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5-HT6

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (70) Adrenergic Receptor (8) Apoptosis (5) Autophagy (6) Cholinesterase (ChE) (1) Dopamine Receptor (9) Drug Metabolite (1) Endogenous Metabolite (2) HDAC (1) Histamine Receptor (2) Isotope-Labeled Compounds (1) mAChR (5) Mitophagy (5) Monoamine Oxidase (5) P2X Receptor (1) Parasite (1) Phospholipase (1)
By Research Areas:	Cancer (7) Cardiovascular Disease (2) Neurological Disease (70)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-155116

5-HT6 agonist 1	5-HT Receptor	Neurological Disease
5-HT6 agonist 1 (Compound 19) is a *5-HT6* agonist (K_i: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability .

HY-155316

5-HT6R antagonist 2	Others	Others
5-HT6R antagonist 2 (compound 29) is a 5-HT6 receptor antagonist .

HY-162636

5HT6-ligand-2	5-HT Receptor	Neurological Disease
5HT6-ligand-2 (compound 15) is a potent *5-HT₆* inhibitor with K_i values of 3.4, 15 nM for 5-HT6, SERT, respectively. 5HT6-ligand-2 shows neuroprotection. 5HT6-ligand-2 has the potential for the research of dementia .

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-163150

5-HT6R antagonist 3	5-HT Receptor	Neurological Disease
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant *5-HT6R* antagonist with K_i values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease .

HY-156017

5-HT6R antagonist 1	5-HT Receptor	Cardiovascular Disease Neurological Disease
5-HT6R antagonist 1 (Comopund 8) is a *5-HT6R* antagonist (K_i: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research .

HY-162682

5-HT6R antagonist 4	5-HT Receptor	Neurological Disease
5-HT6R antagonist 4 (compound 30) is a neutral antagonist of *5-HT6R, with the K_i* of 1 nM .

HY-146677

5-HT6R/MAO-B modulator 1	5-HT Receptor Monoamine Oxidase	Neurological Disease
5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of *5-HT₆R* at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits . 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-101622

5-HT6/7 antagonist 1	5-HT Receptor Dopamine Receptor	Neurological Disease
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-145862

5-HT6/5-HT2AR antagonist-1	5-HT Receptor	Neurological Disease
5-HT6/5-HT2AR antagonist-1 is a potent dual *5-HT₆/5-HT_2AR* antagonist with K_i values of 11 nM and 39 nM, respectively .

HY-146076

5-HT6/5-HT2A receptor ligand-1	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research .

HY-146077

5-HT6/5-HT2A receptor ligand-2	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties .

HY-103113

MS 245 oxalate	5-HT Receptor	Neurological Disease
MS 245 oxalate is a potent antagonist of *5-HT₆* receptor with a K_i of 2 nM .

HY-14337

MS 245	5-HT Receptor	Neurological Disease
MS 245 is an antagonist of the *5-HT₆* receptor wih an K_i value of 1.5 nM .

HY-21995

BGC20-761	5-HT Receptor Dopamine Receptor	Neurological Disease
BGC20-761 is a selecvtive *5-HT6* and dopamine receptor antagonist (human receptor K_i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent .

HY-14336

SB 271046	5-HT Receptor	Neurological Disease
SB 271046 is a potent, selective and orally active 5-HT6 receptor antagonist with a pK_i of 8.92-9.09. SB 271046 show >200-fold selective for the 5-HT6 receptor over other receptors, binding sites and ion channels. SB 271046 has anticonvulsant activity .

HY-14340

WAY-181187 1 Publications Verification 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-W746031

WAY-181187 hydrochloride SAX-187 hydrochloride	5-HT Receptor	Neurological Disease
WAY-181187 (SAX-187) hydrochloride 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 . WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .

HY-110366

WAY-181187 oxalate SAX-187 oxalate	5-HT Receptor	Neurological Disease
WAY-181187 (SAX-187) oxalate 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. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .

HY-103110

ST1936 1 Publications Verification	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 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 also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor* .

HY-103110A

ST1936 oxalate	5-HT Receptor Adrenergic 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 (K_i of 300 nM) for human and rat α2 adrenergic receptor* .

HY-119061

SB357134	5-HT Receptor	Neurological Disease
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .

HY-169114

Goxalapladib	5-HT Receptor Phospholipase	Cardiovascular Disease
Goxalapladib is a 5-HT₆ receptor modulator that blocks lipoprotein-associated phospholipase A2 (Lp-PLA2) activity. Goxalapladib is promising for research of atherosclerosis-associated cardiovascular diseases .

HY-14338A

Idalopirdine hydrochloride Lu AE58054 hydrochloride	5-HT Receptor	Neurological Disease
Idalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a K_i value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .

HY-14338

Idalopirdine Lu AE58054	5-HT Receptor	Neurological Disease
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a K_i value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders .

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-14431A

Cerlapirdine hydrochloride SAM-531 hydrochloride; PF-05212365 hydrochloride	5-HT Receptor	Neurological Disease
Cerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease .

HY-14431

Cerlapirdine 1 Publications Verification SAM-531; PF-05212365	5-HT Receptor	Neurological Disease
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease .

HY-103141

SB-258585 hydrochloride	Others	Neurological Disease
SB-258585 is a high affinity ligand for the 5-HT₆ receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT₆ receptors. SB-258585 can be used to label recombinant and natural 5-HT₆ receptor .

HY-118836

GSK215083	5-HT Receptor	Others
GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation .

HY-103099

SB-399885 hydrochloride 1 Publications Verification	5-HT Receptor	Neurological Disease
SB-399885 hydrochloride is a 5-HT₆ receptor antagonist.

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-120239

Ro 63-0563	5-HT Receptor	Neurological Disease
Ro 63-0563 is a potent, competitive and selective *5-HT₆* receptor antagonist with pK_i values ??of 7.83 and 7.91 for rat and human *5-HT₆* receptors, respectively. Ro 63-0563 has no affinity for other receptors .

HY-14335A

Ro 04-6790 di(hydrochloride)	5-HT Receptor	Neurological Disease
Ro 04-6790 dihydrochloride 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 dihydrochloride has no affinity at other receptors .

HY-105896

SB399885	5-HT Receptor	Neurological Disease
SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pK_i values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties .

HY-103098

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

HY-103133

WAY208466 dihydrochloride	5-HT Receptor	Neurological Disease
WAY 208466 dihydrochloride is a potent and selective 5-HT₆ receptor agonist (EC₅₀=7.3 nM for the human 5-HT₆ receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex . WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects .

HY-13052

SB-737050A	5-HT Receptor	Neurological Disease
SB-737050A is a potent *5-HT6* antagonist to prevent relapse into addiction .

HY-122612

SB-258585	5-HT Receptor	Neurological Disease
SB-258585 is a selective ligand with high affinity for the 5-HT₆ receptor, with a pK_i value of 8.53 .

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-14336A

SB 271046 Hydrochloride SB 271046A	5-HT Receptor	Neurological Disease
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC₅₀=0.16 μM) .

HY-115724

FPPQ	5-HT Receptor	Neurological Disease
FPPQ is a dual-acting 5-HT₃ (K_i = 0.9 nM) and 5-HT₆ (K_i = 3 nM) receptor antagonist with antipsychotic and procognitive properties.

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-14339

Intepirdine 2 Publications Verification 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-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-123272

E6801	5-HT Receptor	Neurological Disease
E6801 is a 5-HT6 receptor agonist that improves recognition memory by jointly modulating cholinergic and glutamatergic neurotransmission. E6801 can be used in studies of dementia, depression, obesity, epilepsy, etc .

HY-120464

PF-05212377 SAM-760	5-HT Receptor	Neurological Disease
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .

HY-117046

AVN-101	Others	Neurological Disease
AVN-101 free base is a multi-target drug candidate with the potential to inhibit central nervous system (CNS) diseases. AVN-101 free base exhibits high inhibitory activity on 5-HT7 receptors and also has certain activity on 5-HT6, 5-HT2A and 5-HT2C receptors. Due to its anxiolytic and antidepressant activities, AVN-101 free base is also expected to be used in diseases such as general anxiety disorder, depression, schizophrenia and multiple sclerosis .

HY-101009

Methiothepin maleate Metitepine maleate; Ro-8-6837 maleate	5-HT Receptor	Neurological Disease
Methiothepin maleate 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).

Cat. No.	Product Name	Target	Research Area

HY-110366

WAY-181187 oxalate SAX-187 oxalate	5-HT Receptor	Neurological Disease
WAY-181187 (SAX-187) oxalate 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. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0049

Nuciferine 4 Publications Verification	Structural Classification Alkaloids Aporphine Alkaloids other families Source classification Plants Isoquinoline Alkaloids	Parasite 5-HT Receptor Dopamine Receptor
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-W015169

5-Methoxytryptamine O-Methylserotonin	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Indole Alkaloids Cancer	Drug Metabolite 5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action .

HY-W015169A

5-Methoxytryptamine hydrochloride	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Indole Alkaloids Cancer	5-HT Receptor Endogenous Metabolite
5-Methoxytryptamine hydrochloride, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine hydrochloride has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine hydrochloride is also a potent antioxidant and has radioprotective action .

HY-N0049R

Nuciferine (Standard)	Structural Classification Alkaloids other families Source classification Plants	5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. 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.

Cat. No.	Product Name	Chemical Structure

HY-14541S

Olanzapine-d3
Olanzapine-d₃ is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].

HY-14541S2

Olanzapine-d8

Olanzapine-d8 is a deuterated labeled Olanzapine . Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic .

Cat. No.	Product Name		Classification

HY-146677

5-HT6R/MAO-B modulator 1		Alkynes
5-HT6R/MAO-B modulator 1 (compound 48) is an antagonist of *5-HT₆R* at Gs signaling and an irreversible MAO-B inhibitor. 5-HT6R/MAO-B modulator 1 exhibits glioprotective properties. 5-HT6R/MAO-B modulator 1 can reverse Scopolamine-induced memory deficits . 5-HT6R/MAO-B modulator 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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