Search Result

Targets Recommended:	Antifolate

Results for "Antifolate Agonists" in MCE Product Catalog:

By Targets:	Antifolate (13) 5-HT Receptor (118) AChE (1) ADC Cytotoxin (2) Adenosine Receptor (28) Adiponectin Receptor (2) Adrenergic Receptor (123) Akt (2) Aldehyde Dehydrogenase (ALDH) (1) Amyloid-β (2) Androgen Receptor (7) Angiotensin Receptor (11) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (7) Apoptosis (42) Aryl Hydrocarbon Receptor (10) ATP Citrate Lyase (1) Autophagy (68) Bacterial (14) Bcl-2 Family (1) Bombesin Receptor (4) Bradykinin Receptor (3) Calcium Channel (9) Cannabinoid Receptor (25) CaSR (2) CCR (2) CDK (1) CGRP Receptor (4) Cholecystokinin Receptor (3) Complement System (7) COMT (1) CRFR (10) CRISPR/Cas9 (1) CXCR (7) Cytochrome P450 (5) DNA/RNA Synthesis (5) Dopamine Receptor (71) Drug Metabolite (11) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) EBI2/GPR183 (2) Endogenous Metabolite (49) Endothelin Receptor (6) Enterovirus (1) ERK (4) Estrogen Receptor/ERR (24) Fatty Acid Synthase (FASN) (1) Ferroptosis (10) Fungal (1) FXR (15) GABA Receptor (37) GHSR (10) Glucagon Receptor (24) Glucocorticoid Receptor (18) GlyT (1) GNRH Receptor (5) GPCR19 (8) GPR109A (3) GPR119 (6) GPR120 (6) GPR139 (1) GPR40 (11) GPR55 (1) GPR84 (2) Guanylate Cyclase (3) HBV (3) HCV (5) HDAC (1) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (22) Histone Methyltransferase (4) HIV (11) HSV (4) IFNAR (4) iGluR (27) IKK (1) Imidazoline Receptor (6) Influenza Virus (6) Insulin Receptor (1) Integrin (4) Interleukin Related (1) JAK (1) Leukotriene Receptor (1) LPL Receptor (14) LXR (13) mAChR (32) MCHR1 (GPR24) (3) MDM-2/p53 (1) Melanocortin Receptor (21) Melatonin Receptor (9) mGluR (33) Mineralocorticoid Receptor (1) Mitophagy (3) Monoamine Oxidase (1) Motilin Receptor (1) nAChR (40) Neurokinin Receptor (13) Neuropeptide Y Receptor (24) Neurotensin Receptor (2) NF-κB (8) NO Synthase (2) Opioid Receptor (71) Orexin Receptor (OX Receptor) (10) Oxytocin Receptor (2) P2X Receptor (2) P2Y Receptor (5) PAK (2) Parasite (8) Phosphatase (3) Phosphodiesterase (PDE) (3) Potassium Channel (7) PPAR (53) Progesterone Receptor (7) Prostaglandin Receptor (18) Protease-Activated Receptor (PAR) (16) RAR/RXR (25) Reactive Oxygen Species (3) RET (1) Reverse Transcriptase (1) ROR (17) SARS-CoV (2) Serotonin Transporter (2) Sigma Receptor (13) Smo (5) Sodium Channel (3) Somatostatin Receptor (4) STAT (2) STING (11) TGF-beta/Smad (1) TGF-β Receptor (1) Thrombin (1) Thrombopoietin Receptor (5) Thyroid Hormone Receptor (9) TNF Receptor (1) Toll-like Receptor (TLR) (26) Trk Receptor (3) TRP Channel (24) TSH Receptor (2) Urotensin Receptor (2) Vasopressin Receptor (11) VD/VDR (3) Virus Protease (3) Wnt (3) β-catenin (3)
By Research Areas:	Cancer (227) Cardiovascular Disease (150) Endocrinology (249) Infection (46) Inflammation/Immunology (230) Metabolic Disease (186) Neurological Disease (576)

By Targets:

Antifolate (13)

5-HT Receptor (118)

AChE (1)

ADC Cytotoxin (2)

Adenosine Receptor (28)

Adiponectin Receptor (2)

Adrenergic Receptor (123)

Akt (2)

Aldehyde Dehydrogenase (ALDH) (1)

Amyloid-β (2)

Androgen Receptor (7)

Angiotensin Receptor (11)

Angiotensin-converting Enzyme (ACE) (1)

Antibiotic (7)

Apoptosis (42)

Aryl Hydrocarbon Receptor (10)

ATP Citrate Lyase (1)

Autophagy (68)

Bacterial (14)

Bcl-2 Family (1)

Bombesin Receptor (4)

Bradykinin Receptor (3)

Calcium Channel (9)

Cannabinoid Receptor (25)

CaSR (2)

CCR (2)

CDK (1)

CGRP Receptor (4)

Cholecystokinin Receptor (3)

Complement System (7)

COMT (1)

CRFR (10)

CRISPR/Cas9 (1)

CXCR (7)

Cytochrome P450 (5)

DNA/RNA Synthesis (5)

Dopamine Receptor (71)

Drug Metabolite (11)

Drug-Linker Conjugates for ADC (1)

E1/E2/E3 Enzyme (1)

EBI2/GPR183 (2)

Endogenous Metabolite (49)

Endothelin Receptor (6)

Enterovirus (1)

ERK (4)

Estrogen Receptor/ERR (24)

Fatty Acid Synthase (FASN) (1)

Ferroptosis (10)

Fungal (1)

FXR (15)

GABA Receptor (37)

GHSR (10)

Glucagon Receptor (24)

Glucocorticoid Receptor (18)

GlyT (1)

GNRH Receptor (5)

GPCR19 (8)

GPR109A (3)

GPR119 (6)

GPR120 (6)

GPR139 (1)

GPR40 (11)

GPR55 (1)

GPR84 (2)

Guanylate Cyclase (3)

HBV (3)

HCV (5)

HDAC (1)

HIF/HIF Prolyl-Hydroxylase (2)

Histamine Receptor (22)

Histone Methyltransferase (4)

HIV (11)

HSV (4)

IFNAR (4)

iGluR (27)

IKK (1)

Imidazoline Receptor (6)

Influenza Virus (6)

Insulin Receptor (1)

Integrin (4)

Interleukin Related (1)

JAK (1)

Leukotriene Receptor (1)

LPL Receptor (14)

LXR (13)

mAChR (32)

MCHR1 (GPR24) (3)

MDM-2/p53 (1)

Melanocortin Receptor (21)

Melatonin Receptor (9)

mGluR (33)

Mineralocorticoid Receptor (1)

Mitophagy (3)

Monoamine Oxidase (1)

Motilin Receptor (1)

nAChR (40)

Neurokinin Receptor (13)

Neuropeptide Y Receptor (24)

Neurotensin Receptor (2)

NF-κB (8)

NO Synthase (2)

Opioid Receptor (71)

Orexin Receptor (OX Receptor) (10)

Oxytocin Receptor (2)

P2X Receptor (2)

P2Y Receptor (5)

PAK (2)

Parasite (8)

Phosphatase (3)

Phosphodiesterase (PDE) (3)

Potassium Channel (7)

PPAR (53)

Progesterone Receptor (7)

Prostaglandin Receptor (18)

Protease-Activated Receptor (PAR) (16)

RAR/RXR (25)

Reactive Oxygen Species (3)

RET (1)

Reverse Transcriptase (1)

ROR (17)

SARS-CoV (2)

Serotonin Transporter (2)

Sigma Receptor (13)

Smo (5)

Sodium Channel (3)

Somatostatin Receptor (4)

STAT (2)

STING (11)

TGF-beta/Smad (1)

TGF-β Receptor (1)

Thrombin (1)

Thrombopoietin Receptor (5)

Thyroid Hormone Receptor (9)

TNF Receptor (1)

Toll-like Receptor (TLR) (26)

Trk Receptor (3)

TRP Channel (24)

TSH Receptor (2)

Urotensin Receptor (2)

Vasopressin Receptor (11)

VD/VDR (3)

Virus Protease (3)

Wnt (3)

β-catenin (3)

By Research Areas:

Cancer (227)

Cardiovascular Disease (150)

Endocrinology (249)

Infection (46)

Inflammation/Immunology (230)

Metabolic Disease (186)

Neurological Disease (576)

1262

Inhibitors & Agonists

Screening Libraries

221

Peptides

122

Natural
Products

Cat. No.	Product Name	Target	Research Areas

HY-19095

TNP-351	Antifolate	Cancer
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.

HY-130569

7-Hydroxymethotrexate	Drug Metabolite	Cancer Inflammation/Immunology
7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.

HY-10446

Pralatrexate	Antifolate Apoptosis	Cancer
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.

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-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-P1334A

DPDPE TFA
Opioid Receptor Neurological Disease

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

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

HY-14521

Lometrexol DDATHF	Antifolate Apoptosis	Cancer
Lometrexol (DDATHF), an antipurine *antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT)* but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

HY-14521B

Lometrexol hydrate DDATHF hydrate	Antifolate Apoptosis	Cancer
Lometrexol hydrate (DDATHF hydrate), an antipurine *antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT)* but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

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-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-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-14523

LY 254155
Antifolate Cancer

LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with K_is of 2.1±0.2 and 1.7±0.1 nM, respectively.

LY 254155	Antifolate	Cancer
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with K_is of 2.1±0.2 and 1.7±0.1 nM, respectively.

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-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-13781

Pemetrexed disodium hemipenta hydrate LY231514 disodium hemipenta hydrate	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed disodium hemipenta hydrate is a novel *antifolate, the K_i* values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

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-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-133624

1,1,3-Tribromoacetone	Others	Cancer
1,1,3-Tribromoacetone is an impurity of methotrexate. Methotrexate, an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.

HY-10820

Pemetrexed LY231514	Antifolate Autophagy	Cancer
Pemetrexed (LY231514) is an *antifolate, the K_i* values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

HY-10820A

Pemetrexed disodium LY231514 disodium	Antifolate Autophagy Apoptosis	Cancer
Pemetrexed disodium (LY231514 disodium) is an antifolate, the K_is of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.

HY-B1833

Afloqualone HQ-495	GABA Receptor	Neurological Disease
Afloqualone 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-101198

Clobenpropit dihydrobromide	Histamine Receptor	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-133887

Methotrexate α-tert-butyl ester	Antifolate DNA/RNA Synthesis	Cancer
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.

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-107981

LSN 3213128	Antifolate	Cancer
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitory activity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC₅₀ of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity.

HY-13673

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

HY-129441

Metoprine BW 197U	Histone Methyltransferase Antifolate	Cancer Neurological Disease
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT. Metoprine is an *antifolate* and antitumor agent.

HY-13673A

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

HY-14519

Methotrexate Amethopterin; CL14377; WR19039	Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis	Cancer Inflammation/Immunology
Methotrexate (Amethopterin), an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).

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-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-14519A

Methotrexate disodium Amethopterin disodium; CL14377 disodium; WR19039 disodium	Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis	Cancer Inflammation/Immunology
Methotrexate (Amethopterin) disodium, an antimetabolite and *antifolate* agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).

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-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-13581A

Buserelin Acetate
GNRH Receptor Cancer Endocrinology

Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).
HY-14234

Glucocorticoid receptor agonist
Glucocorticoid Receptor Metabolic Disease Endocrinology

Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.

Buserelin Acetate	GNRH Receptor	Cancer Endocrinology
Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).

Glucocorticoid receptor agonist	Glucocorticoid Receptor	Metabolic Disease Endocrinology
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist.

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-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-133777

Ciprofibrate impurity A
PPAR Cancer

Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist.
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.

Ciprofibrate impurity A	PPAR	Cancer
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate is a PPARα agonist.

Clenproperol	Adrenergic Receptor	Endocrinology
Clenproperol is a β2-adrenergic agonist.

NSC12404	LPL Receptor	Others
NSC12404 is a weak and specific LPA₂ receptor agonist.

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-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-13239

LY2979165
mGluR Neurological Disease

LY2979165 is the alanine prodrug of 2812223, a selective and potent orthosteric mGlu2 receptor 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-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-P0078

TRAP-6 PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6	Protease-Activated Receptor (PAR)	Inflammation/Immunology
TRAP-6 (PAR-1 agonist peptide) is a protease-activated receptor 1 (PAR1) agonist.

HY-111353

GPR120 Agonist 2
GPR120 Metabolic Disease

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

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-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-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-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-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-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-B1532

Anabasine
(S)-Anabasine
nAChR Neurological Disease

Anabasine is a nicotinic receptor agonist.
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-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-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-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-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-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-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-107743

Naloxone benzoylhydrazone NalBzoH	Opioid Receptor	Neurological Disease
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect.

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-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-B0556A

Tetrahydrozoline hydrochloride Tetryzoline hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Tetrahydrozoline hydrochloride (Tetryzoline hydrochloride) is a α-adrenoceptor agonist.

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-B0664

Ciprofibrate
Win35833
PPAR Cancer

Ciprofibrate is a peroxisome proliferator-activated 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-B0976

Fenoterol Th-1165; Phenoterol	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Fenoterol (Th-1165) is a β2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.

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) and acts as PAR₄-specific agonist.

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-B0976A

Fenoterol hydrobromide Fenoterol bromide; Th-1165a; Phenoterol hydrobromide	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Fenoterol hydrobromide (Fenoterol bromide) is a β2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.

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-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-U00315

Gidazepam
Gidasepam; Hidazepam; Hydazepam
GABA Receptor Neurological Disease

Gidazepam is an agonist of GABA receptor channels (GABA RCs).
HY-U00205

Dopexamine hydrochloride
FPL60278AR
Adrenergic Receptor Cardiovascular Disease Endocrinology

Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
HY-13720A

Pergolide mesylate
Pergolide methanesulfonate; LY127809
Dopamine Receptor Neurological Disease

Pergolide mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.
HY-50108

GW 4064
FXR Autophagy Metabolic Disease Cancer

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.
HY-10473

Eprotirome
KB2115
Thyroid Hormone Receptor Endocrinology Metabolic Disease

Eprotirome is a liver-selective thyroid hormone receptor agonist.
HY-U00123

Guanoxabenz
Hydroxyguanabenz
Adrenergic Receptor Cardiovascular Disease Endocrinology

Guanoxabenz is an α2 adrenergic receptor 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-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-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-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-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-14803

Tasimelteon
BMS-214778; VEC-162
Melatonin Receptor Neurological Disease Endocrinology

Tasimelteon is a melatonin MT1 and MT2 receptor agonist.
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-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-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-19961

KIN1408
HCV Infection

KIN1408 is an antiviral small molecule compound, as agonists of the RLR pathway.
HY-15564

AR 231453
GPR119 Metabolic Disease

AR 231453 is a potent, selective and orally available GPR119 agonist.
HY-103173

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

5'-N-Ethylcarboxamidoadenosine (NECA) is a nonselective adenosine receptor agonist.
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-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-13571A

Beclometasone dipropionate	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone.

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-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-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 specifically activates the DREADD receptor hM3Dq. 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 specifically activates the DREADD receptor hM3Dq. 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-19434A

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

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-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-15451

MDA 19
Cannabinoid Receptor Neurological Disease

MDA 19 is a selective human CB2 receptor agonist with Ki of 43.3 nM.
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-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-50844

Ibutamoren Mesylate
MK-677; MK-0677
GHSR Endocrinology

Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

HY-B0180A

Imiquimod hydrochloride R 837 hydrochloride	Toll-like Receptor (TLR) Autophagy HSV	Inflammation/Immunology
Imiquimod hydrochloride is an immune response modifier that acts as a toll-like receptor 7agonist.

HY-19838

JNJ-63533054
GPR139 Neurological Disease

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.
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-B0180B

Imiquimod maleate
R 837 maleate
Toll-like Receptor (TLR) Autophagy Inflammation/Immunology

Imiquimod maleate is an immune response modifier that acts as a toll-like receptor 7agonist.
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-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 neuropeptide Y receptor agonist.

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-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-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-15108

Purmorphamine
Shh Signaling Antagonist VI
Smo Autophagy Neurological Disease Cancer

Purmorphamine (Shh Signaling Antagonist VI) is a smoothened receptor agonist with an EC₅₀ of 1 μM.
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-14734

Anamorelin
RC-1291; ONO-7643
GHSR Cancer Endocrinology

Anamorelin is a novel ghrelin receptor agonist with EC₅₀ value of 0.74 nM in the FLIPR assay.
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-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-14734A

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

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-11062

Icilin
AG-3-5
TRP Channel Cancer

Icilin(AG 3-5) is a synthetic super-agonist of TRPM8 ion channel.
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-14773

Mirabegron
YM178
Adrenergic Receptor Neurological Disease Endocrinology

Mirabegron is a selective β₃-adrenoceptor agonist with EC₅₀ of 22.4 nM.
HY-12066

GSK1292263
GPR119 Metabolic Disease Inflammation/Immunology

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

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-B0180

Imiquimod
R 837
Toll-like Receptor (TLR) Autophagy HSV Inflammation/Immunology Cancer

Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.
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-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-B0664S

Ciprofibrate D6
PPAR Cancer

Ciprofibrate D6 is deuterium labeled Ciprofibrate, which is a peroxisome proliferator-activated receptor agonist.

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-A0083

Methacholine chloride Acetyl-β-methylcholine chloride	mAChR	Others
Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.

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-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-A0168

Regadenoson CVT-3146	Adenosine Receptor	Cardiovascular Disease Cancer
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing.

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-B0406A

Bethanechol chloride Carbamyl-β-methylcholine chloride	mAChR	Metabolic Disease
Bethanechol Chloride (Carbamyl-β-methylcholine chloride) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.

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-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-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-14899

Taprenepag
CP-544326
Prostaglandin Receptor Endocrinology

Taprenepag (CP-544326) is a potent and selective prostaglandin E2 receptor agonist with an EC₅₀ of 2.8 nM.
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-14933

Prinaberel
ERB-041
Estrogen Receptor/ERR Apoptosis Cancer

Prinaberel(ERB-041) is a potent and selective ERbeta agonist; being >200-fold selective for ERbeta.
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-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-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-14417

VU0155041	mGluR	Neurological Disease
VU0155041 is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC₅₀s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site.

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-14153A

Tegaserod maleate SDZ-HTF-919; HTF-919	5-HT Receptor	Neurological Disease
Tegaserod maleate is a partial agonist of the 5-HT4 receptor; stimulates the peristaltic reflex and accelerates gastrointestinal transit.

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-15565

APD668
GPR119 Metabolic Disease

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.

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-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-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-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-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 beta-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.

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-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-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-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

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-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-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-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-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-101586

Alvameline
Lu 25-109
mAChR Neurological Disease

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

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-B0100

Etomidate R 16659	GABA Receptor	Neurological Disease
Etomidate(R-16659) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.

HY-17034A

Dexmedetomidine hydrochloride (+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride	Adrenergic Receptor Autophagy	Neurological Disease Endocrinology Cancer
Dexmedetomidine Hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.

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-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. IC50 Value:

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-17573

Carbetocin	Oxytocin Receptor	Endocrinology
Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.

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-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-10448

Capsaicin (E)-Capsaicin	TRP Channel Autophagy	Cancer
Capsaicin ((E)-Capsaicin) is a mixture of Capsaicin and Dihydrocapsaicin. Capsaici is a TRPV1 agonist with an EC₅₀ of 0.29 μM in HEK293 cells.

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-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-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-19775

GNE-6468
ROR Inflammation/Immunology

GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC₅₀ value of 13 nM for HEK-293 cell.

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-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-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-101037

Sarcosine N-Methylglycine; Sarcosin	Endogenous Metabolite GlyT	Cancer
Sarcosine is a glycine transporter type 1 (GlyT) inhibitor and an N-methyl-D-aspartate (NMDA) receptor co-agonist at the glycine binding site.

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-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-B0447A

L-Epinephrine Bitartrate (-)-Epinephrine (+)-bitartrate salt; L-Adrenaline (+)-bitartrate salt	Adrenergic Receptor	Neurological Disease Endocrinology
L-Epinephrine bitartrate is an α-adrenergic and β-adrenergic receptor agonist. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands.

HY-B0100A

Etomidate hydrochloride R16659 hydrochloride	GABA Receptor	Neurological Disease
Etomidate Hcl(R16659 Hcl) is a GABAA receptors agonist, which is a short acting intravenous anaesthetic agent used for the induction of general anaesthesia.

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-50919

Paricalcitol	VD/VDR	Metabolic Disease
Paricalcitol 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-14564A

GTS-21 dihydrochloride DMXB-A; DMBX-anabaseine	nAChR	Inflammation/Immunology
GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.

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-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-B0225

L-(-)-α-Methyldopa MK-351; Methyldopa	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Methyldopa is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.

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-100256

Trifarotene CD5789	RAR/RXR Autophagy	Inflammation/Immunology
Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with K_d^app of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.

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-18978

GR79236	Adenosine Receptor	Inflammation/Immunology
GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.

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-14782

Adoprazine SLV313	5-HT Receptor Dopamine Receptor	Neurological Disease
Adoprazine, a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

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-B1473

Serotonin hydrochloride 5-Hydroxytryptamine hydrochloride; 5-HT hydrochloride	5-HT Receptor COMT Endogenous Metabolite	Neurological Disease
Serotonin 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-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-B0556

Tetrahydrozoline Tetryzoline	Adrenergic Receptor	Cardiovascular Disease
Tetrahydrozoline is a potent α-adrenergic agonist and causes vasoconstriction. Tetrahydrozoline is used for the relief of conjunctival, ophthalmic and nasal congestion in vivo.

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-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-14728

Aleglitazar
R1439; RO0728804
PPAR Metabolic Disease

Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.
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-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-B0225B

L-(-)-α-Methyldopa (hydrate) MK-351 hydrate; Methyldopa hydrate	Adrenergic Receptor	Cardiovascular Disease Endocrinology
L-(-)-α-Methyldopa hydrate is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.

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-B0225A

L-(-)-α-Methyldopa hydrochloride MK-351 hydrochloride; Methyldopa hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
L-(-)-α-Methyldopa hydrochloride is an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive drug used as a sympatholytic or antihypertensive.

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-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-13967B

AMG 837 calcium hydrate	GPR40	Metabolic Disease
AMG 837 calcium hydrate is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.

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-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-B0447

DL-Epinephrine (±)-Epinephrine; DL-Adrenaline; (±)-Adrenaline	Adrenergic Receptor	Neurological Disease Endocrinology
DL-Epinephrine is the racemate of epinephrine. L-Epinephrine is a hormone secreted by the medulla of the adrenal glands. L-Epinephrine is an α-adrenergic and β-adrenergic receptor agonist.

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-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-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-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-125824

PF-06882961
Glucagon Receptor Metabolic Disease

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R).

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-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-107384

Asimadoline EMD-61753	Opioid Receptor	Inflammation/Immunology
Asimadoline is a potent κ opioid receptor agonist with IC₅₀s of 5.6 and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.

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-14302

Salmeterol
GR33343X
Adrenergic Receptor Endocrinology

Salmeterol (GR33343X) is a long-acting beta2-adrenergic receptor (beta 2AR) agonist used clinically to treat asthma.

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-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-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-15697

TUG-770
GPR40 Metabolic Disease

TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.

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-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	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-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-P2541

GIP (1-30) amide, porcine	Insulin Receptor	Metabolic Disease
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with high affinity equal to native GIP(1-42).

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-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-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-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-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 pentapeptides 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-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-19752A

VU0357017 hydrochloride CID-25010775	mAChR	Neurological Disease
VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).

HY-100490

Rilmenidine	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	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-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-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-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-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-14554

LY2140023	mGluR	Neurological Disease
LY2140023 is an orally active prodrug of LY404039. LY404039 is a selective metabotropic glutamate 2/3 receptor agonist. LY2140023 has the potential for schizophrenia.

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-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-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-17043

Loratadine Loratidine; SCH 29851	Histamine Receptor Influenza Virus	Infection Endocrinology Inflammation/Immunology
Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity.

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-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-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.

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-100490A

Rilmenidine hemifumarate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy
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-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-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-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-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-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-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-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-15701

Leukadherin-1
Complement System Integrin Inflammation/Immunology

Leukadherin-1 is a specific agonist of complement receptor 3 (CR3) and the leukocyte surface αMβ2 integrin CD11b/CD18.

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-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-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
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-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-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-12641

Pyrantel tartrate	Parasite Antibiotic	Infection
Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.

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-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-15483

DY131 GSK 9089	Estrogen Receptor/ERR	Cancer
DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.

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-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-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-17453

Salmeterol xinafoate GR 33343X xinafoate	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Salmeterol xinafoate is a long-acting beta-2 adrenergic receptor (β₂AR) agonist, with K_i of 1.5 nM for WT β₂AR, and used for asthma treatment.

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-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-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
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-19870

Setmelanotide RM-493; BIM-22493; IRC-022493	Melanocortin Receptor	Metabolic Disease Endocrinology
Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC₅₀s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

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-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-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-19870B

Setmelanotide acetate RM-493 acetate; BIM-22493 acetate; IRC-022493 acetate	Melanocortin Receptor	Endocrinology Metabolic Disease
Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC₅₀s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

HY-W014928

(+)-Anabasine hydrochloride	nAChR	Neurological Disease
(+)-Anabasine hydrochloride is an alkaloid found in Nicotiana, and it is a potent nAChR agonist. (+)-Anabasine hydrochloride induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs with an EC₅₀ of 0.7 µM.

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-16673

PSN632408	GPR119	Metabolic Disease
PSN632408 is an optimized agonist of GPR119 receptors that shows similar potency to OEA at both recombinant mouse and human GPR119 receptors, exhibiting EC50 values of 5.6 and 7.9 uM, respectively.

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	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-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-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-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-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-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-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-135119

Salmeterol-D3	Adrenergic Receptor
Salmeterol-D3 is the deuterium labeled Salmeterol (HY-14302). Salmeterol is a long-acting beta2-adrenergic receptor agonist that is used for the study of asthma and chronic obstructive pulmonary disease (COPD).

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-100781A

L-APB L-AP 4	mGluR	Neurological Disease
L-APB is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively.

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-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-117071

Dabuzalgron Ro 115-1240	Adrenergic Receptor	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-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

6-OAU GTPL5846	GPR84	Inflammation/Immunology
6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay.

HY-100176

PF-4878691 3M-852A	Toll-like Receptor (TLR)	Infection Inflammation/Immunology
PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities.

HY-19522A

Seladelpar sodium salt MBX-8025 sodium salt; RWJ-800025 sodium salt	PPAR	Metabolic Disease
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC₅₀ of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

HY-P1537

Pancreatic Polypeptide, bovine	Neuropeptide Y Receptor	Metabolic Disease Endocrinology
Pancreatic Polypeptide, bovine, a 36-amino acid, straight chain polypeptide derived primarily from the pancreas, inhibits secretin- and cholecystokinin-stimulated pancreatic secretion; Pancreatic Polypeptide, bovine acts as an agonist of NPY receptor, with high affinity at NPYR4.

HY-P1418A

DPC-AJ1951 TFA	Thyroid Hormone Receptor	Endocrinology
DPC-AJ1951 TFA, 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-P7060

NT 13 TPPT	iGluR	Neurological Disease
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.

HY-P1132

Galanin (1-29)(rat, mouse)	Neuropeptide Y Receptor	Neurological Disease
Galanin (1-29)(rat, mouse) is a non-selective galanin receptor agonist, with K_is of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively. Anticonvulsant effect.

HY-112612A

RTI-13951-33 hydrochloride	Others	Neurological Disease
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC₅₀ of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.

HY-122190

TAK-071	mAChR	Neurological Disease
TAK-071 is a novel, potent and highly selective muscarinic acetylcholine receptor 1 (M1R) positive allosteric modulator. EC₅₀ of TAK-071 M1R agonist activities is 520 nM.

HY-112706

PF-06747711	ROR	Inflammation/Immunology
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC₅₀ of 4.1 nM. Anti-skin inflammatory activity.

HY-B1675

Levalbuterol (R)-Albuterol; (R)-Salbutamol; Levosalbutamol	Adrenergic Receptor	Inflammation/Immunology
Levalbuterol ((R)-Albuterol; (R)-Salbutamol) is a short-acting β2-adrenergic receptor agonist and the active (R)-enantiomer of Salbutamol. Levalbuterol is a more potent bronchodilator than Salbutamol and has the potential for the treatment of COPD.

HY-B0471

Phenylephrine hydrochloride (R)-(-)-Phenylephrine hydrochloride; L-Phenylephrine hydrochloride	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
(R)-(-)-Phenylephrine hydrochloride is a selective α₁-adrenoceptor agonist with pK_is of 5.86, 4.87 and 4.70 for α_1D, α_1B and α_1A receptors respectively.

HY-113151

18-Oxocortisol	Mineralocorticoid Receptor Endogenous Metabolite	Cardiovascular Disease
18-Oxocortisol is a derivative of cortisol that is produced by aldosterone synthase (CYP11B2). 18-Oxocortisol is a naturally occurring mineralocorticoid agonist. 18-Oxocortisol is a biomarker in adrenal vein sampling.

HY-100807

Quinolinic acid	Endogenous Metabolite iGluR	Inflammation/Immunology Neurological Disease
Quinolinic acid is an endogenous N-methyl-D-aspartate (NMDA) receptor agonist synthesized from L-tryptophan via the kynurenine pathway and thereby has the potential of mediating N-methyl-D-aspartate neuronal damage and dysfunction.

HY-B1264

Celiprolol hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.

HY-A0261

Pentagastrin ICI-50123	Cholecystokinin Receptor	Cancer Endocrinology
Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCK_B) receptor with an IC₅₀ of 11 nM. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury.

HY-P1279A

[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA	Neurokinin Receptor	Neurological Disease
[Lys5,MeLeu9,Nle10]-NKA(4-10) TFA is a highly selective and potent NK₂ receptor agonist, with an IC₅₀ of 6.1 nM.

HY-124401

BT-13	RET	Neurological Disease
BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.

HY-N0301

Thiocolchicoside	GABA Receptor	Inflammation/Immunology Neurological Disease
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GAB_AA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.

HY-126057S

(R)-Praziquantel D11	Parasite 5-HT Receptor	Infection
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.

HY-100300

AGN 192836	Adrenergic Receptor	Cardiovascular Disease Endocrinology
AGN 192836 is a potent and selective α2 adrenergic agonist with EC₅₀s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.

HY-B0982

Pindolol LB-46	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).

HY-100839

(RS)-(Tetrazol-5-yl)glycine D,L-(tetrazol-5-yl)glycine; LY 285265	iGluR	Neurological Disease
(RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. (RS)-(Tetrazol-5-yl)glycine has EC₅₀s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice.

HY-13693

Mometasone furoate Sch32088	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
Mometasone furoate (Sch32088) is a glucocorticoid receptor agonist with anti-inflammatory and anti-allergic activity. Mometasone furoate acts as a corticosteroid agent and used for topical applications in chronic skin eczema and airway inflammation management of asthma in vivo

HY-15682

TTNPB Ro 13-7410; Arotinoid acid; AGN191183	RAR/RXR Autophagy Apoptosis	Cancer
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC₅₀s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.

HY-18779

PF-4840154	TRP Channel	Inflammation/Immunology
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC₅₀s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.

HY-B1276

Metaproterenol hemisulfate Orciprenaline hemisulfate	Adrenergic Receptor	Inflammation/Immunology Cardiovascular Disease Endocrinology
Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC₅₀ of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.

HY-12597

Quisqualic acid L-Quisqualic acid	iGluR mGluR	Neurological Disease
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC₅₀ of 45 nM and a K_i of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.

HY-N7687

Caulophyllogenin	PPAR	Metabolic Disease Inflammation/Immunology
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC₅₀ of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.

HY-P1132A

Galanin (1-29)(rat, mouse) TFA	Neuropeptide Y Receptor	Neurological Disease
Galanin (1-29)(rat, mouse) TFA is a non-selective galanin receptor agonist, with K_is of 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3, respectively. Anticonvulsant effect.

HY-P1296

Urocortin, rat Urocortin (Rattus norvegicus); Rat urocortin	CRFR	Neurological Disease Endocrinology
Urocortin, rat (Urocortin (Rattus norvegicus)) is a neuropeptide and a potent endogenous CRFR agonist with K_is of 13 nM, 1.5 nM, and 0.97 nM for human CRF₁, rat CRF_2α and mouse CRF_2β, respectively.

HY-16687A

Eltoprazine hydrochloride DU 28853 hydrochloride	5-HT Receptor	Neurological Disease
Eltoprazine hydrochloride (DU 28853 hydrochloride) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.

HY-117516

SR10067	Others	Neurological Disease
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC₅₀ values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.

HY-17609

Difelikefalin CR-845; FE-202845	Opioid Receptor	Neurological Disease
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.

HY-P1502

β-Endorphin, human	Opioid Receptor	Neurological Disease
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.

HY-10912

Fexaramine	FXR Autophagy	Others
Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.

HY-13580

Budesonide	Glucocorticoid Receptor	Cancer Inflammation/Immunology
Budesonide, an inhaled glucocortical steroid, is an orally active glucocorticoid receptor agonist. Budesonide decreases the size of lung tumors, reverses DNA hypomethylation and modulates mRNA expression of genes. Budesonide is an anti-inflammatory agent used for asthma.

HY-123268

Ro 363	Adrenergic Receptor	Cardiovascular Disease
Ro 363 is a potent and highly selective β1-adrenoceptor agonist. RO 363 is an effective inotropic stimulant, and is a cardiovascular modulator that reduces diastolic blood pressure and pronounces increases in myocardial contractility.

HY-W013788

2-Palmitoylglycerol 2-Palm-Gl	Cannabinoid Receptor	Neurological Disease
2-Palmitoylglycerol (2-Palm-Gl), an congener of 2-arachidonoylglycerol (2-AG), is a modest cannabinoid receptor CB1 agonist. 2-Palmitoylglycerol also may be an endogenous ligand for GPR119.

HY-N0285

Imperatorin Ammidin	AChE TRP Channel	Neurological Disease
Imperatorin is an effective of NO synthesis inhibitor (IC₅₀=9.2 μmol), which also is a BChE inhibitor (IC₅₀=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC₅₀ of 12.6±3.2 μM.

HY-102091

(2R,4R)-APDC	mGluR	Neurological Disease
(2R,4R)-APDC is a selective group II metabotropic glutamate receptors (mGluRs) agonist. (2R,4R)-APDC has anticonvulsant and neuroprotective effects.

HY-116506

Bigelovin	RAR/RXR Reactive Oxygen Species Apoptosis Autophagy	Cancer
Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

HY-111455

LP-211	5-HT Receptor	Neurological Disease
LP-211 is a selective and blood−brain barrier penetrant 5-HT₇ receptor agonist, with a K_i of 0.58 nM, with high selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM).

HY-N2037

Higenamine Norcoclaurine	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine (Norcoclaurine) has anti-apoptotic effects.

HY-15293B

JTV-519 hemifumarate K201 hemifumarate	Calcium Channel	Cardiovascular Disease
JTV-519 hemifumarate (K201 hemifumarate) is a Ca²⁺-dependent blocker of sarcoplasmic reticulum Ca²⁺-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.

HY-P1338

PL-017	Opioid Receptor	Neurological Disease
PL-017 is a potent and selective μ opioid receptor agonist with an IC₅₀ of 5.5 nM for ¹²⁵I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats.

HY-B0030

D-Cycloserine	iGluR Bacterial Antibiotic	Infection Neurological Disease
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.

HY-13225A

Rivanicline RJR-2403; (E)-Metanicotine	nAChR	Neurological Disease
Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (K_i=26 nM); > 1,000 fold selectivity than α7 receptors(K_i= 36000 nM).

HY-16687

Eltoprazine DU 28853	5-HT Receptor	Neurological Disease
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.

HY-10061

Lesogaberan AZD-3355	GABA Receptor	Metabolic Disease
Lesogaberan (AZD-3355) is a potent and selective GABA_B receptor agonist with an EC₅₀ of 8.6 nM for human recombinant GABA_B receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABA_B and GABA_A receptors, respectively.

HY-13928

GW0742 GW610742	PPAR	Metabolic Disease Inflammation/Immunology Cardiovascular Disease Cancer
GW0742 is a potent PPARβ and PPARδ agonist, with an IC₅₀ of 1 nM for human PPARδ in binding assay, and EC₅₀s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

HY-103244

CITCO	Apoptosis	Cancer
CITCO, an imidazothiazole derivative, is a selective Constitutive androstane receptor (CAR) agonist. CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC₅₀ of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors.

HY-B0020

Tropisetron Hydrochloride SDZ-ICS-930	5-HT Receptor	Neurological Disease
Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

HY-106993

Cipralisant GT-2331	Histamine Receptor	Neurological Disease Endocrinology
Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pK_i of 9.9 for histamine H3 receptor and a K_i of 0.47 nM for rat histamine H3 receptor; Cipralisant has the potential for attention-deficit hyperactivity disorder treatment.

HY-N2037A

Higenamine hydrochloride Norcoclaurine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology Cancer
Higenamine hydrochloride (Norcoclaurine hydrochloride), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine hydrochloride (Norcoclaurine hydrochloride) has anti-apoptotic effects.

HY-105285

Piromelatine Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

HY-12560A

PNU-282987	nAChR	Neurological Disease
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

HY-17606

Cenerimod ACT-334441	LPL Receptor	Inflammation/Immunology
Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC₅₀ of 2.7 nM.

HY-109083

Cilofexor GS-9674	FXR Autophagy	Inflammation/Immunology
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC₅₀ of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

HY-107495

Betahistine EP Impurity C NSC19005	Histamine Receptor	Inflammation/Immunology
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA).

HY-119243

LY2794193
mGluR Neurological Disease

LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 K_i=0.927 nM，EC₅₀=0.47 nM; hmGlu2 K_i=412 nM，EC₅₀=47.5 nM).

HY-103243

TCPOBOP	Bcl-2 Family	Cancer
TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.

HY-108523

LG100754 UVI 2112	RAR/RXR	Metabolic Disease
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.

HY-129658

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

HY-P0049

Argipressin Vasopressin; Arg8-vasopressin; AVP	Vasopressin Receptor	Neurological Disease
Argipressin binds to the V1, V2, V3-vascular arginine vasopressin receptor, with a K_d value of 1.31 nM in A7r5 rat aortic smooth muscle cells for V1. Argipressin is a selective V2 agonist.

HY-P1294

α-Helical CRF(9-41)	CRFR	Neurological Disease
α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with K_B of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC₅₀ of 140 nM.

HY-111547

M1001	HIF/HIF Prolyl-Hydroxylase	Cancer
M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a K_d of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex.

HY-P1252

Parathyroid Hormone (1-34), bovine	Thyroid Hormone Receptor	Metabolic Disease
Parathyroid Hormone (1-34), bovine is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.

HY-110000

(+)-PD 128907 hydrochloride	Dopamine Receptor	Neurological Disease
(+)-PD 128907 hydrochloride is a selective dopamine D₂/D₃ receptor agonist, with K_is of 1.7, 0.84 nM for human and rat D₃ receptors, 179, 770 n M for human and rat D₃ receptors, respectively.

HY-108699

TM-N1324	GHSR	Neurological Disease Endocrinology
TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC₅₀s of 9 nM/5 nM in the presence of Zn²⁺, and 280 nM/180 nM in the absence of Zn²⁺ for human/murine GPR39.

HY-101310

SYM 2081	iGluR	Neurological Disease
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [³H]-kainate binding with an IC₅₀ of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.

HY-15128

9-cis-Retinoic acid ALRT1057	RAR/RXR Apoptosis	Cancer Inflammation/Immunology Neurological Disease
9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

HY-14442

ML 10302 hydrochloride	5-HT Receptor	Metabolic Disease
ML 10302 hydrochloride is a potent and selective 5-HT₄ receptor agonist, with an EC₅₀ of 4 nM。ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT₃ receptor in binding assay.

HY-19360

Sulprostone SHB 286; CP-34089; ZK-57671	Prostaglandin Receptor	Inflammation/Immunology Cardiovascular Disease
Sulprostone (SHB 286), a prostaglandin E2 (PGE2) analogue, is a potent and selective EP3 receptor agonist. Sulprostone has potential antiulcer and nonsteroidal abortifacient effects used for the research of pregnancy termination and hemorrhages during delivery.

HY-P1298

Sauvagine	CRFR	Endocrinology Neurological Disease Cardiovascular Disease
Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.

HY-12720A

Apraclonidine hydrochloride ALO 2145	Others	Neurological Disease
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid.

HY-P1338A

PL-017 TFA	Opioid Receptor	Neurological Disease
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC₅₀ of 5.5 nM for ¹²⁵I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.

HY-A0095S

Flibanserin D4 BIMT-17 D4; BIMT-17BS D4	5-HT Receptor	Neurological Disease
Flibanserin D4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (K_i=1 nM) and an antagonist of 5-HT2A (49 nM).

HY-12585

AM-4668	GPR40	Metabolic Disease
AM-4668 is a GPR40 agonist for type 2 diabetes. EC₅₀s of 3.6 nM and 36 nM for GPR40 in A9 cells (GPR40 IP3 assay) and CHO cells (GPR40 aequorin assay), respectively.

HY-12365

Namodenoson CF-102; 2-Cl-IB-MECA	Adenosine Receptor	Cancer
Namodenoson (CF-102) is a selective A3 adenosine receptor (A3AR) agonist (K_i=0.33 nM). Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.

HY-P1252A

Parathyroid Hormone (1-34), bovine TFA	Thyroid Hormone Receptor	Metabolic Disease
Parathyroid Hormone (1-34), bovine TFA is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.

HY-117407

ALLO-2	Smo	Cancer
ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC₅₀ of 6 nM.

HY-15293A

JTV-519 free base K201 free base	Calcium Channel	Cardiovascular Disease
JTV-519 free base (K201 free base) is a Ca²⁺-dependent blocker of sarcoplasmic reticulum Ca²⁺-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties.

HY-110120

DSR-6434	Toll-like Receptor (TLR)	Cancer
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC₅₀s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.

HY-19383

Ertiprotafib PTP 112	Phosphatase IKK PPAR	Metabolic Disease
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC₅₀ of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC₅₀ of ~1 μM for PPARα/PPARβ.

HY-P1249

Neuropeptide SF(mouse,rat)	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-131265

Mesalamine impurity P	PPAR PAK NF-κB	Cancer Inflammation/Immunology
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

HY-136238

PM226	Cannabinoid Receptor	Neurological Disease
PM226 is a selective cannabinoid CB2R agonist (K_i (CB2R)=13 nM; EC₅₀ (CB2R)=39 nM; K_i (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.

HY-13665

Leuprolide Acetate Leuprorelin acetate	GNRH Receptor	Endocrinology Cancer
Leuprolide Acetate (Leuprorelin acetate) is an analogue of gonadotrophin-releasing hormone (GnRH), acts as a GnRH receptor agonist. Leuprolide Acetate can be used for the research of prostate cancer, endometriosis, uterine fibroids, central precocious puberty, multiple sclerosis. Leuprolide Acetate improves experimental autoimmune encephalomyelitis in rat model.

HY-B0072

Tropisetron SDZ-ICS-930 free base	5-HT Receptor nAChR	Neurological Disease
Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

HY-129105

Clomethiazole	GABA Receptor Cytochrome P450	Neurological Disease
Chlormethiazole is an potent and orally active *GABA_A* agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.

HY-P1294A

α-Helical CRF(9-41) TFA	CRFR	Neurological Disease
α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with K_B of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC₅₀ of 140 nM.

HY-12498

GV-58	Calcium Channel	Neurological Disease
GV-58 is a potent, selective N- and P/Q-type Ca2+ channels agonist with EC50 of 7.21/8.81 uM for N-type/P-Q-type Ca2+ channel; 20-fold less potent CDK inhibitor activity.

HY-133024

Flumexadol	5-HT Receptor	Neurological Disease
Flumexadol is an orally active non-narcotic analgesic. Flumexadol is a selective and affinity 5-HT_2C receptor agonist with a K_i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT_2A receptor.

HY-121653

Flesinoxan	5-HT Receptor	Neurological Disease
Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC₅₀ value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.

HY-P1319

Nociceptin(1-7)	Opioid Receptor	Inflammation/Immunology
Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.

HY-18282

AZ876
LXR Cancer

AZ876 is a potent and high-affinity LXR agonist. AZ876 displays 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.

HY-103551A

LY 541850	mGluR	Neurological Disease
LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells. LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC₅₀ values of 0.161 μM and 0.038 μM, respectively.

HY-15296

Cabergoline FCE-21336	Dopamine Receptor Autophagy	Endocrinology
Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and 5-HT_2B receptors (K_i=0.7, 1.5, and 1.2, respectively).

HY-15778A

AVE 0991 sodium salt	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [¹²⁵I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC₅₀ of 21 nM.

HY-108015

RO5263397	Others	Neurological Disease
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC₅₀s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.

HY-136657

SC-43	Phosphatase STAT Apoptosis	Cancer
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

HY-100488

Bay 59-3074	Cannabinoid Receptor	Cancer
Bay 59-3074 is a selective cannabinoid CB₁/CB₂ receptor partial agonist with K_i values of 48.3 and 45.5 nM at human CB₁ and CB₂ receptors, respectively. Bay 59-3074 has analgesic properties.

HY-110318

VUF11207 fumarate	CXCR	Cancer
VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pK_i of 8.1) ligand that induces recruitment of β-arrestin2 (pEC₅₀ of 8.8) and subsequent internalization (pEC₅₀ of 7.9) of CXCR7.

HY-12023

GTx-007 S-4	Androgen Receptor	Cancer
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with K_i of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity.

HY-15701B

ADH-503 (Z)-Leukadherin-1 choline	Complement System	Cancer
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

HY-14903

Ulimorelin TZP-101	GHSR Adrenergic Receptor	Metabolic Disease
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC₅₀ of 29 nM and a K_i of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.

HY-P1214

γ1-MSH	Melanocortin Receptor	Cardiovascular Disease
γ1-MSH is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH displays ~40-fold selectivity over MC4 (K_i=1318 nM).

HY-P1298A

Sauvagine TFA	CRFR	Endocrinology Neurological Disease Cardiovascular Disease
Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.

HY-P1341

OXA(17-33)	Orexin Receptor (OX Receptor)	Neurological Disease
OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC₅₀=8.29 nM) over OX2 (187 nM).

HY-100689

Propyl pyrazole triol PPT	Estrogen Receptor/ERR	Cancer
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

HY-P1249A

Neuropeptide SF(mouse,rat) TFA	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide SF (mouse,rat) TFA is a potent neuropeptide FF receptor agonist with K_i values are 48.4 nM and 12.1 nM for NPFF1 and NPFF2, respectively. Neuropeptide SF TFA increases the amplitude of the sustained current of heterologously expressed acid sensing ion channel 3 (ASIC3) .

HY-105296

Blarcamesine AVex-73; AE-37	Sigma Receptor mAChR
Blarcamesine (AVex-73;AE-37) is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome.

HY-16995

Pirinixic acid Wy-14643	PPAR	Metabolic Disease Inflammation/Immunology
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC₅₀s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

HY-109035

Inarigivir soproxil SB9200	HCV	Infection
Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC₅₀s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.

HY-15780

Brexpiprazole OPC-34712	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole (OPC-34712), an atypical antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM.

HY-13221

BRL 54443	5-HT Receptor	Cardiovascular Disease
BRL 54443 is a potent 5-HT_1E/1F receptor agonist (K_i values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.

HY-N7032

Uridine 5′-diphosphoglucose disodium salt UDP-D-Glucose disodium salt	Endogenous Metabolite P2Y Receptor	Neurological Disease
Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycoproteins, and glycolipids in animal tissues and in some microorganisms. Uridine-5′-diphosphoglucose is an agonist of the P2Y₁₄ receptor, a neuroimmune system GPCR.

HY-10349

WAY-100635	5-HT Receptor Dopamine Receptor	Neurological Disease
WAY-100635 is a potent and selective 5-HT_1A Receptor antagonist with a pIC₅₀ of 8.87, an apparent pA₂ of 9.71. WAY-100635 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 has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D₄ receptor agonist.

HY-120528A

GB-110 hydrochloride	Protease-Activated Receptor (PAR)	Cancer Inflammation/Immunology
GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca²⁺ release in HT29 cells with an EC₅₀ of 0.28 μM.

HY-P1091

Hemopressin (human, mouse)	Cannabinoid Receptor	Neurological Disease
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.

HY-103186

MRS-1706	Adenosine Receptor	Inflammation/Immunology
MRS-1706 is a potent and selective adenosine A_2B receptor inverse agonist. MRS-1706 has K_i values of 1.39, 112, 157, and 230 nM for human A_2B, A_2A, A₁ and A₃ receptors respectively.

HY-13225

Rivanicline oxalate RJR-2403 oxalate; (E)-Metanicotine oxalate	nAChR	Neurological Disease
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (K_i=26 nM); > 1,000 fold selectivity than α7 receptors(K_i= 3.6 μM).

HY-B0637

Bezafibrate BM15075	PPAR	Metabolic Disease Cardiovascular Disease
Bezafibrate is an agonist of PPAR, with EC₅₀s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

HY-107514

(RS)-PPG	mGluR	Neurological Disease
(RS)-PPG is a potent and selective agonist for group III mGluRs. The EC₅₀s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.

HY-13225B

Rivanicline hemioxalate RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate	nAChR	Neurological Disease
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (K_i=26 nM); > 1,000 fold selectivity than α7 receptors(K_i= 3.6 μM).

HY-124136

WYC-209	RAR/RXR Apoptosis Autophagy	Cancer
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC₅₀=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity.

HY-P1256

JMV 449	Neurotensin Receptor	Neurological Disease
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC₅₀ of 0.5 nM in binding to mouse brain membranes and an EC₅₀ of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.

HY-P2454

CSP1	Bacterial	Infection
CSP1 is a potent and selective ComD1 receptor agonist, with an IC₅₀ of 10.3 nM. CSP1 is a major variants of competence-stimulating peptide (CSP), and it can regulate genetic transformation of S. pneumonia by modulating quorum sensing (QS). CSP1 can act as an antibacterial agent.

HY-101173

Imetit dihydrobromide VUF 8325 dihydrobromide; SKF 91105 dihydrobromide	Histamine Receptor	Neurological Disease
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with K_i values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC₅₀=25 nM).

HY-P1316

Ac-RYYRWK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [³H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a K_d of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.

HY-19358A

2-Methyl-5-HT hydrochloride 2-Methyl-5-hydroxytryptamine hydrochloride; 2-Methylserotonin hydrochloride; 2-Me-HT hydrochloride	5-HT Receptor	Neurological Disease
2-Methyl-5-HT hydrochloride (2-Methyl-5-hydroxytryptamine hydrochloride) is a potent and selective 5-HT₃ receptor agonist. 2-Methyl-5-HT hydrochloride is shown to display anti-depressive-like effects.

HY-106660

BP 897	Dopamine Receptor	Neurological Disease
BP 897 is a potent and selective dopamine D3 receptor agonist, and a weak dopamine D2 receptor antagonist, with K_is of 0.92 nM and 61 nM for D3 and D2 receptors, and shows low affinities at D1 and D4 receptors (K_is, 3 and 0.3 µM, respectively).

HY-100999

(R)-(-)-α-Methylhistamine dihydrobromide	Histamine Receptor	Neurological Disease
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a K_d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats.

HY-15701A

(Z)-Leukadherin-1 ADH-503 free base	Complement System	Cancer
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.

HY-P1341A

OXA(17-33) TFA	Orexin Receptor (OX Receptor)	Neurological Disease
OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC₅₀=8.29 nM) over OX2 (187 nM).

HY-135750

VAF347	Aryl Hydrocarbon Receptor	Inflammation/Immunology
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14⁺CD11b⁺ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.

HY-15129

O-Phospho-L-serine L-Serine O-phosphate; L-SOP	mGluR Endogenous Metabolite	Neurological Disease
O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.

HY-19231

DPI-3290 Org 41793	Opioid Receptor	Neurological Disease
DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with K_i values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.

HY-P1316A

Ac-RYYRWK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [³H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a K_d of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors.

HY-19358

2-Methyl-5-HT 2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT	5-HT Receptor	Neurological Disease
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT₃ receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.

HY-P1319A

Nociceptin(1-7) TFA	Opioid Receptor	Inflammation/Immunology
Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL₁ (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.

HY-116637

Tetrahydromagnolol Magnolignan	Cannabinoid Receptor GPR55	Inflammation/Immunology
Tetrahydromagnolol (Magnolignan), a main metabolite of Magnolol, is a potent and selective cannabinoid CB2 receptor agonist with an EC₅₀ of 170 nM and a K_i of 416 nM. Tetrahydromagnolol possesses 20-fold more selective for CB2 receptor than CB1 receptor. Tetrahydromagnolol is also a weak GPR55 receptor antagonist.

HY-108741

Plecanatide	Guanylate Cyclase	Inflammation/Immunology
Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC₅₀ of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

HY-12752

Alimemazine Trimeprazine	Others	Inflammation/Immunology Neurological Disease
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays sedative, antiserotonin, antispasmodic, and antiemetic properties.

HY-P1214A

γ1-MSH TFA	Melanocortin Receptor	Cardiovascular Disease
γ1-MSH TFA is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH TFA displays ~40-fold selectivity over MC4 (K_i=1318 nM).

HY-19358B

2-Methyl-5-HT maleate 2-Methyl-5-hydroxytryptamine maleate; 2-Methylserotonin maleate; 2-Me-HT maleate	5-HT Receptor	Neurological Disease
2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT₃ receptor agonist. 2-Methyl-5-HT maleate is shown to display anti-depressive-like effects.

HY-103697A

Gardiquimod diTFA	Toll-like Receptor (TLR) HIV	Cancer Infection
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.

HY-119744

BAY 38-7271	Cannabinoid Receptor	Neurological Disease
BAY 38-7271 is selective and highly potent and cannabinoid CB₁/CB₂ receptor agonist, with K_is of 1.85 nM and 5.96 nM for recombinant human CB₁ receptor and CB₂ receptor, respectively. BAY 38-7271 has strong neuroprotective properties.

HY-10046

Plerixafor AMD 3100; JM3100; SID791	CXCR HIV Virus Protease	Cancer Infection Endocrinology Inflammation/Immunology
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM.

HY-14611

3,3'-Difluorobenzaldazine DFB	mGluR	Neurological Disease
3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC₅₀s in the 2 to 5 μM range.

HY-B0032A

Lurasidone SM-13496	5-HT Receptor Dopamine Receptor	Neurological Disease
Lurasidone (SM-13496) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

HY-B0032

Lurasidone Hydrochloride SM-13496 Hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D₂ and 5-HT₇ with IC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75 nM.

HY-B1557A

Betazole dihydrochloride Ametazole dihydrochloride	Histamine Receptor	Metabolic Disease
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.

HY-W063968

RO8191 RO4948191	IFNAR JAK STAT HCV	Infection
RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC₅₀ of 200 nM for HCV replicon.

HY-13956S

Pioglitazone D4 U 72107 D4	PPAR Ferroptosis	Cancer Metabolic Disease
Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. 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-W020468

Linopirdine DuP 996	Potassium Channel TRP Channel	Neurological Disease
Linopirdine (DuP 996) is an orally active, selective M-type K⁺ current (IM; Kv7; KCNQ Channels) inhibitor with an IC₅₀ of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing drug, increases acetylcholine release in rat brain tissue.

HY-112813

TUG-1375	Others	Metabolic Disease
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pK_i of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.

HY-P0227

SHU 9119	Melanocortin Receptor	Metabolic Disease
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC₅₀ values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.

HY-113854

AZD2906	Glucocorticoid Receptor	Cardiovascular Disease Endocrinology
AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC₅₀s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively.

HY-B1810

Tulobuterol C-78 free base	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Tulobuterol (C-78 free base) is a long-acting β₂-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol is also a sympathomimetic agent used as a transdermal patch, and increases normal diaphragm muscle strength.

HY-P1112

Sarafotoxin S6a	Endothelin Receptor	Neurological Disease Cardiovascular Disease
Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an ET_A/ET_B selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC₅₀ value of 7.5 nM.

HY-100450

BML-111	Angiotensin-converting Enzyme (ACE)	Cancer Inflammation/Immunology Cardiovascular Disease
BML-111, a lipoxin A₄ analog, is a lipoxin A₄ receptor agonist. BML-111 represses the activity of angiotensin converting enzyme (ACE) and increases the activity of angiotensinconverting enzyme 2 (ACE2). BML-111 has antiangiogenic, antitumor and anti-inflammatory properties.

HY-133533

O-2050	Cannabinoid Receptor
O-2050 is a high affinity cannabinoid CB₁ receptor silent antagonist. O-2050 also acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC₅₀=40.4 nM). O-2050 antagonizes effects of CP-55940 in vitro.

HY-12150

CCMI	nAChR	Neurological Disease
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.

HY-101176

2-Iodomelatonin	Melatonin Receptor	Cancer
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a K_i value of 28 pM, it is more 5-fold selective for MT₁ over MT₂. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.

HY-113008A

cis-Urocanic acid (Z)-Urocanic acid; cis-UCA	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (K_d=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

HY-13306

Pyrintegrin	Integrin	Metabolic Disease
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.

HY-W010907

Pamoic acid disodium	ERK	Neurological Disease
Pamoic acid disodium is a potent GPR35 agonist with an EC₅₀ value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC₅₀ values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect.

HY-128865

BPR1M97	Opioid Receptor	Neurological Disease
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with K_i values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.

HY-101854

N6-(2-Phenylethyl)adenosine N6-Phenethyladenosine; N6-Phenylethyladenosine	Adenosine Receptor	Cancer Inflammation/Immunology
N6-(2-Phenylethyl)adenosine (N6-Phenethyladenosine), an adenosine derivative, is a potent adenosine receptors (AR) agonist with K_i values of 11.8 nM, 30.1 nM, 0.63 nM for rat A₁AR, human A₁AR and hA₃AR, respectively.

HY-B1322A

Amodiaquine Amodiaquin	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-100804

L-Cysteinesulfinic acid	mGluR Endogenous Metabolite	Neurological Disease
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

HY-110173

TC-G 1005	GPCR19	Metabolic Disease
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC₅₀s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.

HY-14813

Cutamesine SA4503; AGY 94806	Sigma Receptor	Neurological Disease
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.

HY-P1112A

Sarafotoxin S6a TFA	Endothelin Receptor	Neurological Disease Cardiovascular Disease
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ET_A/ET_B selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC₅₀ value of 7.5 nM.

HY-P1090

Hemopressin(rat)	Cannabinoid Receptor	Neurological Disease
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.

HY-W017230

L-Cysteinesulfinic acid monohydrate	mGluR	Neurological Disease
L-Cysteinesulfinic acid monohydrate is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC₅₀s of 3.92, 4.6, 3.9, 2.7, 4.0, and 3.94 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively.

HY-111793

NUCC-390	CXCR	Neurological Disease
NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.

HY-P1091A

Hemopressin(human, mouse) TFA	Cannabinoid Receptor	Neurological Disease
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.

HY-B0061

Tandospirone citrate SM-3997 citrate	5-HT Receptor	Neurological Disease
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).

HY-76772

Cevimeline hydrochloride hemihydrate SNI-2011; AF102B hydrochloride hemihydrate	mAChR	Neurological Disease
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).

HY-111793A

NUCC-390 dihydrochloride	CXCR	Neurological Disease
NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.

HY-P1072

PHM-27 (human)	CGRP Receptor	Metabolic Disease Cardiovascular Disease
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC₅₀ of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.

HY-100808

(R)-Serine	iGluR Endogenous Metabolite	Others
(R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. (R)-Serine has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.

HY-110279

Ogerin	Others	Neurological Disease
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC₅₀ of 6.83. Ogerin shows inverse agonist and antagonist activity (K_i, 220 nM) at A_2A receptoor and weak antagonist activity (K_i, 736 nM) at 5-HT_2B receptor. Ogerin blocks recall in fear conditioning in mice.

HY-14262

Vilazodone EMD 68843; SB659746A	5-HT Receptor Serotonin Transporter	Neurological Disease
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT₁A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.

HY-117066

CL075 3M002	Toll-like Receptor (TLR)	Inflammation/Immunology
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.

HY-108497

L-803087	Somatostatin Receptor	Cancer Neurological Disease
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a K_i of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.

HY-101698

Alniditan Alnitidan	5-HT Receptor	Neurological Disease
Alniditan is a potent 5-HT_1B/1D receptors agonist, with IC₅₀ of 1.7 and 1.3 nM in HEK 293 cells, and pK_i value of 8.96 and 9.40 for 5-HT_1B/1D receptors, respectively.

HY-14539

Clozapine HF 1854	Dopamine Receptor mAChR	Neurological Disease
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors, with a K_i of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

HY-134130

Integrin modulator 1	Integrin	Inflammation/Immunology
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC₅₀ of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC₅₀ of 12.9 nM.

HY-70020B

Cevimeline hydrochloride AF102B hydrochloride	mAChR	Neurological Disease
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).

HY-126351

PROTAC ERRα ligand 2	Estrogen Receptor/ERR	Cancer
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC₅₀ of 5.67 nM. PROTAC ERRα ligand 2 (IC₅₀=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC₅₀=61.3 nM).

HY-12980

Batefenterol GSK961081; TD-5959	Adrenergic Receptor mAChR	Inflammation/Immunology Endocrinology
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β₂-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ₂-adrenoceptor with K_i values of 1.4, 1.3 and 3.7 nM, respectively.

HY-10964

Vadimezan DMXAA; ASA-404	STING IFNAR Influenza Virus	Cancer Infection
Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.

HY-129851

NTP42	Prostaglandin Receptor	Cardiovascular Disease
NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC₅₀ of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca²⁺] mobilization following stimulation of cells with the alternative TP agonist U46609. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).

HY-120006A

(rel)-AR234960	ERK	Cardiovascular Disease
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.

HY-14151

Prucalopride	5-HT Receptor	Neurological Disease
Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.

HY-12598

(S)-3,5-DHPG	mGluR	Neurological Disease
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with K_i values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.

HY-42110

Deschloroclozapine	mAChR	Neurological Disease
Deschloroclozapine is a potent, high affinity, selective, metabolically stable agonist of muscarinic-based DREADDs. Deschloroclozapine inhibites [³H]quinuclidinyl benzilate (QNB) binding to hM₃Dq and hM₄Di with K_i of 6.3 and 4.2 nM. Deschloroclozapine is reported with utility in both mice and non-human primates for a variety of applications.

HY-B1816

Zaprinast M&B 22948	Phosphodiesterase (PDE)	Neurological Disease Cardiovascular Disease Endocrinology
Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.

HY-15688

8-Hydroxy-DPAT hydrobromide 8-OH-DPAT hydrobromide	5-HT Receptor	Neurological Disease
8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT_1A agonist with a pIC₅₀ of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT₁ binding site.

HY-10232

THIP Gaboxadol	GABA Receptor	Neurological Disease
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.

HY-113209

8-Isoprostaglandin F2α	Endogenous Metabolite	Others
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.

HY-15536

Cebranopadol GRT6005	Opioid Receptor	Neurological Disease
Cebranopadol is an analgesic NOP and opioid receptor agonist with K_is/EC₅₀s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.

HY-136363

MDR-652	TRP Channel	Neurological Disease
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The K_is are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC₅₀s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.

HY-14558

Tandospirone SM-3997	5-HT Receptor	Neurological Disease
Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).

HY-104037

Cintirorgon LYC-55716	ROR	Cancer
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.

HY-P1423

BA 1	Bombesin Receptor
BA 1 is a potent bombesin receptor agonist (IC₅₀ values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). BA 1 enhances glucose transport in obese and diabetic primary myocytes. BA 1 also stimulates NCI-H1299 lung cancer cell proliferation in vitro.

HY-124071

ACT-389949	Others	Inflammation/Immunology
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC₅₀ of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders.

HY-108795A

Albiglutide TFA	Glucagon Receptor	Metabolic Disease
Albiglutide TFA, a glucagon-like peptide (GLP)-1 mimetic, is a long acting GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus (T2DM). Albiglutide TFA is generated by the genetic fusion of a DPP-4-resistant GLP-1 dimer to human albumin.

HY-N3940

Gelsevirine	Others	Cancer Neurological Disease
Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC₅₀ values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively.

HY-14539S

Clozapine D8 HF 1854 D8	Dopamine Receptor mAChR	Neurological Disease
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a K_i of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

HY-70020

Cevimeline AF102B	mAChR	Neurological Disease
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).

HY-P1090A

Hemopressin(rat) TFA	Cannabinoid Receptor	Neurological Disease
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.

HY-101364A

CHPG sodium salt	mGluR NF-κB ERK Akt	Inflammation/Immunology Neurological Disease
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways..

HY-102022

α-Galactosylceramide α-GalCer; KRN7000	Others	Cancer Inflammation/Immunology
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).

HY-50906

LY404039	mGluR	Neurological Disease
LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with K_is of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.

HY-B1322

Amodiaquine dihydrochloride dihydrate Amodiaquin dihydrochloride dihydrate	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-108741A

Plecanatide acetate	Guanylate Cyclase	Inflammation/Immunology
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC₅₀ of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis.

HY-P1131

M617	Others	Cardiovascular Disease
M617 is a selective galanin receptor 1 (GAL1) agonist, with K_is of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats.

HY-10426

XCT790	Estrogen Receptor/ERR Autophagy	Cancer
XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

HY-101478

Fenobam	mGluR	Neurological Disease
Fenobam is a selective, orally active, and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (K_d values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC₅₀ of 84 nM. Fenobam exerts anxiolytic activity.

HY-14422

SR1078	ROR	Cancer
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.

HY-12598A

DHPG (RS)-3,5-DHPG	mGluR	Neurological Disease
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs. DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D.

HY-14363

TUG-424	GPR40	Metabolic Disease
TUG-424 is a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC₅₀ of 32 nM. TUG-424 significantly increases glucose-stimulated insulin secretion at 100 nM. TUG-424 may serve to explore the role of FFA1 in metabolic diseases such as diabetes or obesity.

HY-P1250

RFRP-3(human) Neuropeptide VF(124-131)(human)	Neuropeptide Y Receptor	Neurological Disease
RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca²⁺ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC₅₀ of 0.7 nM.

HY-101364

CHPG	mGluR NF-κB ERK Akt	Inflammation/Immunology Cardiovascular Disease
CHPG is a selective mGluR5 agonist, and attenuates SO₂-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells. CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.

HY-B1322B

Amodiaquine dihydrochloride Amodiaquin dihydrochloride	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-108768

Pasireotide pamoate SOM230 pamoate	Somatostatin Receptor	Cancer
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

HY-P1119

WRW4	Others	Neurological Disease
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC₅₀ of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.

HY-14649

Retinoic acid Vitamin A acid; all-trans-Retinoic acid; ATRA	RAR/RXR PPAR Endogenous Metabolite Autophagy	Cancer
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with K_d of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

HY-12554

Terlipressin	Vasopressin Receptor	Endocrinology Inflammation/Immunology Cardiovascular Disease
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

HY-131454

SR-717	STING	Cancer Inflammation/Immunology
SR-717 is a non-nucleotide STING agonist with EC₅₀s of 2.1 μM and 2.2 μM in ISG-THP1 (WT) and ISG-THP1 cGAS KO (cGAS KO) cell lines, respectively. SR-717 is a stable cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic. Antitumor activity.

HY-16688

RU 24969	5-HT Receptor	Neurological Disease
RU 24969 is a preferential 5-HT_1B agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.

HY-15543A

CP-809101 hydrochloride	5-HT Receptor	Neurological Disease
CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively.

HY-13717

AGN194204 IRX4204; NRX194204; VTP 194204	RAR/RXR Apoptosis	Cancer Inflammation/Immunology
AGN194204 (IRX4204) is an orally active and selective RXR agonist with K_d values 0.4 nM, 3.6 nM and 3.8 nM and EC₅₀s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.

HY-14648

Dexamethasone Hexadecadrol; Prednisolone F	Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic	Cancer Infection Endocrinology Inflammation/Immunology
Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.

HY-101299A

Dihydrexidine DAR-0100	Dopamine Receptor	Neurological Disease
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC₅₀ of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.

HY-12554A

Terlipressin acetate	Vasopressin Receptor	Endocrinology Inflammation/Immunology Cardiovascular Disease
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

HY-B0731

Perospirone hydrochloride SM-9018	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT_2A receptor (K_i of 0.6 nM) and dopamine D₂ receptor (K_i of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT_1A receptor (K_i of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.

HY-107676

SIB-1553A	nAChR	Neurological Disease
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.

HY-13591

Piclidenoson IB-MECA; CF-101	Adenosine Receptor Apoptosis	Cancer
Piclidenoson (IB-MECA;CF-101) is a first-in-class, orally bioavailable and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.

HY-P1390

d[Cha4]-AVP	Vasopressin Receptor
d[Cha4]-AVP is a potent and selective human vasopressin V1B receptor agonist (K_i values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.

HY-P1423A

BA 1 TFA	Bombesin Receptor	Cancer
BA 1 TFA is a potent bombesin receptor agonist (IC₅₀ values are 0.26, 1.55 and 2.52 nM for BB1, BB2 and BB3 respectively). BA 1 TFA enhances glucose transport in obese and diabetic primary myocytes. BA 1 TFA also stimulates NCI-H1299 lung cancer cell proliferation in vitro.

HY-19976

RN-1747	TRP Channel	Cardiovascular Disease
RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 (TRPV4) agonist, with EC₅₀ values are 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively. RN-1747 also antagonizes TRPM8, with an IC₅₀ of 4 μM.

HY-128932

Cefminox sodium MT-141	Bacterial PPAR Prostaglandin Receptor Antibiotic	Infection Cardiovascular Disease Endocrinology
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.

HY-W008634

Bropirimine	Toll-like Receptor (TLR)	Cancer
Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract.

HY-P1250A

RFRP-3(human) TFA Neuropeptide VF(124-131)(human) TFA	Neuropeptide Y Receptor	Neurological Disease
RFRP-3 (Neuropeptide VF(124-131))(human) TFA, a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca²⁺ mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC₅₀ of 0.7 nM.

HY-108057A

Facinicline hydrochloride RG3487 hydrochloride	nAChR 5-HT Receptor	Neurological Disease
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K_i of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT₃Rs with a K_i value of 1.2 nM.

HY-W011733

Tulobuterol hydrochloride C-78	Adrenergic Receptor Influenza Virus Antibiotic	Infection Endocrinology Inflammation/Immunology
Tulobuterol hydrochloride (C-78) is a long-acting β₂-adrenoceptor agonist, which reduces the frequency of exacerbations of chronic obstructive pulmonary disease and bronchial asthma. Tulobuterol hydrochloride is also a sympathomimetic agent used as a transdermal patch, increases normal diaphragm muscle strength. Tulobuterol hydrochloride inhibit rhinovirus replication and modulate airway inflammation.

HY-117388

THI0019	Integrin	Inflammation/Immunology
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC₅₀ range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.

HY-19436

Solabegron GW 427353	Adrenergic Receptor	Metabolic Disease Endocrinology
Solabegron (GW 427353) is a selective β₃-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β₃-AR, with an EC₅₀ value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of overactive bladder and irritable bowel syndrome.

HY-101299B

Dihydrexidine hydrochloride DAR-0100 hydrochloride	Dopamine Receptor	Neurological Disease
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC₅₀ of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.

HY-A0072S

Zilpaterol-d7	Adrenergic Receptor
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.

HY-16688B

RU 24969 hemisuccinate	5-HT Receptor	Neurological Disease
RU 24969 hemisuccinate is a preferential 5-HT_1B agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion.

HY-136527

BMS-986251	ROR Interleukin Related	Inflammation/Immunology
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC₅₀ of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC₅₀ of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).

HY-P1390A

d[Cha4]-AVP TFA	Vasopressin Receptor
d[Cha4]-AVP TFA is a potent and selective human vasopressin V1B receptor agonist (K_i values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP TFA stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.

HY-B0623A

Ropinirole hydrochloride SKF 101468 hydrochloride	Dopamine Receptor	Neurological Disease
Ropinirole hydrochloride is a potent D₃/D₂ receptor agonist with a K_i of 29 nM for D₂ receptor. Ropinirole hydrochloride has pEC₅₀s of 7.4, 8.4 and 6.8 for hD₂, hD₃ and hD₄ receptors, respectively. Ropinirole hydrochloride has no affinity for the D₁ receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.

HY-100822

(R)-(+)-HA-966
(+)-HA-966
iGluR

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