Trace Amine-associated Receptor (TAAR)

Trace amine associated-receptors (TAARs) are a class of G protein-coupled receptors that were discovered in 2001. Humans possess six functional isoforms (TAAR1, TAAR2, TAAR5, TAAR6, TAAR8, and TAAR9), whereas some fish species express over 100. It acts as an endogenous receptor for the trace amines. Trace amines are endogenous compounds classically regarded as comprising β-phenylethyalmine, p-tyramine, tryptamine, p-octopamine, and some of their metabolites.

Although all other TAARs serve predominantly or exclusively as chemosensory receptors in the main olfactory system, TAAR 1 has been demonstrated to be a novel modulator of dopaminergic, serotonergic and glutamatergic activity in the brain. And TAAR 1 has been identified as a novel therapeutic target for schizophrenia, depression, and addiction. In the periphery, TAAR1 regulates nutrient-induced hormone secretion, suggesting its potential as a novel therapeutic target for diabetes and obesity. TAAR1 may also regulate immune responses by regulating leukocyte differentiation and activation.

Trace Amine-associated Receptor (TAAR) Related Products (34):

By Effects:	Agonists (24) Antagonist (1) Activators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-110098

Ro 5212773		99.85%
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (K_i=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids.

HY-12700

RO5256390	Agonist	98.75%
RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages.

HY-42346

ZH8651	Agonist	99.71%
ZH8651 is an agonist of TAAR1 which can activate both Gs and Gq signal pathway. ZH8651 can used in study schizophrenia.

HY-108015

RO5263397		99.10%
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC₅₀s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.

HY-147319

RTI-7470-44	Antagonist	99.85%
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD).

HY-183428

LK00764	Agonist
LK00764 is a TAAR1 agonist with an EC₅₀ of 4 nM. LK00764 alleviates Dizocilpine (HY-15084B)-induced hyperlocomotion, reduces vertical locomotor activity, attenuates spontaneous hyperlocomotion in dopamine transporter knockout rats, and inhibits stress-induced hyperthermia in rats. LK00764 can be used for the research of schizophrenia.

HY-117021

RO 5073012	Agonist
RO 5073012 is a selective, orally active and brain-penetrant TAAR1 agonist. RO 5073012 shows a K_i of 6 nM for hTAAR1 and EC₅₀ values of 23 and 25 nM for mTAAR1 and rTAAR1. RO 5073012 can be used for the research of neurological disease, such as schizophrenia.

HY-183489

TAAR1-agonist-4	Agonist
TAAR1-agonist-4 is a TAAR1 agonist and oral hypoglycemic agent with an EC₅₀ of 0.0046 μM for TAAR1. TAAR1-agonist-4 alleviates antipsychotic-related metabolic side effects, improves negative and cognitive symptoms, and reduces drug abuse behaviors. TAAR1-agonist-4 is applicable to research on schizophrenia, acute manic episodes associated with bipolar disorder, and glucose intolerance.

HY-12699

RO5166017	Agonist	98.21%
RO5166017 is an orally active and species-crosses TAAR1 agonist, with K_i values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.

HY-109157

Ralmitaront	Agonist	99.92%
Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC₅₀ value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.

HY-103054

RO5203648		98.10%
RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric research.

HY-135065

3-Iodothyronamine hydrochloride	Activator	99.5%
3-Iodothyronamine (hydrochloride) is an endogenous and rapid-acting derivative of thyroid hormone. 3-Iodothyronamine potently activates an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale. 3-Iodothyronamine can be used for the research of congestive heart failure.

HY-B1421

Ractopamine hydrochloride	Agonist	99.2%
Ractopamine hydrochloride (LY031537) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine hydrochloride also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine hydrochloride promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine hydrochloride can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

HY-W005394

2-Phenylpropan-1-amine hydrochloride		98.96%
2-Phenylpropan-1-amine hydrochloride, a phenethylamine compound, is an agonist of the human trace amine-associated receptor 1 (TAAR1).

HY-160001A

ZH8659 hydrochloride	Activator	99.21%
ZH8659 hydrochloride is a trace amine-associated receptor 1 (TAAR1)-Gq agonist. ZH8659 hydrochloride can be used for the research of neurological disorders.

HY-176141

ZH8965	Agonist	99.48%
ZH8965 is an orally active TAAR1-Gs/Gq agonist (EC₅₀: 6.1/14.8 nM). ZH8965 improves antipsychotic-like phenotypes and cognitive impairment in the MK-801-induced mouse psychosis model. ZH8965 can be used in schizophrenia research.

HY-160001

ZH8659	Activator
ZH8659 is a trace amine-associated receptor 1 (TAAR1) –Gq agonist. ZH8659 can be used for the research of schizophrenia.

HY-W751276

Ractopamine-¹³C₆	Agonist
Ractopamine-¹³C₆ is the ¹³C-labeled Ractopamine (HY-113781). Ractopamine (LY031537 free base) is a potent and orally active β-adrenergic receptor (βAR) agonist with K_d value of ~25 nM for pig β1AR and β2AR. Ractopamine also is a mTAAR1 agonist with an EC₅₀ of 16 μM. Ractopamine promotes muscle mass development, limits fat deposition, reduces feed consumption, increases total cellular protein synthesis, and improves growth rate and feed efficiency in finishing swine. Ractopamine can be used for researching to increase lean tissue growth and improve production efficiency in pigs.

HY-161317

Gαq/11 protein-IN-1	Agonist
Gαq/11 protein-IN-1 (compound F33) is an inhibitor of Gαq/11 protein with an IC₅₀ value of 9.4 μM. Gαq/11 protein-IN-1 has antitumor activity.

HY-157955A

TAAR1 agonist 1 hydrochloride	Agonist
TAAR1 agonist 1 hydrochloride (6e·HCl) is a novel G-protein-coupled receptor TAAR1 agonist. TAAR1 agonist 1 hydrochloride is used in the study of schizophrenia.

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