties.

HY-13008

MK-0354
GPR109A Cardiovascular Disease

MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.

HY-18286

NCGC00229600	TSH Receptor	Endocrinology
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.

HY-P1308A

SLIGRL-NH2 TFA Protease-Activated Receptor-2 Activating Peptide TFA	Protease-Activated Receptor (PAR)	Inflammation/Immunology
SLIGRL-NH2 TFA (Protease-Activated Receptor-2 Activating Peptide TFA) is an agonist of Protease-Activated Receptor-2 (PAR-2).

HY-N3977

Grifolic acid	GPR120	Inflammation/Immunology
Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).

HY-P0199

Pancreatic Polypeptide, human Human pancreatic polypeptide	Neuropeptide Y Receptor	Metabolic Disease Endocrinology
Pancreatic Polypeptide, human is a C-terminally amidated 36 amino acid peptide, which acts as a neuropeptide Y (NPY) Y4/Y5 receptor agonist.

HY-121251

BI-167107	Adrenergic Receptor	Cancer Neurological Disease Endocrinology
BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant K_d of 84 pM.

HY-P1333

Dynorphin A	Opioid Receptor	Neurological Disease
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).

HY-19650

Pumosetrag Hydrochloride MKC-733; DDP-733	5-HT Receptor	Metabolic Disease
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.

HY-114118

Semaglutide	Glucagon Receptor	Metabolic Disease
Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide has the potential for type 2 diabetes treatment.

HY-110238

MK6-83
TRP Channel Metabolic Disease

MK6-83 is a new candidate agonist of TRPML1 with an improved efficacy and potency. MK6-83 has the potential for Mucolipidosis type IV study.

HY-A0181A

Adenosine 5'-monophosphate monohydrate 5'-AMP monohydrate	Adenosine Receptor HSV	Infection Neurological Disease
Adenosine 5'-monophosphate monohydrate is an adenosine A₁ receptor agonist. Adenosine 5'-monophosphate monohydrate has significant antiviral activity against HSV-1 and HSV-2.

HY-20019

L-165041	PPAR	Metabolic Disease
L-165041 is a cell permeable PPARδ agonist, with K_is of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

HY-13740

Resiquimod R848; S28463	Toll-like Receptor (TLR) HCV	Inflammation/Immunology Cancer
Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.

HY-101325

BRL 37344 sodium BRL 37344A	Adrenergic Receptor	Metabolic Disease Endocrinology
BRL 37344 sodium (BRL 37344A) is a specific β3-adrenergic receptor agonist. BRL 37344 sodium treatment significantly lowers the body weight of obese mice.

HY-N2148

Cytosporone B
Csn-B; Dothiorelone G
Others Cancer

Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC₅₀ of 0.278 nM.

HY-112219A

H3R-IN-1 Hydrochloride	Histamine Receptor	Inflammation/Immunology Endocrinology
H3R-IN-1 Hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.

HY-P2287

Cortagine	CRFR	Neurological Disease
Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC₅₀ of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.

HY-105634

Nomegestrol	Progesterone Receptor	Endocrinology
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a K_d of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.

HY-106266

Chiglitazar
PPAR Metabolic Disease

Chiglitazar is a PPARα/γ dual agonist, with EC₅₀s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

HY-101372A

Oxotremorine M iodide	mAChR	Neurological Disease
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.

HY-100815B

(RS)-AMPA (±)-AMPA	iGluR	Neurological Disease
(RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors.

HY-P1180

Pam3CSK4
Pam3Cys-Ser-(Lys)4
Toll-like Receptor (TLR) Infection Inflammation/Immunology

Pam3CSK4 is a toll-like receptor 1/2 (TLR1/2) agonist with an EC₅₀ of 0.47 ng/mL for human TLR1/2.

HY-120384

AZD-0284	ROR	Inflammation/Immunology
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.

HY-13861

GW7647
PPAR Cardiovascular Disease

GW7647 is a potent PPARα agonist, with EC₅₀s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

HY-B1415

Clofibric acid Chlorofibrinic acid	PPAR Drug Metabolite	Others
Clofibric acid (Chlorofibrinic acid), the pharmaceutically active metabolite of lipid regulators Clofibrate, Etofibrate and Etofyllinclofibrate, is a PPARα agonist which exhibits hypolipidemic effects. Clofibric acid also is an herbicide.

HY-A0010

Eletriptan hydrobromide
Eletriptan HBr
5-HT Receptor Neurological Disease

Eletriptan HBr is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

HY-123291

SM-276001	Toll-like Receptor (TLR) IFNAR	Cancer Inflammation/Immunology
SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer.

HY-106147

Frakefamide	Opioid Receptor	Neurological Disease
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

HY-18295

Erteberel LY500307	Estrogen Receptor/ERR	Neurological Disease
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with K_i and EC₅₀ of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.

HY-15484

Pifithrin-α hydrobromide Pifithrin hydrobromide; PFTα hydrobromide	MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis	Cancer
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.

HY-16639

ML314	Neurotensin Receptor	Neurological Disease Endocrinology
ML314 is a potent molecule agonist of NTR1 (EC50 = 1.9 μM); showed good selectivity against NTR2 and GPR35, but did not stimulate Ca2+ mobilization.

HY-N6691

Veratridine 3-Veratroylveracevine	Sodium Channel	Neurological Disease
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM.

HY-19996

AH-7614	GPR120	Metabolic Disease
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC₅₀s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC₅₀<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.

HY-10349A

WAY-100635 Maleate	5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 maleate has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D₄ receptor agonist.

HY-119222

GSK256073	GPR109A	Metabolic Disease
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC₅₀ of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2

HY-P1321

GR231118 1229U91; GW1229	Neuropeptide Y Receptor	Neurological Disease
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pK_i of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC₅₀=8.6; pK_i=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide Y Y6 receptor (pK_i= 8.8).

HY-131032

KI-7	Adenosine Receptor	Others
KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC₅₀=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC₅₀s of 2390 nM and 2550 nM, respectively.

HY-P1321A

GR231118 TFA 1229U91 TFA; GW1229 TFA	Neuropeptide Y Receptor	Neurological Disease
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pK_i of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC₅₀=8.6; pK_i=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pK_i= 8.8).

HY-15124

(S)-(-)-Bay-K-8644
Calcium Channel Cardiovascular Disease

(S)-(-)-Bay-K-8644 is an agonist of L-type Ca²⁺ channel. (S)-(-)-Bay-K-8644 activates Ba²⁺ currents (I_Ba) (EC₅₀=32 nM).

HY-B0584

Travoprost Fluprostenol isopropyl ester; AL6221; Flu-Ipr	Prostaglandin Receptor	Endocrinology
Travoprost (Fluprostenol isopropyl ester), an isopropyl ester prodrug, is a high affinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension.

HY-111809

N6-Ethyladenosine	Adenosine Receptor	Others
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with K_is of 4.9 and 4.7 nM for hA₁AR and hA₃AR, respectively.

HY-15564

AR 231453
GPR119 Metabolic Disease

AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.

HY-B0820

Nitenpyram	nAChR	Neurological Disease
Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC₅₀ of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.

HY-P1180A

Pam3CSK4 TFA Pam3Cys-Ser-(Lys)4 TFA	Toll-like Receptor (TLR)	Infection Inflammation/Immunology
Pam3CSK4 TFA is a toll-like receptor 1/2 (TLR1/2) agonist with an EC₅₀ of 0.47 ng/mL for human TLR1/2.

HY-106157

Donitriptan
5-HT Receptor Neurological Disease

Donitriptan is a potent, high efficacy agonist at 5-HT_1B/1D receptors with pK_is of 9.4 and 9.3, respectively.

HY-G0014

Quetiapine sulfoxide Quetiapine S-oxide	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.

HY-105170B

ABT-418 hydrochloride	nAChR	Neurological Disease
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.

HY-13720A

Pergolide mesylate Pergolide methanesulfonate; LY127809	Dopamine Receptor	Neurological Disease
Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D₁ and D₂ receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research.

HY-G0014B

Quetiapine sulfoxide hydrochloride Quetiapine S-oxide hydrochloride	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide hydrochloride (Quetiapine S-oxide hydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.

HY-P2036

FSL-1
Toll-like Receptor (TLR) Antibiotic Infection

FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.

HY-106025

Radequinil AC-3933	GABA Receptor	Neurological Disease
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with K_is of 5.15 and 6.11 nM, respectively.

HY-P1125

4-CMTB
Others Others

4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC₅₀=6.38).

HY-G0014A

Quetiapine sulfoxide dihydrochloride Quetiapine S-oxide dihydrochloride	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide dihydrochloride (Quetiapine S-oxide dihydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic. Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist.

HY-18760

LY2812223	mGluR	Neurological Disease
LY2812223 is a highly potent, functionally selective mGlu₂ receptor agonist with mGlu₂ binding affinity for mGlu₂ and mGlu₃ (K_i=144 nM and 156 nM, respectively).

HY-100155

4-IBP	Sigma Receptor	Cancer
4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 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-100271

Org41841	TSH Receptor	Endocrinology
Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC₅₀s of 0.2 and 7.7 μM, respectively.

HY-18678A

Bremelanotide Acetate PT-141 Acetate	Melanocortin Receptor	Endocrinology
Bremelanotide Acetate (PT-141 Acetate), a synthetic peptide analogue of α-MSH, is an agonist at melanocortin receptors including the MC3R and MC4R for the treatment of sexual dysfunction.

HY-101085

SKL2001	Wnt β-catenin	Cancer
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.

HY-106007

Trabodenoson INO-8875	Adenosine Receptor	Inflammation/Immunology
Trabodenoson (INO-8875), an adenosine mimetic, is a highly selective Adenosine A1 receptor agonist. Trabodenoson (INO-8875) is used in the study for Primary Open-Angle Glaucoma.

HY-B1270

Isoxsuprine hydrochloride	Adrenergic Receptor iGluR	Neurological Disease Endocrinology
Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with K_is of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.

HY-135392

N-Desmethyl Pimavanserin AC-279	Drug Metabolite	Neurological Disease
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-14608

(S)-Glutamic acid (+)-L-Glutamic acid	Endogenous Metabolite iGluR Ferroptosis Apoptosis	Neurological Disease
(S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.

HY-P1160A

Bay 55-9837 TFA	Glucagon Receptor	Metabolic Disease
Bay 55-9837 TFA is a potent and highly selective agonist of VPAC2, with a K_d of 0.65 nM. Bay 55-9837 TFA may be a useful therapy for the research of type 2 diabetes.

HY-15043

ELN-441958	Bradykinin Receptor	Cancer Endocrinology
ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM.

HY-131106S

Clorprenaline D7	Adrenergic Receptor	Endocrinology Inflammation/Immunology
Clorprenaline D7 is a deuterium labeled Clorprenaline. Clorprenaline is a β2-adrenergic receptor agonist that is implicated in bronchial expansion. Clorprenaline has the potential for asthma research.

HY-12694

Prucalopride succinate
R-108512
5-HT Receptor Others

Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.

HY-B0287

Clofibrate	PPAR	Metabolic Disease
Clofibrate is an agonist of PPAR, with EC₅₀s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.

HY-15655

GW1929	PPAR	Metabolic Disease Neurological Disease
GW1929 is a potent PPAR-γ agonist, with a pK_i of 8.84 for human PPAR-γ, and pEC₅₀s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively.

HY-13410

Xanomeline oxalate LY246708 oxalate	mAChR	Neurological Disease
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.

HY-10678

BMS-687453	PPAR	Cardiovascular Disease
BMS-687453 is a potent and selective PPARα agonist, with an EC₅₀ and IC₅₀ of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

HY-19483

ABT-670	Dopamine Receptor	Neurological Disease
ABT-670 is a selective, oral bioavailable agonist of dopamine D₄ receptor, with EC₅₀ of 89 nM, 160 nM, and 93 nM for human D₄, ferret D₄, and rat D₄, respectively.

HY-106147B

Frakefamide TFA	Opioid Receptor	Neurological Disease
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.

HY-103005

Ramelteon metabolite M-II	Melatonin Receptor	Neurological Disease Endocrinology
Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC₅₀s of 208 pM, 1470 pM for human melatonin receptors (MT₁ or MT₂). Ramelteon is a selective melatonin agonist.

HY-19937

Saroglitazar	PPAR	Metabolic Disease
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC₅₀ values of 0.65 pM and 3 nM in HepG2 cells, respectively.

HY-W013372

7,8-Dihydroxyflavone	Trk Receptor Apoptosis	Neurological Disease
7,8-Dihydroxyflavone is a potent and selective TrkB agonist that mimics the physiological actions of Brain-derived neurotrophic factor (BDNF). Displays therapeutic efficacy toward various neurological diseases.

HY-N0163

Magnolol	RAR/RXR PPAR Autophagy Bacterial	Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC₅₀ values of 10.4 µM and 17.7 µM, respectively.

HY-16751

Ralinepag APD811	Prostaglandin Receptor	Cardiovascular Disease Endocrinology
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC₅₀s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

HY-105124A

Bufuralol hydrochloride Ro 3-4787 hydrochloride	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Bufuralol hydrochloride (Ro 3-4787 hydrochloride) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate.

HY-105040C

Pomaglumetad methionil hydrochloride LY2140023 hydrochloride	mGluR	Neurological Disease
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. Pomaglumetad methionil hydrochloride has the potential for schizophrenia research.

HY-104049

Lanifibranor IVA337	PPAR	Metabolic Disease Cancer
Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC₅₀s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.

HY-P1016A

BQ-3020 TFA	Endothelin Receptor	Cardiovascular Disease Endocrinology
BQ-3020 (TFA) is a selective agonist of ET_B receptor, inhibits [¹²⁵I]ET-1 binding to ET_B receptor with an IC₅₀ of 0.2 nM in cerebellum, and causes vasoconstriction.

HY-14221

Siramesine Lu 28-179	Sigma Receptor Ferroptosis	Cancer
Siramesine(Lu 28-179) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.

HY-N6642

Ankaflavin	PPAR	Cancer Inflammation/Immunology
Ankaflavin, isolated from Monascus-Fermented red rice, is a PPARγ agonist with anti-inlfammatory activity. Ankaflavin exhibits selective cytotoxic effect and induces cell death on cancer cells.

HY-P2625

GLP-2(3-33)
Glucagon Receptor Metabolic Disease

GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC₅₀=5.8 nM).

HY-17416

Guanfacine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.

HY-14296

PF-610355	Adrenergic Receptor	Inflammation/Immunology
PF-610355 is a long-acting inhaled β₂-adrenoreceptor agonist, with an EC₅₀ of 0.26 nM. PF-610355 has the potential for the study of asthma and COPD.

HY-19937A

Saroglitazar Magnesium	PPAR	Metabolic Disease
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC₅₀ values of 0.65 pM and 3 nM in HepG2 cells, respectively.

HY-12222

Obeticholic acid INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid	FXR Autophagy	Others
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC₅₀ of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.

HY-10622

PF-00446687
Melanocortin Receptor Endocrinology

PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.

HY-100806

Kynurenic acid Quinurenic acid	iGluR Endogenous Metabolite Apoptosis	Inflammation/Immunology Neurological Disease Endocrinology
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.

HY-17034

Medetomidine	Adrenergic Receptor	Neurological Disease Endocrinology
Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively).

HY-14221A

Siramesine hydrochloride Lu 28-179 hydrochloride	Sigma Receptor Ferroptosis	Cancer
Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.

HY-112217A

PSEM 89S TFA	nAChR	Neurological Disease
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.

HY-107982

VU6005649
mGluR Neurological Disease

VU6005649 is a CNS penetrant mGlu_7/8 receptor agonist with EC₅₀s of 0.65 μM and 2.6 μM for mGlu₇ receptor and mGlu₈ receptor, respectively.

HY-11035

WAY-262611	β-catenin	Cancer
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC₅₀ of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.

HY-114118A

Semaglutide TFA	Glucagon Receptor	Metabolic Disease
Semaglutide TFA, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide TFA has the potential for type 2 diabetes treatment.

HY-U00036A

Naveglitazar LY519818	PPAR	Metabolic Disease
Naveglitazar (LY519818) is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.

HY-107512

Kynurenic acid sodium	iGluR Apoptosis	Inflammation/Immunology Neurological Disease Endocrinology
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.

HY-W017500

N-Methyl-DL-aspartic acid	iGluR	Neurological Disease
N-Methyl-DL-aspartic acid is a glutamate analogue and acts as a potent neuronal excitant. N-Methyl-DL-aspartic acid is a NMDA receptor* agonist* and can be used for neurological diseases research.

HY-12560D

PNU-282987 S enantiomer free base	nAChR	Others
PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.

HY-13713

LY377604	Adrenergic Receptor	Metabolic Disease Endocrinology
LY377604 is a human β₃-adrenergic receptor agonist with an EC₅₀ of 2.4 nM and also a β₁- and β₂-adrenergic receptor antagonist.

HY-13715C

Noradrenaline tartrate Levarterenol tartrate; L-Noradrenaline tartrate	Endogenous Metabolite Adrenergic Receptor Autophagy	Endocrinology Cardiovascular Disease
Norepinephrine tartrate (Levarterenol tartrate), a naturally occurring chemical in the body that acts as both a stress hormone and neurotransmitter, is a β₁-selective adrenergic receptor agonist with EC₅₀ of 5.37 μM.

HY-136290

Mc-Dexamethasone	Drug-Linker Conjugates for ADC	Cancer
Mc-Dexamethasone is a drug-linker conjugate for ADC. Mc-Dexamethasone is made toxin Dexamethasone (HY-14648) conjugated to the non-cleavable MC linker. Dexamethasone is a glucocorticoid receptor agonist.

HY-10680

MK-6892	GPR109A	Cancer
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. K_i and GTPγS EC₅₀ of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.

HY-14546S

Aripiprazole (D8) OPC-14597 D8	5-HT Receptor	Neurological Disease
Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.

HY-B2054

Tebufenozide
Apoptosis Others

Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.

HY-113970A

Nebracetam hydrochloride WEB 1881 FU hydrochloride	mAChR	Neurological Disease
Nebracetam hydrochloride, a nootropic M₁-muscarinic agonist, induces a rise of intracellular Ca²⁺ concentration. Nebracetam hydrochloride exhibits an EC₅₀ of 1.59 mM for elevating [Ca²⁺]_i.

HY-14608A

L-Glutamic acid monosodium salt Monosodium glutamate	iGluR Apoptosis Ferroptosis	Neurological Disease
L-Glutamic acid monosodium salt acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). (S)-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.

HY-N6825

Hydroxy-α-sanshool	TRP Channel Endogenous Metabolite	Neurological Disease
Hydroxy-α-sanshool is an alkylamide isolated from pepper, acts as a TRPA1 covalent and TRPV1 non-covalent agonist, with EC₅₀s of 69 and 1.1 µM, respectively.

HY-103546

BETP
Glucagon Receptor Metabolic Disease

BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC₅₀s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively.

HY-116214

Cyprodinil	Fungal Androgen Receptor	Infection Endocrinology
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC₅₀s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC₅₀=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC₅₀=15.1 µM).

HY-103409

ABT-724 trihydrochloride	Dopamine Receptor	Neurological Disease
ABT-724 trihydrochloride is a potent and highly selective dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

HY-16056

Arbutamine	Adrenergic Receptor	Cardiovascular Disease
Arbutamine is a short-acting, potent and nonselective β-adrenoceptor agonist that increases heart rate, cardiac contractility, and systolic blood pressure. Arbutamine is a catecholamine for a pharmacological cardiac stress agen.

HY-104070

LG-100064	RAR/RXR Autophagy	Cancer
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC₅₀s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.

HY-P1317

Nociceptin (1-13), amide	Opioid Receptor	Neurological Disease
Nociceptin (1-13), amide is a potent ORL1 (OP4) receptor agonist with a pEC₅₀ of 7.9 for mouse vas deferens and a K_i of 0.75 nM for binding to rat forebrain membranes.

HY-17642

Omidenepag	Prostaglandin Receptor	Endocrinology
Omidenepag,a pharmacologically active form of Omidenepag Isopropyl, is a selective, non-prostanoid EP2 receptor agonist, with an EC₅₀ of 1.1 nM. Omidenepag shows binding affinities (IC₅₀) 10 nM for h-EP2.

HY-133113

7-Desmethyl-agomelatine	5-HT Receptor	Neurological Disease
7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C.

HY-128770

LY3154207	Dopamine Receptor	Neurological Disease
LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀=3 nM).

HY-P0186A

Endomorphin 2 TFA	Opioid Receptor	Neurological Disease
Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa₃ binding sites, with K_i value between 20 and 30 nM.

HY-P1731

Tirzepatide LY3298176	Glucagon Receptor	Metabolic Disease
Tirzepatide (LY3298176) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.

HY-120160

Darglitazone CP-86325	PPAR	Metabolic Disease Neurological Disease
Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research.

HY-10957

L-692429 MK-0751	GHSR	Metabolic Disease
L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a K_i of 63 nM.

HY-18941

Eglumegad LY354740; Eglumetad	mGluR	Neurological Disease
Eglumegad (LY354740) is a highly potent and selective group II (mGlu2/3) receptor agonist with IC₅₀s of 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively.

HY-103007

TC-G-1008 GPR39-C3	GHSR	Metabolic Disease Endocrinology
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC₅₀ values of 0.4 and 0.8 nM for rat and human receptors respectively.

HY-P1731B

Tirzepatide hydrochloride LY3298176 hydrochloride	Glucagon Receptor	Metabolic Disease
Tirzepatide hydrochloride (LY3298176 hydrochloride) is a dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist that is being developed for the treatment of type 2 diabetes.

HY-14554

Pomaglumetad methionil anhydrous LY2140023	mGluR	Neurological Disease
Pomaglumetad methionil anhydrous (LY2140023) is an orally active, methionine prodrug of the selective mGlu2/3 receptor agonist LY404039. LY2140023 has the potential for schizophrenia research.

HY-108529

BMS493	RAR/RXR	Metabolic Disease
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation.

HY-128064

Adenosine amine congener ADAC	Adenosine Receptor	Inflammation/Immunology Neurological Disease
Adenosine amine congener (ADAC) is a selective A1 adenosine receptor agonist, can ameliorate noise- and Cisplatin-induced cochlear injury. Adenosine amine congener also has neuroprotective effects.

HY-13956

Pioglitazone U 72107	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

HY-110241

Dianicline dihydrochloride	nAChR	Neurological Disease
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.

HY-B1500

2,2,2-Trichloroethanol	Potassium Channel	Neurological Disease
2,2,2-Trichloroethanol, the active form of the sedative hypnotic drug chloral hydrate, is an agonist for the nonclassical K_2P channels TREK-1 (KCNK2) and TRAAK (KCNK4).

HY-N0164

Matrine Matridin-15-one; Vegard; α-Matrine	Opioid Receptor Autophagy Mitophagy Ferroptosis	Cancer
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.

HY-135270

*ADRA1D receptor agonist* 1**	Adrenergic Receptor	Endocrinology
ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α_1D adrenoceptor antagonist, with a K_i of 1.6 nM.

HY-15378

Talibegron hydrochloride ZD2079 hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Talibegron hydrochloride (ZD2079 hydrochloride) is a potent β3-adrenoceptor agonist with a pD₂ of 3.72 on phenylephrine-preconstricted rat mesenteric artery. Talibegron hydrochloride has potent vasorelaxant effect.

HY-113044

Uridine diphosphate glucose	Endogenous Metabolite P2Y Receptor	Metabolic Disease
Uridine diphosphate glucose is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine diphosphate glucose is an agonist of the P2Y₁₄ receptor, a neuroimmune system GPCR^1.

HY-12707

Piribedil	Adrenergic Receptor Dopamine Receptor	Neurological Disease Endocrinology
Piribedil is a dopamine D₂ receptor (D₂R) agonist which also displays antagonist property at hα_1A-adrenoceptor (hα_1A-AR).

HY-112692

AT-121	Opioid Receptor	Neurological Disease
AT-121 is a bifunctional nociception and mu opioid receptor agonist, with K_is of 3.67 and 16.49 nM, respectively. AT-121 is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.

HY-119943

PF-06256142	Dopamine Receptor	Neurological Disease
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC₅₀ and K_i of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.

HY-N6868

Dimethyl lithospermate B dmLSB	Sodium Channel	Cardiovascular Disease
Dimethyl lithospermate B (dmLSB) is a selective Na⁺ channel agonist. Dimethyl lithospermate B slows inactivation of sodium current (INa), leading to increased inward current during the early phases of the action potential (AP).

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-P1348

GLP-1 moiety from Dulaglutide	Glucagon Receptor	Metabolic Disease
GLP-1 moiety from Dulaglutide is a 31-amino acid fragment of Dulaglutide which is a glucagon-like peptide 1 receptor (GLP-1) agonist, extracted from patent US 20160369010 A1.

HY-19864

Aganepag AGN 210937	Prostaglandin Receptor	Inflammation/Immunology
Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC₅₀ of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.

HY-103178

MRE3008F20	Adenosine Receptor	Cancer
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC₅₀ of 5 nM.

HY-112692A

AT-121 hydrochloride	Opioid Receptor	Neurological Disease
AT-121 hydrochloride is a bifunctional nociception and mu opioid receptor agonist, with K_is of 3.67 and 16.49 nM, respectively. AT-121 hydrochloride is a safe, non-addictive analgesic, and shows antinociceptive and antiallodynic effects.

HY-128344

BR102375	PARP Apoptosis	Metabolic Disease
BR102375 is a non-TZD peroxisome proliferator-activated receptor γ (PPAR γ) full agonist for the treatment of type 2 diabetes, reveals EC₅₀ value of 0.28 μM and A_max ratio of 98%.

HY-B1276A

Metaproterenol Orciprenaline	Adrenergic Receptor	Inflammation/Immunology Cardiovascular Disease Endocrinology
Metaproterenol (Orciprenaline) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC₅₀ of 68 nM. Metaproterenol also has anti-inflammatory activity.

HY-14823

Sobetirome GC-1; QRX-431	Thyroid Hormone Receptor	Metabolic Disease Endocrinology
Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC₅₀ of 0.16 μM.

HY-101370

2-Methylthio-ATP tetrasodium	Others	Metabolic Disease
2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation.

HY-P1167

[Orn5]-URP	Urotensin Receptor	Cardiovascular Disease
[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP displays no agonist activity.

HY-107773

GSK3004774	CaSR	Metabolic Disease
GSK3004774 is a potent, nonabsorbable agonist of CaSR, with an pEC₅₀ of 7.3, 6.6 and 6.5 for human, mouse and rat CaSR, respectively. GSK3004774 shows an EC₅₀ of 50 nM for human CaSR.

HY-U00036

Naveglitazar racemate LY519818 racemate	PPAR	Metabolic Disease
Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.

HY-N0630

Shanzhiside methyl ester	Glucagon Receptor	Neurological Disease
Shanzhiside methy lester is isolated from L. rotata. Shanzhiside methyl ester is a small molecule glucagon-like peptide-1 (GLP-1) receptor agonist and has the ability to induce anti-allodynic tolerance.

HY-121885

LMD-009	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-14171S

Bexarotene D4 LGD1069 D4	RAR/RXR Autophagy	Cancer
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.

HY-14330

ABT-724	Dopamine Receptor	Neurological Disease
ABT-724 is a potent and highly selective dopamine D₄ receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D₄ receptor. ABT-724 is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM). ABT-724 has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.

HY-19733

Lumateperone tosylate ITI-007 tosylate	5-HT Receptor Dopamine Receptor	Neurological Disease
Lumateperone tosylate (ITI-007 tosylate) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).

HY-19608

GSK1016790A	TRP Channel Calcium Channel	Metabolic Disease Cardiovascular Disease
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca²⁺ influx and elevate intracellular Ca²⁺ in HEK cells.

HY-14728

Aleglitazar R1439; RO0728804	PPAR	Metabolic Disease
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC₅₀s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

HY-P1418

DPC-AJ1951	Thyroid Hormone Receptor	Endocrinology
DPC-AJ1951, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.

HY-N0170

Indole-3-carbinol I3C; 3-Indolemethanol	NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite	Cancer
Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).

HY-12848

SAG	Smo	Cancer
SAG is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

HY-70081A

Sumanirole maleate U-95666E; PNU-95666	Dopamine Receptor	Neurological Disease
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED₅₀ of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.

HY-135895

Detomidine carboxylic acid	Adrenergic Receptor	Endocrinology Neurological Disease
Detomidine carboxylic acid is the major urinary metabolite of Detomidine. Detomidine is a synthetic α2-adrenergic agonist and an animal analgesic sedative. Detomidine also has cardiac and respiratory effects and an antidiuretic action.

HY-109137

Selgantolimod GS-9688	Toll-like Receptor (TLR) HBV	Infection
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.

HY-B0154

Fluticasone (propionate)	Glucocorticoid Receptor Enterovirus Endogenous Metabolite	Infection Endocrinology Inflammation/Immunology
Fluticasone propionate, a potent topical anti-inflammatory corticosteroid, is a selective glucocorticoid receptor agonist, with an absolute affinity (K_D) of 0.5 nM. Fluticasone propionate shows little or no activity at other steroid receptors. Anti-viral activity.

HY-111149A

PS372424 hydrochloride	CXCR	Inflammation/Immunology
PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.

HY-12848C

SAG dihydrochloride	Smo	Cancer
SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

HY-12848B

SAG hydrochloride	Smo	Cancer
SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG hydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

HY-12288

Ozanimod RPC-1063	LPL Receptor	Inflammation/Immunology
Ozanimod (RPC-1063) is a potent and selective S1P₁ and S1P₅ receptor agonist with EC₅₀s of 410 pM and 11 nM in [³⁵S]-GTPγS binding, respectively.

HY-P1279

[Lys5,MeLeu9,Nle10]-NKA(4-10)
Neurokinin Receptor Inflammation/Immunology

[Lys5,MeLeu9,Nle10]-NKA(4-10) is a highly selective and potent NK₂ receptor agonist, with an IC₅₀ of 6.1 nM.

HY-P1295

Urocortin, human Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I	CRFR	Neurological Disease Endocrinology
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF₂ receptor, with K_is of 0.4, 0.3, and 0.5 nM for hCRF₁, rCRF_2α and mCRF_2β, respectively.

HY-100013A1

(1R,2R)-2-PCCA hydrochloride	Others	Neurological Disease
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC₅₀ of 3 nM in cell-free assay, and 603 nM in cell assay.

HY-14289

Cimetidine SKF-92334	Histamine Receptor	Cancer Endocrinology
Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a K_i of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.

HY-111149

PS372424	CXCR	Inflammation/Immunology
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.

HY-P1540

Angiotensin III, human, mouse	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Angiotensin III, human, mouse is a heptapeptide, acts as an endogenous angiotensin type 2 receptor (AT₂R) agonist, with IC₅₀s of 0.648 nM and 21.1 nM for AT₂R and AT₁R, respectively.

HY-110060

NDT 9513727	Complement System	Inflammation/Immunology
NDT 9513727 is a potent, selective, orally active and competitive inverse agonist of the human C5aR (C5a receptor), with an IC₅₀ of 11.6 nM. NDT 9513727 can be used for the research of human inflammatory diseases.

HY-117071

Dabuzalgron Ro 115-1240	Adrenergic Receptor Apoptosis	Endocrinology Cardiovascular Disease
Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function.

HY-50760

L-692585	GHSR	Endocrinology
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a K_i of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.

HY-108525

Fluorobexarotene	RAR/RXR	Cancer
Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a K_i value of 12 nM and an EC₅₀ value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

HY-P1124

AS2034178 free base	GPR40	Metabolic Disease
AS2034178 free base, a specific and orally active GPR40 agonist, exhibits glucose-dependent insulin secretion enhancement. AS2034178 free base has potential for type 2 diabetes mellitus research.

HY-14848

Naluzotan PRX 00023	5-HT Receptor Potassium Channel	Neurological Disease
Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC₅₀ and K_i of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K⁺ channel blocker, with IC₅₀ of 3800 nM.

HY-103181

N6-Cyclopentyladenosine CPA; UK-80882	Adenosine Receptor	Neurological Disease
N6-Cyclopentyladenosine (CPA) is a selective Adenosine A₁ receptor agonist, with K_i values of 2.3 nM, 790 nM and 43 nM for human A₁, A_2A and A₃ receptors, respectively.

HY-12764