Search Result

Targets Recommended:	5-HT Receptor 5 alpha Reductase FLAP CD73 RAR/RXR CXCR nAChR mGluR iGluR Protease-Activated Receptor (PAR) PPAR PIKfyve TGF-β Receptor Serotonin Transporter Oct3/4

Results for "5-ht5 Receptors Inhibitors" in MCE Product Catalog:

By Targets:	5-HT Receptor (117) CXCR (2) iGluR (2) mGluR (7) nAChR (5) PPAR (1) Protease-Activated Receptor (PAR) (1) Serotonin Transporter (3) TGF-β Receptor (2) AChE (2) ADC Cytotoxin (1) Adenosine Receptor (2) Adrenergic Receptor (15) ALK (1) AMPK (2) Androgen Receptor (2) Antibiotic (2) Apoptosis (2) Autophagy (5) Bacterial (5) Bcr-Abl (1) Bradykinin Receptor (1) Calcium Channel (4) CaMK (1) Cannabinoid Receptor (2) Casein Kinase (1) CCR (2) CFTR (1) CGRP Receptor (2) Chloride Channel (1) Complement System (3) CRFR (1) Cytochrome P450 (2) Dopamine Receptor (34) Drug Metabolite (1) DYRK (2) E3 Ligase Ligand-Linker Conjugate (1) EBI2/GPR183 (1) Endogenous Metabolite (10) Endothelin Receptor (2) Ephrin Receptor (1) Epoxide Hydrolase (1) Factor Xa (1) Fatty Acid Synthase (FASN) (1) FXR (1) GABA Receptor (7) GHSR (1) Glucocorticoid Receptor (1) GLUT (1) GPR119 (1) GPR84 (1) Histamine Receptor (5) HIV (1) IGF-1R (1) Influenza Virus (2) Insulin Receptor (1) Integrin (1) Ligand for E3 Ligase (2) Ligand for Target Protein for PROTAC (2) LPL Receptor (1) mAChR (13) MicroRNA (1) Microtubule/Tubulin (1) Mitophagy (1) MMP (1) Neurokinin Receptor (1) Neuropeptide Y Receptor (1) NO Synthase (2) Opioid Receptor (9) Orexin Receptor (OX Receptor) (3) Oxytocin Receptor (2) P-glycoprotein (4) P2X Receptor (2) p38 MAPK (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PKA (1) PKC (1) Potassium Channel (2) Prostaglandin Receptor (1) PROTAC (1) PROTAC Linker (2) Reverse Transcriptase (1) RIP kinase (1) ROR (1) SARS-CoV (2) Sigma Receptor (1) Sodium Channel (3) Somatostatin Receptor (2) Thrombin (1) Thymidylate Synthase (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) Topoisomerase (1) TRP Channel (5) TSH Receptor (1) Urotensin Receptor (2)
By Research Areas:	Cancer (32) Cardiovascular Disease (33) Endocrinology (18) Infection (6) Inflammation/Immunology (23) Metabolic Disease (23) Neurological Disease (185)

By Targets:

5-HT Receptor (117)

CXCR (2)

iGluR (2)

mGluR (7)

nAChR (5)

PPAR (1)

Protease-Activated Receptor (PAR) (1)

Serotonin Transporter (3)

TGF-β Receptor (2)

AChE (2)

ADC Cytotoxin (1)

Adenosine Receptor (2)

Adrenergic Receptor (15)

ALK (1)

AMPK (2)

Androgen Receptor (2)

Antibiotic (2)

Apoptosis (2)

Autophagy (5)

Bacterial (5)

Bcr-Abl (1)

Bradykinin Receptor (1)

Calcium Channel (4)

CaMK (1)

Cannabinoid Receptor (2)

Casein Kinase (1)

CCR (2)

CFTR (1)

CGRP Receptor (2)

Chloride Channel (1)

Complement System (3)

CRFR (1)

Cytochrome P450 (2)

Dopamine Receptor (34)

Drug Metabolite (1)

DYRK (2)

E3 Ligase Ligand-Linker Conjugate (1)

EBI2/GPR183 (1)

Endogenous Metabolite (10)

Endothelin Receptor (2)

Ephrin Receptor (1)

Epoxide Hydrolase (1)

Factor Xa (1)

Fatty Acid Synthase (FASN) (1)

FXR (1)

GABA Receptor (7)

GHSR (1)

Glucocorticoid Receptor (1)

GLUT (1)

GPR119 (1)

GPR84 (1)

Histamine Receptor (5)

HIV (1)

IGF-1R (1)

Influenza Virus (2)

Insulin Receptor (1)

Integrin (1)

Ligand for E3 Ligase (2)

Ligand for Target Protein for PROTAC (2)

LPL Receptor (1)

mAChR (13)

MicroRNA (1)

Microtubule/Tubulin (1)

Mitophagy (1)

MMP (1)

Neurokinin Receptor (1)

Neuropeptide Y Receptor (1)

NO Synthase (2)

Opioid Receptor (9)

Orexin Receptor (OX Receptor) (3)

Oxytocin Receptor (2)

P-glycoprotein (4)

P2X Receptor (2)

p38 MAPK (1)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

PKA (1)

PKC (1)

Potassium Channel (2)

Prostaglandin Receptor (1)

PROTAC (1)

PROTAC Linker (2)

Reverse Transcriptase (1)

RIP kinase (1)

ROR (1)

SARS-CoV (2)

Sigma Receptor (1)

Sodium Channel (3)

Somatostatin Receptor (2)

Thrombin (1)

Thymidylate Synthase (1)

TNF Receptor (1)

Toll-like Receptor (TLR) (1)

Topoisomerase (1)

TRP Channel (5)

TSH Receptor (1)

Urotensin Receptor (2)

By Research Areas:

Cancer (32)

Cardiovascular Disease (33)

Endocrinology (18)

Infection (6)

Inflammation/Immunology (23)

Metabolic Disease (23)

Neurological Disease (185)

285

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas

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-U00408

5-HT3 antagonist 2
5-HT Receptor Neurological Disease

5-HT3 antagonist 2 is a 5-HT3 receptor antagonist.

5-HT3 antagonist 2	5-HT Receptor	Neurological Disease
5-HT3 antagonist 2 is a *5-HT3* receptor antagonist.

HY-U00322

5-HT3 antagonist 3	5-HT Receptor	Neurological Disease
5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with K_i of 0.25 nM.

HY-101638

FK1052 hydrochloride
5-HT Receptor Neurological Disease

FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
HY-100170

5-HT4 antagonist 1
5-HT Receptor Neurological Disease

5-HT4 antagonist 1 is a 5-HT₄ receptor antagonist with a pK_i of 9.6.

FK1052 hydrochloride	5-HT Receptor	Neurological Disease
FK1052 hydrochloride is a potent *5-HT3* and *5-HT4* receptor dual antagonist.

5-HT4 antagonist 1	5-HT Receptor	Neurological Disease
5-HT4 antagonist 1 is a 5-HT₄ receptor antagonist with a pK_i of 9.6.

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-107836

Methiothepin mesylate Metitepine mesylate; Ro 8-6837 mesylate	5-HT Receptor	Neurological Disease
Methiothepin mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-U00368

5-HT3 antagonist 1
5-HT Receptor Neurological Disease

5-HT3 antagonist 1 is a potent and selective antagonist of serotonin 3 (5-HT3) receptor.

5-HT3 antagonist 1	5-HT Receptor	Neurological Disease
5-HT3 antagonist 1 is a potent and selective antagonist of *serotonin 3 (5-HT3) receptor*.

HY-U00365

5-HT2 antagonist 1	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.

HY-19889

JNJ-18038683	5-HT Receptor	Neurological Disease
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT₇) receptor antagonist, with pK_is of 8.19, 8.20 for rat and human 5-HT₇ in HEK293 cells, respectively.

HY-B0274

Chlorprothixene	Dopamine Receptor Bacterial	Neurological Disease
Chlorprothixene has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.

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-B0352

Mirtazapine Org3770; 6-Azamianserin	5-HT Receptor	Neurological Disease
Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.

HY-103110A

ST1936 oxalate	5-HT Receptor	Neurological Disease
ST1936 oxalate is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human *5-HT₆, 5-HT₇* and 5-HT_2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.

HY-101632

Irindalone
Lu 21-098
5-HT Receptor Neurological Disease

Irindalone is a novel serotonin 5-HT₂ antagonist.
HY-101668

Sulamserod
RS-100302
5-HT Receptor Cardiovascular Disease

Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
HY-103099

SB-399885 hydrochloride
5-HT Receptor Neurological Disease

SB-399885 hydrochloride is a 5-HT₆ receptor antagonist.

Irindalone Lu 21-098	5-HT Receptor	Neurological Disease
Irindalone is a novel serotonin *5-HT₂* antagonist.

Sulamserod RS-100302	5-HT Receptor	Cardiovascular Disease
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.

SB-399885 hydrochloride	5-HT Receptor	Neurological Disease
SB-399885 hydrochloride is a 5-HT₆ receptor antagonist.

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-15574

Piboserod
SB-207266
5-HT Receptor Cardiovascular Disease

Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.
HY-19684

Pancopride
LAS 30451
5-HT Receptor Neurological Disease

Pancopride is a new potent and selective 5-HT₃ receptor antagonist.

Piboserod SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod (SB 207266) is a selective 5-HT(4) receptor antagonist.

Pancopride LAS 30451	5-HT Receptor	Neurological Disease
Pancopride is a new potent and selective 5-HT₃ receptor antagonist.

HY-103142

AS19	5-HT Receptor	Neurological Disease
AS19 is a potent, selective 5-HT₇ receptor agonist with an IC₅₀ value of 0.83 nM and a K_i of 0.6 nM. AS19 is selective for *5-HT₇* over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.

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-100943

Cinanserin hydrochloride SQ 10643	5-HT Receptor Influenza Virus	Infection Inflammation/Immunology
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT₂ receptor antagonist with a K_i of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the *5-HT₂* than for the 5-HT₁ receptor (K_i of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.

HY-14335

Ro 04-6790	5-HT Receptor	Neurological Disease
Ro 04-6790 is a potent, competitive and selective *5-HT₆* receptor antagonist with pK_i values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 has no affinity at other receptors.

HY-U00443

SB 258719
5-HT Receptor Neurological Disease

SB 258719 is a selective 5-HT₇ receptor antagonist with a pK_i of 7.5.
HY-B0366A

Cyproheptadine hydrochloride
5-HT Receptor Neurological Disease

Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM.
HY-15574A

Piboserod hydrochloride
SB-207266 hydrochloride
5-HT Receptor Cardiovascular Disease

Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.
HY-12392

Iprindole
5-HT Receptor Metabolic Disease Neurological Disease

Iprindole, a tricyclic indole antidepressant, is a weak inhibitor of the uptake of noradrenaline and 5-HT.

SB 258719	5-HT Receptor	Neurological Disease
SB 258719 is a selective 5-HT₇ receptor antagonist with a pK_i of 7.5.

Cyproheptadine hydrochloride	5-HT Receptor	Neurological Disease
Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM.

Piboserod hydrochloride SB-207266 hydrochloride	5-HT Receptor	Cardiovascular Disease
Piboserod (SB 207266) Hcl is a selective 5-HT(4) receptor antagonist.

Iprindole	5-HT Receptor	Metabolic Disease Neurological Disease
Iprindole, a tricyclic indole antidepressant, is a weak inhibitor of the uptake of noradrenaline and 5-HT.

HY-103090

NPS ALX Compound 4a	5-HT Receptor	Neurological Disease
NPS ALX Compound 4a is a potent and selective *5-hydroxytryptamine₆ (5-HT₆)* receptor antagonist, with an IC₅₀ of 7.2 nM and a K_i** of 0.2 nM.

HY-103090A

NPS ALX Compound 4a dihydrochloride	5-HT Receptor	Neurological Disease
NPS ALX Compound 4a dihydrochloride is a potent and selective *5-hydroxytryptamine₆ (5-HT₆)* receptor antagonist, with an IC₅₀ of 7.2 nM and a K_i** of 0.2 nM.

HY-14149

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

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

Cisapride (±)-Cisaprid; R 51619	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-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-14336A

SB 271046 Hydrochloride
SB 271046A
5-HT Receptor Neurological Disease

SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
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.

SB 271046 Hydrochloride SB 271046A	5-HT Receptor	Neurological Disease
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.

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-14338A

Idalopirdine Hydrochloride Lu AE58054 Hydrochloride	5-HT Receptor	Neurological Disease
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a potent and selective 5-HT6 receptor antagonist with a K_i of 0.83 nM.

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-103098

EMDT oxalate
5-HT Receptor Neurological Disease

EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects.
HY-14338

Idalopirdine
Lu AE58054
5-HT Receptor Neurological Disease

Idalopirdine (Lu AE58054) is a potent and selective 5-HT6 receptor antagonist with a K_i of 0.83 nM.
HY-19110

RG-12915
5-HT Receptor Cancer

RG-12915 is a selective 5-HT3 antagonist, with IC₅₀ value of 0.16 nM.

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.

EMDT oxalate	5-HT Receptor	Neurological Disease
EMDT oxalate is a selective *5-HT6* agonist, and has antidepressant effects.

Idalopirdine Lu AE58054	5-HT Receptor	Neurological Disease
Idalopirdine (Lu AE58054) is a potent and selective 5-HT6 receptor antagonist with a K_i of 0.83 nM.

RG-12915	5-HT Receptor	Cancer
RG-12915 is a selective *5-HT3* antagonist, with IC₅₀ value of 0.16 nM.

HY-101583

NEO 376 SPI-376	5-HT Receptor GABA Receptor Dopamine Receptor	Neurological Disease
NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.

HY-14940

Volinanserin MDL100907; M 100907	5-HT Receptor	Neurological Disease
Volinanserin is a potent and selective antagonist of 5-HT₂ receptor, with a K_i of 0.36 nM, and shows 300-fold selectivity for 5-HT₂ receptor over 5-HT_1c, alpha-1 and DA D₂ receptors. Volinanserin has antipsychotic activity.

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-B0595

Ramosetron Hydrochloride YM060	5-HT Receptor	Neurological Disease
Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.

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-A0018

Palonosetron
5-HT Receptor Cardiovascular Disease

Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Palonosetron	5-HT Receptor	Cardiovascular Disease
Palonosetron is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

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-U00028

T 82
5-HT Receptor AChE Neurological Disease

T 82 is a potent 5-HT3 antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.

T 82	5-HT Receptor AChE	Neurological Disease
T 82 is a potent *5-HT3* antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.

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-B0352S

Mirtazapine D3 Org3770 D3; 6-Azamianserin D3	5-HT Receptor	Neurological Disease
Mirtazapine D3 (Org3770 D3; 6-Azamianserin D3) is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors.

HY-A0021

Palonosetron Hydrochloride	5-HT Receptor	Cardiovascular Disease
Palonosetron Hcl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

HY-A0077AS

Perphenazine D8 Dihydrochloride	5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor	Endocrinology Neurological Disease
Perphenazine D8 Dihydrochloride is the deuterium labeled Perphenazine, which is a typical antipsychotic drug(5-HT, Dopamine receptor ligand).

HY-14340

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

HY-B0071

Granisetron BRL 43694	5-HT Receptor	Neurological Disease
Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

HY-B0750

Dolasetron
MDL-73147
5-HT Receptor Others

Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
HY-15370

SB-269970
5-HT Receptor Neurological Disease

SB269970 is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

HY-B0071A

Granisetron Hydrochloride BRL 43694A	5-HT Receptor	Neurological Disease
Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.

HY-10792

Eplivanserin SR-46349	5-HT Receptor	Neurological Disease
Eplivanserin is a potent, selective and orally available 5-HT₂ receptor antagonist, with an IC₅₀ of 5.8 nM in rat cortical membrane, and a K_d of 1.14 nM.

HY-B0068

Azasetron hydrochloride Y-25130 hydrochloride	5-HT Receptor	Neurological Disease
Azasetron (hydrochloride) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

HY-U00126

5HT6-ligand-1
5-HT Receptor Neurological Disease

5HT6-ligand-1 is a potent 5-HT6 receptor ligand with a K_i of 1.43 nM.

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-109118A

Masupirdine mesylate SUVN-502 mesylate	5-HT Receptor	Neurological Disease
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (K_i of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.

HY-102064

SR 57227A	5-HT Receptor	Neurological Disease
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC₅₀) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

HY-B0750B

Dolasetron Mesylate hydrate MDL-73147EF hydrate	5-HT Receptor	Others
Dolasetron Mesylate hydrate (MDL-73147EF hydrate) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.

HY-B0750A

Dolasetron Mesylate
MDL-73147EF
5-HT Receptor Cancer

Dolasetron Mesylate (MDL-73147EF) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.

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-10564

Sarpogrelate hydrochloride MCI-9042	5-HT Receptor	Cardiovascular Disease
Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.

HY-14339

Intepirdine SB-742457; GSK-742457; RVT-101	5-HT Receptor	Neurological Disease
Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.

HY-B1541

Bemesetron
MDL 72222
5-HT Receptor Neurological Disease

Bemesetron (MDL 72222) is a selective 5-HT₃ receptor antagonist with an IC₅₀ of 0.33 nM. Neuroprotective effect.

HY-B0002B

Ondansetron GR 38032; SN 307	5-HT Receptor	Neurological Disease
Ondansetron(GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.

HY-B0002

Ondansetron hydrochloride GR 38032 hydrochloride; SN 307 hydrochloride	5-HT Receptor	Neurological Disease
Ondansetron hydrochloride (GR 38032 hydrochloride; SN 307 hydrochloride) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.

HY-B0115

Pizotifen
BC-105; Pizotyline
5-HT Receptor Neurological Disease

Pizotifen (BC-105) is a potent 5-HT₂ receptor antagonist, with a high affinity for 5-HT_1C binding site.

HY-109118

Masupirdine free base SUVN-502 free base	5-HT Receptor	Neurological Disease
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (K_i of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.

HY-U00367

(4E)-SUN9221	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease Endocrinology
(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.

HY-U00413

5-HT3-In-1
5-HT Receptor Neurological Disease Cardiovascular Disease

5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.

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-B1107

Naftidrofuryl oxalate Nafronyl oxalate salt	5-HT Receptor	Cardiovascular Disease
Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.

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-B0115A

Pizotifen malate BC-105 malate; Pizotyline malate	5-HT Receptor	Neurological Disease
Pizotifen malate (BC-105 malate) is a potent *5-HT₂* receptor antagonist, with a high affinity for 5-HT_1C binding site.

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-B0002A

Ondansetron hydrochloride dihydrate GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate	5-HT Receptor	Neurological Disease
Ondansetron hydrochloride dihydrate (GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.

HY-N0925

Tetrahydroberberine Canadine	Dopamine Receptor	Neurological Disease
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).

HY-14325

L-745870	Dopamine Receptor	Neurological Disease
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-14325B

L-745870 hydrochloride	Dopamine Receptor	Neurological Disease
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-N4157

Isopteropodine	mAChR 5-HT Receptor	Neurological Disease
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and *5-HT2* receptors.

HY-15370A

SB-269970 hydrochloride SB-269970A	5-HT Receptor	Neurological Disease
SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pK_i of 8.3, exhibits >50-fold selectivity against other receptors.

HY-101622

5-HT6/7 antagonist 1	5-HT Receptor Dopamine Receptor
5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.

HY-101094

Ocaperidone R79598	5-HT Receptor Dopamine Receptor	Neurological Disease
Ocaperidone is an effective antipsychotic agent, acting as a potent *5-HT₂* and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.

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-14559

PRX-07034 hydrochloride	5-HT Receptor	Neurological Disease
PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a K_i= 4-8 nM and an IC₅₀ of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.

HY-101755

Tedatioxetine hydrobromide Lu AA 24530 hydrobromide	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT_2A, 5-HT_2C, *5-HT₃* and α_1A-adrenergic receptor antagonist.

HY-11018

Risperidone R 64 766	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-B1213

Trimipramine maleate	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate is a 5-HT receptor antagonist, with pK_is of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively.

HY-B0032S

Lurasidone D8 Hydrochloride SM-13496 D8	Others	Neurological Disease
Lurasidone D8 Hydrochloride is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.

HY-11018A

Risperidone hydrochloride R 64 766 hydrochloride	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-B0352B

(R)-Mirtazapine (R)-Org3770; (R)-6-Azamianserin	5-HT Receptor	Neurological Disease
(R)-Mirtazapine ((R)-Org3770) is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT₃ receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.

HY-11018B

Risperidone mesylate R 64 766 mesylate	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-15414

Vortioxetine Lu AA 21004	5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine is a inhibitor of 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT, with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-136281

DuP 734	Sigma Receptor	Neurological Disease
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.

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-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-B0352A

(S)-Mirtazapine (S)-Org3770; (S)-6-Azamianserin	5-HT Receptor	Neurological Disease
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT₂ receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.

HY-10791

Ritanserin R 55667	5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT₂ receptor, with an IC₅₀ of 0.9 nM, less active on Histamine H₁, Dopamine D₂, Adrenergic α₁, Adrenergic α₂ receptors.

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-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-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-135194

Risperidone E-oxime	Others	Others
Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .

HY-15414A

Vortioxetine hydrobromide Lu AA21004 hydrobromide	5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine hydrobromide is a multimodal serotonergic agent, inhibits 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-14264

Cyamemazine	5-HT Receptor	Neurological Disease
Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent *5-HT₃* (K_i of 12 nM), 5-HT_2A (K_i = 1.5 nM) and 5-HT_2C (K_i of 75 nM) receptors antagonist with antipsychotic activity.

HY-103104

Fananserin RP 62203	5-HT Receptor Dopamine Receptor	Neurological Disease
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT₂) receptor antagonist, with a K_i of 0.37 nM for the rat 5-HT_2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a K_i of 2.93 nM for the human dopamine D4 receptor.

HY-14325A

L-745870 trihydrochloride	Dopamine Receptor	Neurological Disease
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-B0352BS

(R)-Mirtazapine D3 (R)-Org3770 D3; (R)-6-Azamianserin D3	5-HT Receptor	Neurological Disease
(R)-Mirtazapine D3 ((R)-Org3770 D3) is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT₃ receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.

HY-15414S

Vortioxetine D8 Lu AA 21004 D8	5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT, with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-B0352AS

(S)-Mirtazapine D3 (S)-Org3770 D3; (S)-6-Azamianserin D3	5-HT Receptor	Neurological Disease
(S)-Mirtazapine D3 ((S)-Org3770 D3) is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT₂ receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.

HY-U00439

Protein kinase inhibitors 1
DYRK Cancer

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.

HY-112061

8-OH-DPAT 8-Hydroxy-DPAT	5-HT Receptor	Neurological Disease
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A and a K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

HY-32329

Setiptiline Org-8282	5-HT Receptor Adrenergic Receptor	Neurological Disease
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

HY-103152

GR 113808	5-HT Receptor	Inflammation/Immunology Neurological Disease
GR 113808 is a potent and highly selective 5-HT₄ receptor antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors.

HY-B1658A

Frovatriptan succinate hydrate	5-HT Receptor	Neurological Disease
Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT_1B, HT_1D receptor agonist and a moderately potent 5-HT₇ receptor agonist, with pK_i values of 8.6, 8.4, and 6.7, respectively. Frovatriptan succinate hydrate is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine.

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-P1441

Mambalgin 1	Sodium Channel
Mambalgin 1 is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-P1441A

Mambalgin 1 TFA	Sodium Channel
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-108400

SCH-23390 maleate R-(+)-SCH-23390 maleate	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 maleate also binds with high affinity to the *5-HT₂* and 5-HT_1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

HY-19545A

SCH-23390 hydrochloride R-(+)-SCH-23390 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the *5-HT₂* and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

HY-109112

Brilaroxazine RP5063	Dopamine Receptor 5-HT Receptor	Inflammation/Immunology Neurological Disease
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
HY-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

HY-19373

RWJ-445167 3DP-10017	Thrombin Factor Xa	Cardiovascular Disease
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with K_i of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.

HY-16787

ICA-121431	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 µM).

HY-U00439A

*Protein kinase inhibitors* 1 hydrochloride** (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride	DYRK	Cancer
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2.

HY-W012037

8-Hydroxyquinoline hemisulfate 8-Quinolinol hemisulfate	Bacterial Antibiotic	Infection
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.

HY-135813

LtaS-IN-1	Bacterial	Infection
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.

HY-125957

A-3 hydrochloride	PKA Casein Kinase CaMK PKC	Others
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (K_i=4.3 µM), casein kinase II (K_i=5.1 µM) and myosin light chain kinase (MLCK) (K_i=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with K_i values of 47 µM and 80 µM, respectively.

HY-101918

DS-1040 Tosylate	Others	Cardiovascular Disease
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC₅₀s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

HY-18728

STF-31
GLUT Autophagy Cancer

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].

HY-15583

Auristatin F	Microtubule/Tubulin ADC Cytotoxin	Cancer
Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).

HY-122470

Stampidine	Reverse Transcriptase HIV	Infection
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV_IIIB (B-envelope subtype) and primary clinical isolates with IC₅₀s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC₅₀s of 8.7 nM and 11.2 nM, respectively.

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-11007

GNF-2
Bcr-Abl SARS-CoV Cancer

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

HY-B1510S

Acrivastine D7 BW825C D7	Histamine Receptor	Endocrinology Inflammation/Immunology
Acrivastine D7 (BW825C D7) is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.

HY-P1868A

α2β1 Integrin Ligand Peptide TFA	Integrin	Others
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

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-P1106A

K41498 TFA	CFTR	Cardiovascular Disease
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with K_i values of 0.66 nM, 0.62 nM and 425 nM for human CRF_2α, CRF_2β and CRF₁ receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF_2α- and hCRF_2β-expressing cells. K41498 TFA can be used for hypotension study.

HY-N7247

Thiochrome	mAChR	Metabolic Disease
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.

HY-P1167A

[Orn5]-URP TFA	Urotensin Receptor	Cardiovascular Disease
[Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP TFA displays no agonist activity.

HY-P1167

[Orn5]-URP	Urotensin Receptor	Cardiovascular Disease
[Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC₅₀ of 7.24. [Orn5]-URP displays no agonist activity.

HY-P1335

CTAP	Opioid Receptor	Neurological Disease
CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC₅₀=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).

HY-103407A

PD 168568 dihydrochloride
Dopamine Receptor Neurological Disease

PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a K_i of 8.8 nM.

HY-P1335A

CTAP TFA	Opioid Receptor	Neurological Disease
CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC₅₀=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).

HY-135329

Solifenacin D5 hydrochloride	mAChR	Neurological Disease
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

HY-135588

Raloxifene 6,4'-Bis-β-D-glucuronide	Others	Metabolic Disease
Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis.

HY-129995A

TSHR antagonist S37a	TSH Receptor	Endocrinology
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.

HY-130842

β-Naphthoflavone-CH2-Br β-NF-CH2-Br	Ligand for E3 Ligase	Cancer
β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256).

HY-P1329A

CTOP TFA
Opioid Receptor Neurological Disease

CTOP TFA is a peptide that acts as a μ-opioid receptor antagonist.

HY-14415

SR8278	Others	Metabolic Disease
SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC₅₀ of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.

HY-P1329

CTOP
Opioid Receptor Neurological Disease

CTOP is a peptide that acts as a μ-opioid receptor antagonist.

HY-110303

Xanthine amine congener dihydrochloride XAC dihydrochloride	Adenosine Receptor	Neurological Disease
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC₅₀ values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.

HY-101348

L-741626	Dopamine Receptor	Neurological Disease
L-741626 is a selective D2 dopamine receptor antagonist, with the K_i values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively.

HY-107457

AZD-8529	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-15656S

Ceritinib D7 LDK378 D7	ALK Insulin Receptor IGF-1R	Cancer Endocrinology
Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.

HY-124759

CCR1 antagonist 9
CCR Inflammation/Immunology

CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC₅₀ of 6.8 nM in calcium flux assay.

HY-108495

CYM50308	LPL Receptor	Cardiovascular Disease
CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P₄-R) agonist with an EC₅₀ of 56 nM. CYM50308 displays 37-fold more selective for S1P₄-R than S1P₅-R. CYM50308 has no activity at S1P₁-R, S1P₂-R and S1P₃-R subtypes at concentrations up to 25 μM.

HY-17497S

Acebutolol D7	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Acebutolol D7 is a deuterium labeled Acebutolol. Acebutolol is a selective β1 adrenergic receptor antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

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.

HY-W040146

Propionylpromazine hydrochloride Propiopromazine hydrochloride	Dopamine Receptor	Neurological Disease
Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease.

HY-133045

VHL Ligand 8	Ligand for E3 Ligase	Cancer
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM.

HY-133189

Bis-propargyl-PEG9	PROTAC Linker	Endocrinology
Bis-propargyl-PEG9 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG9 can be used to synthesize the bivalent estrogen receptor ligands.

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-128128

ASN04421891	Others	Neurological Disease
ASN04421891 is a potent GPR17 receptor modulator, with an EC₅₀ of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.

HY-133014

RIP2 kinase inhibitor 1	RIP kinase	Inflammation/Immunology
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC₅₀ of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.

HY-13418A

Dorsomorphin Compound C; BML-275	AMPK TGF-β Receptor Autophagy	Cancer
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (K_i=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.

HY-100658

Didesmethyl cariprazine	5-HT Receptor Dopamine Receptor	Neurological Disease
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D₃ and D₂ receptors, and moderate affinity for the 5-HT_1A receptor.

HY-108258A

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

HY-107457A

AZD-8529 mesylate	mGluR	Neurological Disease
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

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.

HY-N0050

Allomatrine (+)-Allomatrine	Others	Neurological Disease
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.

HY-B0098S

Doxazosin D8 UK 33274 D8	Adrenergic Receptor	Endocrinology Cardiovascular Disease
Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors.

HY-115613

ML-180 SR1848	Others	Cancer
ML-180 (SR1848) is a potent orphan nuclear receptor *liver receptor homolog 1 (LRH-1; NR5A2)* inverse agonist with an IC₅₀ of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC₅₀>10 µM). ML-180 has the potential for LRH-1-dependent cancers.

HY-122872

MKK7-COV-9	p38 MAPK	Cancer
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC₅₀ of 4.98 μM.

HY-P1345A

TLQP-21 TFA	Complement System	Endocrinology Neurological Disease
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca²⁺. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.

HY-P1345

TLQP-21	Complement System	Endocrinology Neurological Disease
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca²⁺. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.

HY-W001909

Myosmine	nAChR	Metabolic Disease
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a K_i of 3300 nM.

HY-14551

Osanetant SR142801	Neurokinin Receptor	Neurological Disease
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.

HY-12206

Thioperamide MR-12842	Histamine Receptor	Neurological Disease
Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [³H]histamine release. Thioperamide inhibits [³H]histamine synthesis with a K_i of 31 nM.

HY-13418

Dorsomorphin dihydrochloride Compound C dihydrochloride; BML-275 dihydrochloride	AMPK TGF-β Receptor Autophagy	Cancer
Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a K_i of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.

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-90010

Tolterodine tartrate Kabi-2234; PNU-200583E	mAChR	Neurological Disease
Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.

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-P1302A

Orphanin FQ(1-11) TFA	Opioid Receptor	Neurological Disease
Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a K_i of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (K_i>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.

HY-13728

Plevitrexed ZD 9331; BGC9331	Thymidylate Synthase	Cancer
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a K_i of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.

HY-P1302

Orphanin FQ(1-11)	Opioid Receptor	Neurological Disease
Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a K_i of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (K_i>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.

HY-N1064

Xanthoplanine	nAChR	Neurological Disease
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2).

HY-N7272

Cirsimarin	Phosphodiesterase (PDE)	Metabolic Disease
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase.

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability.

HY-B1494

Picrotoxinin	Chloride Channel GABA Receptor	Neurological Disease
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABA_A receptor antagonist, which negatively modulates the action of GABA on GABA_A receptors.

HY-135147

ONC206	Dopamine Receptor	Cancer Neurological Disease
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.

HY-10847A

SB-277011 dihydrochloride SB-277011A dihydrochloride	Dopamine Receptor	Neurological Disease
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D₃ receptor antagonist, with pK_is of 8.0, 6.0, <5.2 and 5.9 for D₃, D₂, 5-HT_1B, and 5-HT_1D receptors, respectively.

HY-42849

Sultopride
LIN-1418
Dopamine Receptor Neurological Disease

Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.

HY-130492

ARCC-4	PROTAC Androgen Receptor	Cancer
ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC₅₀ of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.

HY-107380A

PGlu-3-methyl-His-Pro-NH2 TFA A-42872 TFA	Others	Endocrinology
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.

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-106224

Orexin A (human, rat, mouse)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

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.

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-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-110278

ADX71743	mGluR	Neurological Disease
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.

HY-106224A

Orexin A (human, rat, mouse) (TFA)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.

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-P2307

Tat-NR2Baa	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.

HY-70002B

Enzalutamide carboxylic acid MDV3100 carboxylic acid	Drug Metabolite	Cancer
Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.

HY-42849A

Sultopride hydrochloride LIN-1418 hydrochloride	Dopamine Receptor	Neurological Disease
Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

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-P2307A

Tat-NR2Baa TFA	iGluR NO Synthase	Neurological Disease
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.

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-133044

Boc-Pip-alkyne-Ph-COOH	PROTAC Linker	Cancer
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM.

HY-111269

AZD8848	Toll-like Receptor (TLR)	Inflammation/Immunology
AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.

HY-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-76569

Desfesoterodine PNU-200577; 5-Hydroxymethyl Tolterodine	mAChR	Neurological Disease
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a K_B and a pA₂ of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.

HY-100634

4-Hydroxypropranolol hydrochloride (±)-4-hydroxy Propranolol hydrochloride	Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA₂ values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.

HY-108847

Etanercept	TNF Receptor	Inflammation/Immunology
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.

HY-135892

GNE-1858	Others	Inflammation/Immunology
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC₅₀s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.

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-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-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-136181

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

HY-103200

SR59230A hydrochloride	Adrenergic Receptor	Metabolic Disease Cardiovascular Disease
SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

HY-B0649

Propofol 2,6-Diisopropylphenol	GABA Receptor Endogenous Metabolite	Neurological Disease
Propofol potently and directly activates GABA_A receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.

HY-122203

PCS1055 dihydrochloride	mAChR AChE	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively.

HY-100672

SR59230A	Adrenergic Receptor	Metabolic Disease Cardiovascular Disease
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

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-112055

DIM-C-pPhOH	Apoptosis	Cancer
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.

HY-133046

VHL Ligand-Linker Conjugates 17	E3 Ligase Ligand-Linker Conjugate	Cancer
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.

HY-113313

Aldosterone	Endogenous Metabolite	Cardiovascular Disease
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.

HY-133073

CCR7 Ligand 1 CCR7-Cmp2105	CCR Ligand for Target Protein for PROTAC	Cancer
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a K_d of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC₅₀ of 7.3 μM.

HY-16489A

Terodiline hydrochloride	mAChR Calcium Channel	Neurological Disease
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with K_bs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca²⁺ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.

HY-126941

Hecogenin acetate	Opioid Receptor	Neurological Disease
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.

HY-14569

CDPPB	mGluR	Neurological Disease
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC₅₀ of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.

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-19589

JTS-653	TRP Channel	Inflammation/Immunology Neurological Disease
JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.

HY-119486

Tavapadon PF-06649751; CVL-751	Dopamine Receptor	Neurological Disease
Tavapadon (PF-06649751; CVL-751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease.

HY-110237

BX430	P2X Receptor Calcium Channel	Cardiovascular Disease
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC₅₀ of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.

HY-N6932

Voacamine	Cannabinoid Receptor P-glycoprotein	Cancer Metabolic Disease
Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.

HY-108625

SHA 68	Neuropeptide Y Receptor	Neurological Disease
SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC₅₀s of 22.0 and 23.8 nM for NPSR Asn¹⁰⁷ and NPSR Ile¹⁰⁷, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.

HY-15319

AMG 487	CXCR	Cancer Inflammation/Immunology Endocrinology
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively.

HY-N2080

Songorine	GABA Receptor	Cancer
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).

HY-100634S

4-Hydroxypropranolol D7 hydrochloride (±)-4-hydroxy Propranolol D7 hydrochloride	Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA₂ values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.

HY-130992

*Androgen receptor* antagonist 1**	Androgen Receptor Ligand for Target Protein for PROTAC	Cancer
Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC₅₀ of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

HY-116330A

Hyperforin dicyclohexylammonium salt Hyperforin DCHA	TRP Channel Calcium Channel	Neurological Disease
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca²⁺ levels by activating Ca²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.

HY-13965

Parmodulin 2 ML161	Protease-Activated Receptor (PAR)	Cardiovascular Disease
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC₅₀ of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.

HY-B0589C

(3S,5S)-Atorvastatin	Cytochrome P450	Metabolic Disease
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.

HY-15319A

(±)-AMG 487	CXCR	Cancer
(±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC₅₀s of 8.0 and 8.2 nM, respectively.

HY-136561

GRK5-IN-2	Others	Metabolic Disease
GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.

HY-124733

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

HY-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-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-100371

(RS)-MCPG alpha-MCPG	mGluR	Neurological Disease
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.

HY-113962

7α,25-Dihydroxycholesterol 7α,25-OHC	EBI2/GPR183 Endogenous Metabolite	Inflammation/Immunology
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC₅₀=140 pM; K_d=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.

HY-133552

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

HY-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-135303

GLPG1205	GPR84	Inflammation/Immunology
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.

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-P1471

Adrenomedullin (AM) (22-52), human 22-52-Adrenomedullin (human)	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.

HY-P1471A

Adrenomedullin (AM) (22-52), human TFA 22-52-Adrenomedullin (human) (TFA)	CGRP Receptor	Cardiovascular Disease
Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH₂ terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.

HY-N0686

Pseudoprotodioscin	Fatty Acid Synthase (FASN) MicroRNA	Metabolic Disease
Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.

HY-118743

KMN-80	Prostaglandin Receptor	Metabolic Disease
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP₄ receptor with an IC₅₀ and a K_i of 3 nM and 2.35 nM, respectively. KMN-80 is against EP₃ receptor with an IC₅₀ of 1.4 μM and >10 μM for all other prostanoid receptors.

HY-121538

CUDA	Epoxide Hydrolase PPAR	Cardiovascular Disease
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC₅₀s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.

HY-120944

BAY-7598	MMP	Inflammation/Immunology
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC₅₀s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.

HY-135880A

OMDM-4
Endogenous Metabolite Neurological Disease

OMDM-4 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a K_i 17.7 μM.

HY-135882

OMDM-6	TRP Channel Cannabinoid Receptor Endogenous Metabolite	Neurological Disease
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC₅₀=75 nM) and cannabinoid receptor type 1 (CB1) (K_i=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a K_i of 7.0 μM.

HY-111615A

J-2156 TFA	Somatostatin Receptor	Neurological Disease
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.

HY-121557

OMDM-1
Endogenous Metabolite Neurological Disease

OMDM-1 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a K_i of 2.4 μM.

HY-135881

OMDM-5	TRP Channel Endogenous Metabolite	Neurological Disease
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a K_i of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC₅₀ of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (K_i=4.9 μM).

HY-135880

OMDM-3
Endogenous Metabolite Neurological Disease

OMDM-3 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a K_i of 16.6 μM.

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-14886

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

HY-103342

OMDM-2
Endogenous Metabolite Neurological Disease

OMDM-2 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a K_i of 3.0 μM.

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-111615

J-2156	Somatostatin Receptor	Neurological Disease
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.

HY-70053A

Fesoterodine L-mandelate	mAChR	Metabolic Disease Neurological Disease
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).

HY-N0179

Ecdysone α-Ecdysone	Endogenous Metabolite Apoptosis	Metabolic Disease
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).

HY-A0030

Fesoterodine fumarate	mAChR	Metabolic Disease Neurological Disease
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).

HY-70053

Fesoterodine	mAChR	Metabolic Disease Neurological Disease
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pK_i values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB).

HY-110155

LM11A-31 dihydrochloride	Others	Neurological Disease
LM11A-31 dihydrochloride, a non-peptide p75^NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.

HY-110155A

(Rac)-LM11A-31 dihydrochloride	Others	Neurological Disease
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75^NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.

HY-122575

Aurintricarboxylic acid	P2X Receptor Influenza Virus Topoisomerase	Infection Inflammation/Immunology Neurological Disease
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC₅₀s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.

Cat. No.	Product Name	Target	Research Area