Search Result
Results for "
partial
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
34
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-123813
-
|
Arrestin
|
Cancer
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CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .
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-
-
- HY-10019
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CP 526555
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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-
-
- HY-10020
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CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
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Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-10021
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CP 526555-18
|
nAChR
ERK
p38 MAPK
|
Others
Neurological Disease
Cancer
|
Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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-
-
- HY-103418
-
|
Dopamine Receptor
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Neurological Disease
|
Dopamine D2 receptor agonist-3 (compound 3) is a selective D2 receptor
partial agonist and Dopamine D3 receptor antagonist (with pEC50 of 8.3 and <5.5 respectively) .
|
-
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- HY-106206
-
-
-
- HY-107680
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3-Pyr-Cyt
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nAChR
|
Neurological Disease
|
3-Pyr-Cytisine (3-Pyr-Cyt) is a cytisine derivative. 3-Pyr-Cytisine is a very weak α4β2 nAChR partial agonist that has been studied as an antidepressant .
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-
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- HY-19082
-
|
GABA Receptor
|
Neurological Disease
|
Y-23684 is a partial agonist of benzodiazepine receptor (BZR) with anticonvulsant and anxiolytic activities. Y-23684 can be used in the research of treatment of anxiety disorders .
|
-
-
- HY-145698
-
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5-HT Receptor
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Neurological Disease
|
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR .
|
-
-
- HY-110142
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CC4
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nAChR
|
Neurological Disease
|
Thermopsidine (CC4) is a selective partial agonist at α4β2/α6β2 nAChR with EC50 values of 2.2 μM target α4β2 .
|
-
-
- HY-10019A
-
CP 526555 dihydrochloride
|
nAChR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Varenicline (CP 526555-18) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-121249
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SL65.0155
|
5-HT Receptor
|
Neurological Disease
|
Capeserod hydrochloride (SL65.0155) is a 5-HT4(e) receptor partial agonist (Ki=0.6 nM) with potent cognitive enhancing properties. Capeserod hydrochloride acts as a partial agonist in cells expressing 5-HT4(b) and 5-HT4(e) splice variants, stimulating cAMP production with IC50 values ??of 244 and 29 nM, respectively. Capeserod hydrochloride is used in the study of memory impairment and dementia .
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-
-
- HY-103548
-
|
Glucocorticoid Receptor
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Endocrinology
|
GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone .
|
-
-
- HY-10021R
-
|
nAChR
ERK
p38 MAPK
|
Others
Neurological Disease
|
Varenicline (Tartrate) (Standard) is the analytical standard of Varenicline (Tartrate). This product is intended for research and analytical applications. Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-10019S1
-
CP 526555-15N,13C,d2
|
nAChR
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-W062702
-
|
nAChR
|
Neurological Disease
|
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia .
|
-
-
- HY-106964A
-
|
5-HT Receptor
|
Neurological Disease
|
(Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia .
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-
-
- HY-109065
-
|
5-HT Receptor
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Others
|
Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the 5-HT4 receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C) .
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-
-
- HY-59201A
-
|
nAChR
5-HT Receptor
|
Neurological Disease
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
|
-
-
- HY-13479
-
|
HSP
|
Cancer
|
EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases . EC144 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-10019AS1
-
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
|
-
-
- HY-155707
-
|
Others
|
Inflammation/Immunology
|
MOR agonist-3 (Compound 84) is a D3R/MOR antagonist (Ki 382 nM and 55.2 nM respectively). MOR agonist-3 has the potential to produce analgesic effects through MOR (μ-opioid receptor) (HY-149337) partial agonists and to reduce opioid abuse through D3R antagonists. MOR agonist-3 can be used in the treatment of inflammation and neuropathic pain research .
|
-
-
- HY-103476
-
|
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 . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
-
- HY-14417
-
|
mGluR
|
Neurological Disease
|
VU0155041 is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
|
-
-
- HY-14417B
-
|
mGluR
|
Neurological Disease
|
VU0155041 sodium is a potent, selective positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 has potential for the research of Parkinson's disease (PD) .
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-
-
- HY-118097
-
|
PPAR
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Others
|
GW0072 is a partial agonist of PPARγ and does not directly bind to the AF-2 helix of PPARγ, resulting in specific partial receptor transcriptional activation properties .
|
-
-
- HY-Y1176
-
-
-
- HY-U00066
-
-
-
- HY-107480
-
-
-
- HY-114703
-
-
-
- HY-B0982
-
-
-
- HY-B0570
-
-
-
- HY-U00216
-
-
-
- HY-118299
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-
-
- HY-14958
-
-
-
- HY-14958A
-
-
-
- HY-116257
-
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Others
|
Others
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GSK-7227 (compound 32) is a PPARδ partial agonist with the activity of regulating the expression of related genes. GSK-7227 has partial agonist effects on PPARδ target genes CPT1a and PDK4 in skeletal muscle cells.
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-
-
- HY-17622
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-
-
- HY-N0175
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Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
Cancer
|
Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
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-
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- HY-101639
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-
-
- HY-19250
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-
-
- HY-100140
-
-
-
- HY-101639A
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-
-
- HY-117526
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-
-
- HY-116888
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-
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- HY-124225
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-
-
- HY-121393
-
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GABA Receptor
|
Neurological Disease
|
Imidazenil is a partial positive allosteric modulator of GABAA receptors with anxiolytic, antipanic and anticonvulsant activities.
|
-
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- HY-111419
-
|
Serotonin Transporter
5-HT Receptor
|
Neurological Disease
|
DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity .
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-
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- HY-111419A
-
|
Serotonin Transporter
5-HT Receptor
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Neurological Disease
|
DSP-1053, a benzylpiperidine derivative, is a potent serotonin transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity .
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-
-
- HY-101384A
-
|
Dopamine Receptor
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Others
|
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
|
-
- HY-100140A
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PK-8165 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
Pipequaline hydrochloride (PK-8165 hydrochloride) is a partial benzodiazepine receptor agonist with anxiolytic activity .
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- HY-103170
-
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Adenosine Receptor
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Others
|
LUF5834 is a selective A2B adenosine receptor (A2BR) partial agonist (EC50 = 12 nM). LUF5834 is also a partial A1/A2A adenosine receptor agonist (lacking selectivity) with Ki values of 2.6 and 28 nM, respectively .
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- HY-14262
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EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-120418
-
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Others
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Others
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L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
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- HY-16086
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DRF 2593; NN 2344
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PPAR
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Metabolic Disease
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Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
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-
- HY-30006
-
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iGluR
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Neurological Disease
|
1-Aminocyclobutanecarboxylic acid is a NMDA receptor partial agonist acting at the glycine site, NR1 .
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- HY-138809
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-
- HY-B0982R
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LB-46 (Standard)
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
Endocrinology
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Pindolol (Standard) is the analytical standard of Pindolol. This product is intended for research and analytical applications. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).
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- HY-19308
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-
- HY-19919
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EXEL04286652; XL-652; BMS-788
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LXR
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Metabolic Disease
|
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
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- HY-U00215
-
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GABA Receptor
|
Neurological Disease
|
Ro 41-3290 is the desethylated derivative of Ro 41-3696, which is a nonbenzodiazepine partial agonist at the benzodiazepine receptor.
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- HY-102053
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NRX-1074; AGN-241660
|
iGluR
|
Neurological Disease
|
Apimostinel (NRX-1074; AGN-241660) is an orally active NMDA receptor partial agonist .
|
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- HY-116970
-
-
- HY-128040
-
-
- HY-162491
-
-
- HY-101665
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(+)-RP-59037; IP-456; RP-62955
|
GABA Receptor
|
Neurological Disease
|
Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.
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- HY-119277
-
|
Dopamine Receptor
|
Neurological Disease
|
CJB-090 dihydrochloride is a partial agonist with activity at dopamine D3 receptors. CJB-090 exhibits partial agonist characteristics in vitro. CJB-090 elicits yawning responses only in monkeys with an extensive history of cocaine use. CJB-090 reduces the reinstatement effects of cocaine in reinstatement behaviors induced by cocaine .
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- HY-15430A
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EVP-6124 hydrochloride
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nAChR
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Neurological Disease
|
Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
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- HY-B0735
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-
- HY-15430
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EVP-6124
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nAChR
|
Neurological Disease
|
Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
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- HY-146742
-
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PPAR
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Metabolic Disease
|
PPARγ agonist 2 is a potent PPARγ partial agonist and can be used for metabolic disease research .
|
-
- HY-118259
-
-
- HY-N0175R
-
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nAChR
|
Metabolic Disease
Cancer
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Cytisinicline (Standard) is the analytical standard of Cytisinicline. This product is intended for research and analytical applications. Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs , and partial to full agonist at β4 containing receptors and α7 receptors . Has been used medically to help with smoking cessation .
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- HY-14261
-
-
- HY-112152
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-
- HY-113681
-
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- HY-118987
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- HY-14831
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MBX 102; JNJ 39659100
|
PPAR
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Metabolic Disease
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Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
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- HY-14953
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AWD 131-138
|
GABA Receptor
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Neurological Disease
|
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
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- HY-16728
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GLYX-13
|
iGluR
|
Neurological Disease
|
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
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- HY-101586
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-
- HY-W001692
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DOV 273547
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GABA Receptor
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Neurological Disease
|
Ocinaplon (DOV 273547) is a partial GABAA receptor positive allosteric modulator with relatively high efficacy at the α1 subunit .
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- HY-154924
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-
- HY-107744
-
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Opioid Receptor
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Neurological Disease
|
Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .
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- HY-120633A
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-
- HY-106917
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Ro 41-3696
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GABA Receptor
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Neurological Disease
|
Lirequinil (Ro 41-3696) is an orally active partial agonist of the benzodiazepine (BDZ) receptor. Lirequinil has the effect of promoting sleep .
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- HY-B1485
-
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Opioid Receptor
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Neurological Disease
|
Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .
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- HY-B0982S
-
-
- HY-14262R
-
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5-HT Receptor
Serotonin Transporter
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Neurological Disease
|
Vilazodone (Standard) is the analytical standard of Vilazodone. This product is intended for research and analytical applications. Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-10629
-
LXR-623
Maximum Cited Publications
9 Publications Verification
WAY 252623
|
LXR
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Metabolic Disease
Cancer
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LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
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- HY-N1951
-
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GABA Receptor
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Neurological Disease
|
Miltirone is a natural compound present in the root of Salvia miltiorrhiza. Miltirone is a central benzodiazepine receptor partial agonist, with an IC50 of 0.3 μM .
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- HY-103108
-
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5-HT Receptor
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Metabolic Disease
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CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect .
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- HY-Y1176S
-
-
- HY-N11464
-
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Others
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Others
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Kuwanon O is a flavonoid derivative with a fused dihydrochalcone partial moiety, that can be isolated from the root bark of Morus lhou (set.) Koidz .
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- HY-125043
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-
- HY-153264
-
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Others
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Others
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TAS2R14 agonist is a potent TAS2R14 partial agonist with an EC50 of 116.6 ±23.6 nM .
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- HY-Y0850O
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PVA (Mw 31000-50000, 87-89% hydrolyzed); Poly(Ethenol) (Mw 31000-50000, 87-89% hydrolyzed)
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Biochemical Assay Reagents
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Others
Cancer
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Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) is a synthetic polymer derived from polyvinyl acetate through partial or complete hydroxylation .
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- HY-129507
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DAB-452 fumarate
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Dopamine Receptor
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Neurological Disease
|
Aplindore fumarate (DAB-452 fumarate) is a dopamine D2 receptor partial agonist. Aplindore fumarate could be used in studies of Parkinson's disease and schizophrenia .
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- HY-121740
-
-
- HY-162851
-
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Adenosine Receptor
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Others
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Adenosine receptor agonist 1 (compound 6m) is an A3 adenosine receptor (AR) partial agonist with Ki value of 6.7 nM .
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- HY-16728B
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GLYX-13 Trifluoroacetate
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iGluR
|
Neurological Disease
|
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.
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- HY-101869
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MRK-409
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GABA Receptor
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Neurological Disease
|
MK0343 (MRK-409) is an orally bioavailable GABAA receptor subtype-selective partial agonist. MK0343 is a non-sedating anxiolytic .
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-
- HY-N8505
-
8,10-Diphenyllobelidione
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Others
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Others
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Lobelanine (8,10-Diphenyllobelidione) is a chemical precursor for the biosynthesis of Lobeline. Lobeline is a partial nicotinic agonist and is used as a smoking cessation agent .
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-
- HY-100908
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N10-Acetyltryptamine; Nb-Acetyltryptamine; Nω-Acetyltryptamine
|
Melatonin Receptor
|
Neurological Disease
|
N-Acetyltryptamine is a partial agonist for melatonin receptors in the retina . N-Acetyltryptamine is also used for determination of serotonin N-acetyl transferase activity .
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- HY-11053
-
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nAChR
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Neurological Disease
|
S 24795 is a partial agonist of α7 nAChR and improves mnemonic function in aged mice for the research of aging-related memory disturbances .
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-
- HY-103417
-
-
- HY-167865
-
-
- HY-119060
-
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mGluR
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Neurological Disease
|
FP0429 is a full mGlu4 agonist and partial mGlu8 agonist with EC50 values of 48.3 μM and 56.2 μM, respectively .
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-
- HY-107480R
-
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Androgen Receptor
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Metabolic Disease
|
YK11 (Standard) is the analytical standard of YK11. This product is intended for research and analytical applications. YK11 is a partial agonist of androgen receptor, with osteogenic activity.
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- HY-109136
-
BAY 1101042
|
Guanylate Cyclase
|
Cardiovascular Disease
|
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists .
|
-
- HY-109164
-
AGN-241751; GATE-251
|
iGluR
|
Neurological Disease
|
Zelquistinel (AGN-241751) is a N-methyl-D-aspartate (NMDA) receptor partial agonist used for the research of depression, anxiety and other related psychiatric disorders .
|
-
- HY-108569
-
|
Antibiotic
Bacterial
PPAR
|
Infection
|
nTZDpa is an antibiotic. nTZDpa is a PPARG partial agonist. nTZDpa has antibacterial activity. nTZDpa is effective against growing and persistent Staphylococcus aureus by lipid bilayer disruption .
|
-
- HY-125374A
-
XRP9881 dihydrate
|
Others
|
Cancer
|
Larotaxel (dihydrate) (XRP9881 (dihydrate)), a new taxane compound prepared by partial synthesis from 10-deacetyl baccatin III, is active against tumors .
|
-
- HY-123127
-
-
- HY-126057
-
|
Parasite
5-HT Receptor
|
Infection
|
(R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer .
|
-
- HY-169140
-
WY-47846
|
5-HT Receptor
|
Neurological Disease
|
Zalospirone (WY-47846) is a novel cyclic imide with 5-HT1A partial agonist activity. Zalospirone shows antidepressant efficacy .
|
-
- HY-16729
-
YKP10811
|
5-HT Receptor
|
Metabolic Disease
|
Relenopride is a agonist of novel potent 5-HT4 receptor partial with weak binding to 5-HT 2B receptors (Ki = 31 nM) .
|
-
- HY-U00443
-
|
5-HT Receptor
|
Neurological Disease
Cancer
|
SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
|
-
- HY-103123
-
|
5-HT Receptor
|
Neurological Disease
Cancer
|
SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases .
|
-
- HY-122235
-
-
- HY-14417A
-
|
mGluR
|
Neurological Disease
|
(1R,2S)-VU0155041, Cis regioisomer of VU0155041, is a partial mGluR4 agonist with an EC50 of 2.35 μM.
|
-
- HY-106851
-
FG 10571; PNU 78875
|
GABA Receptor
|
Neurological Disease
|
Panadiplon (FG 10571; PNU 78875), a benzodiazepine receptor, is a 5GABAA partial agonist. Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors .
|
-
- HY-120456
-
|
Opioid Receptor
|
Neurological Disease
|
SR16835 has high affinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
|
-
- HY-155099
-
-
- HY-Z4690
-
-
- HY-13008
-
MK-0354
1 Publications Verification
|
GPR109A
|
Cardiovascular Disease
|
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
|
-
- HY-U00183
-
-
- HY-100322
-
|
Chloride Channel
|
Cardiovascular Disease
|
H100 is a Cl - transport inhibitor, with partial effects against both the NaK2Cl cotransporter and the Band 3 anion exchanger, but no effect against KCl cotransporter, in human erythrocytes.
|
-
- HY-14261S
-
-
- HY-106432A
-
SB-202026 hydrochloride; Memric hydrochloride
|
mAChR
|
Neurological Disease
|
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research .
|
-
- HY-122208
-
|
Others
|
Inflammation/Immunology
|
SGA360 suppress inflammatory SAA1 signaling in an AHR-dependent manner through a mechanism that does not require AHR binding to its cognate response element (partial antagonist) .
|
-
- HY-106432
-
SB-202026; Memric
|
mAChR
|
Neurological Disease
|
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research .
|
-
- HY-141495A
-
(-)-PW0464
|
Dopamine Receptor
|
Neurological Disease
|
Razpipadon ((-)-PW0464), an aromatic compound, is a dopamine receptor partial agonist. Razpipadon can be used in the study of dopamine D1 ligand-mediated related psychiatric disorders .
|
-
- HY-141551
-
|
Estrogen Receptor/ERR
|
Cancer
|
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
|
-
- HY-121542
-
|
PPAR
|
Metabolic Disease
|
PPARδ agonist 10 (compound 7) is an orally active, selective, and partial agonist of PPARδ, with EC50 values of 0.053 μM and 0.30 µM for hPPARδ(LBD)-GAL4 and mPPARδ, respectively. PPARδ agonist 10 is a partial PPARδ agonist in transactivation assay but a full agonist on free fatty acids (FFA) oxidation in muscle cells both in vitro and in vivo. PPARδ agonist 10 can be used for dyslipidemia research .
|
-
- HY-137055
-
|
Others
|
Others
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-19650
-
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-106025
-
AC-3933
|
GABA Receptor
|
Neurological Disease
|
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively .
|
-
- HY-P2625
-
|
GCGR
|
Metabolic Disease
|
GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM) .
|
-
- HY-103054
-
|
Others
|
Neurological Disease
|
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-111985
-
BAY Vq 7813
|
5-HT Receptor
Adenylate Cyclase
|
Others
|
Revospirone (BAY Vq 7813) is a partial agonist of the 5-HT1A receptor with a Ki of 2 nmol/L. Revospirone inhibits adenylate cyclase activity with an IC50 of 124 nmol/L .
|
-
- HY-114706
-
MDL-26479
|
GABA Receptor
|
Neurological Disease
|
Suritozole (MGL-26479) is a cognitive enhancer that acts as a partial inverse agonist of benzodiazepine receptor sites on GABAA ion channel complexes. Suritozole can be used in the study of neurodegenerative diseases .
|
-
- HY-100271
-
|
TSH Receptor
|
Endocrinology
|
Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.
|
-
- HY-109654
-
|
Reactive Oxygen Species
|
Metabolic Disease
|
Ensulizole is a sulfonated UV absorber and can intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation .
|
-
- HY-105124A
-
Ro 3-4787 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-P5535
-
OCE-205
|
Vasopressin Receptor
|
Inflammation/Immunology
|
Invopressin (Compound 42) is a vasopressin V1A receptor partial agonist (EC50: 1.0 nM). Invopressin can be used for research of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites .
|
-
- HY-155206
-
|
5-HT Receptor
|
Neurological Disease
|
(+)-OSU6162 is an stabilizer on dopaminergic and serotonergic brain signaling. (+)-OSU6162 is a partial agonist of 5-HT2A receptor. (+)-OSU6162 can be used for neurological research .
|
-
- HY-107671
-
|
nAChR
|
Neurological Disease
|
DMAB-anabaseine dihydrochloride is a selective nicotinic α7 receptor partial agonist and an α4β2 nAChR antagonist. DMAB-anabaseine dihydrochloride shows cognition-enhancing effects .
|
-
- HY-120609
-
|
nAChR
|
Neurological Disease
|
BMS-902483 is a quinuclidine-containing spirooxazolidine that is a partial agonist of the α7 nicotinic acetylcholine receptor (nAChR). BMS-902483 improves cognitive ability in preclinical rodent models. .
|
-
- HY-163916
-
|
Opioid Receptor
|
Neurological Disease
|
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .
|
-
- HY-14546
-
OPC-14597
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
|
-
- HY-14546A
-
OPC-14597 monohydrate
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19 .
|
-
- HY-101393A
-
(±)-CGP 12177 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery .
|
-
- HY-110241
-
|
nAChR
|
Neurological Disease
|
Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of agents that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner .
|
-
- HY-106234
-
-
- HY-14261R
-
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
Vilazodone (Hydrochloride) (Standard) is the analytical standard of Vilazodone (Hydrochloride). This product is intended for research and analytical applications. Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
|
-
- HY-U00448
-
|
Others
|
Cancer
|
ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
|
-
- HY-105124
-
-
- HY-156972
-
|
Opioid Receptor
|
Metabolic Disease
|
NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats .
|
-
- HY-P3563
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC50 of 1.5 nM .
|
-
- HY-P5358
-
|
Protease Activated Receptor (PAR)
|
Others
|
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
|
-
- HY-P10325
-
-
- HY-13696
-
-
- HY-115494
-
Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
|
-
- HY-123353
-
Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
|
Cardiovascular Disease
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
|
-
- HY-15293
-
K201
|
Calcium Channel
|
Cardiovascular Disease
|
JTV-519 (K201) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties .
|
-
- HY-107527
-
|
GlyT
|
Neurological Disease
|
Org 25543 hydrochloride is a selective and irreversible GlyT2 inhibitor (IC50: 16 nM). Org 25543 hydrochloride has analgesia effect. Org 25543 hydrochloride ameliorates mechanical allodynia after partial sciatic nerve ligation injury in mice .
|
-
- HY-125717
-
|
mGluR
|
Neurological Disease
|
VU0029251 is a mGluR5 partial antagonist (Ki: 1.07 μM). VU0029251 inhibits glutamate induced calcium mobilization in HEK293 cell membranes expressing rat mGluR5 (IC50: 1.7 μM) .
|
-
- HY-114871
-
|
GABA Receptor
|
Neurological Disease
|
SL651498 is a full agonist of α2 and α3 GABAA receptors, and a partial agonist of α1 and α5 GABAA receptors. SL651498 shows anxiolytic and anticonvulsant activities .
|
-
- HY-116507
-
|
nAChR
|
Neurological Disease
|
AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
|
-
- HY-B0489A
-
-
- HY-N2364
-
-
- HY-14546R
-
OPC-14597 (Standard)
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
|
-
- HY-P7060
-
TPPT
|
iGluR
|
Neurological Disease
|
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
|
-
- HY-119486
-
PF-06649751; CVL-751
|
Dopamine Receptor
|
Neurological Disease
|
Tavapadon (PF-06649751) 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-N7687
-
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation .
|
-
- HY-100976
-
-
- HY-103403
-
PNU96391 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability .
|
-
- HY-B0030
-
|
iGluR
Bacterial
Antibiotic
|
Infection
Neurological Disease
Cancer
|
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
|
-
- HY-15293B
-
K201 hemifumarate
|
Calcium Channel
|
Cardiovascular Disease
|
JTV-519 hemifumarate (K201 hemifumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties .
|
-
- HY-126057S
-
|
Parasite
5-HT Receptor
|
Infection
|
(R)-Praziquantel-d11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].
|
-
- HY-B2078A
-
|
Neurokinin Receptor
|
Inflammation/Immunology
|
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen .
|
-
- HY-P1294
-
|
CRFR
|
Neurological Disease
|
α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-103509
-
|
GABA Receptor
|
Neurological Disease
|
NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
|
-
- HY-P1123
-
|
ATP Citrate Lyase
Free Fatty Acid Receptor
|
Metabolic Disease
|
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120 .
|
-
- HY-115766
-
|
nAChR
|
Neurological Disease
|
Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
|
-
- HY-121541
-
|
Cannabinoid Receptor
|
Cancer
|
CB-25 is a ligand of CB1 cannabinoid receptors, acting as a partial agonist. CB-25 enhances Forskolin (HY-15371)-induced cAMP formation in cancer cells but not hCB1-CHO cells .
|
-
- HY-131651
-
LTB4 ethanolamide
|
Endogenous Metabolite
Leukotriene Receptor
|
Cancer
|
Leukotriene B4 ethanolamide (LTB4 ethanolamide) is an antagonist and a partial agonist for Leukotriene B4 (LTB4) receptor 1 (BLTR1). Leukotriene B4 ethanolamide ameliorates the tumor progression, which is only asscociated with inflammation .
|
-
- HY-B0489
-
methyl 1,2,5,6-tetrahydro-1-methyl-3-pyridinecarboxylate hydrobromide
|
mAChR
nAChR
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
|
-
- HY-15293A
-
K201 free base
|
Calcium Channel
|
Cardiovascular Disease
|
JTV-519 free base (K201 free base) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. Antiarrhythmic and cardioprotective properties .
|
-
- HY-107688A
-
|
nAChR
|
Neurological Disease
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- HY-P1294A
-
|
CRFR
|
Neurological Disease
|
α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-111616
-
|
PPAR
Angiotensin Receptor
|
Cardiovascular Disease
Others
|
GSK1820795A, as a telmisartan analog, is a selective hGPR132a antagonist. GSK1820795A blocks activation of yeast cells expressing hGPR132a by N-acylamides . GSK1820795A is also a angiotensin II antagonists and partial PPARγ agonists (compound 38) .
|
-
- HY-107688
-
|
nAChR
|
Neurological Disease
|
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
|
-
- HY-110312
-
K201 fumarate
|
Calcium Channel
Others
|
Cardiovascular Disease
|
JTV-519 fumarate (K201 fumarate) is a Ca 2+-dependent blocker of sarcoplasmic reticulum Ca 2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle. JTV-519 fumarate is a cardioprotective agent with antiarrhythmic effects .
|
-
- HY-P10377
-
|
Neuropeptide FF Receptor
|
Metabolic Disease
|
GUB03385 is a long-acting PrRP31 analogue. GUB03385 is a potent dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM). GUB03385 has anti-obesity effect .
|
-
- HY-158012
-
|
γ-secretase
|
Others
|
LY3056480 is a gamma-secretase inhibitor (GSI) that inhibits Notch signaling. LY3056480 improves mild to moderate sensorineural hearing loss and is safe and tolerable. Intratympanic administration of LY3056480 induces hair cell regeneration and partial hearing recovery in mammals .
|
-
- HY-167648
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
PD 158771 is an antipsychotic agent that functions as a partial agonist for D2 /D3 receptors (Ki = 42.0/13.7 nM) and as an agonist for 5-HT1A receptors (Ki = 2.6 nM). PD 158771 can be utilized in antipsychotic research .
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- HY-12023
-
GTx-007
3 Publications Verification
S-4
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Androgen Receptor
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Cancer
|
GTx-007 (S-4) is an orally active and selective nonsteroidal androgen receptor (AR) modulator (SARM) and a partial agonist, with Ki of 4 nM. GTx-007 (S-4) is identified as SARMs with potent and tissue-selective in vivo pharmacological activity .
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- HY-14558
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SM-3997
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5-HT Receptor
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Neurological Disease
|
Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .
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- HY-100488
-
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Cannabinoid Receptor
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Cancer
|
Bay 59-3074 is a selective cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. Bay 59-3074 has analgesic properties .
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- HY-145425
-
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IRE1
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Cancer
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PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing .
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- HY-110053
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SM-3997 hydrochloride
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5-HT Receptor
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Neurological Disease
|
Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone hydrochloride has anxiolytic and antidepressant activities. Tandospirone hydrochloride can be used for the research of the central nervous system disorders and the underlying mechanisms .
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- HY-100606
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(-)-Pindolol; (S)-(-)-Pindolol; S-Pindolol
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5-HT Receptor
Adrenergic Receptor
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Neurological Disease
|
l-Pindolol ((-)-pindolol) is a reversible, competitive and orally active 5-HT1A/1B antagonist. l-Pindolol is a partial β-adrenoceptor agonist. l-Pindolol can be used for the research of neurological disease .
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- HY-106316
-
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GABA Receptor
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Neurological Disease
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CGS 20625 is a potent, selective and orally active partial agonist for the central benzodiazepine receptor. CGS 20625 inhibits [3H]-flunitrazepam binding to central benzodiazepine receptors with an IC50 of 1.3 nM. CGS 20625 can be used for the research of pentylenetetrazol-induced seizures .
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- HY-121964
-
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iGluR
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Neurological Disease
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Cis-piperidine-2,3-dicarboxylic acid is a non-specific antagonist of NMDA, AMPA and kainate ionotropic receptors and a partial agonist for NMDA receptors. Cis-piperidine-2,3-dicarboxylic acid can be used in blocking general excitatory synaptic transmissions .
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- HY-112658
-
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Adrenergic Receptor
Adenosine Receptor
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Endocrinology
|
p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
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- HY-131037
-
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Dynamin
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Cancer
|
MB-0223 is a potent and selective dynamin-related GTPase Drp1 partial inhibitor (IC50=1.3 μM) over other dynamin family members, Opa 1 and dynamin-1 (IC50>100 μM) .
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- HY-101708
-
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Others
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Neurological Disease
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N-[(1R)-4-[(Aminoiminomethyl)amino]-1-[[[(1R)-1-(4-hydroxyphenyl)ethyl]amino]carbonyl]butyl]-α-phenylbenzeneacetamide is an anticonvulsant agent with potential for the treatment of generalized tonic-clonic and partial seizures.
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- HY-151203
-
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PKG
|
Cardiovascular Disease
|
PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research .
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- HY-P99794
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BAY 1213790
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Factor Xa
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Cardiovascular Disease
|
Osocimab (BAY 1213790), an anti-FXIa antibody (Ki=2.4 nM; EC50=0.2 nM). FXI inhibition may reduce the risk of thrombosis. Osocimab inhibits thrombin generation, and prolongs activated partial thromboplastin time. Osocimab exhibits anticoagulant effects .
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- HY-108565
-
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Adenylate Cyclase
Prostaglandin Receptor
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Cardiovascular Disease
|
BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor .
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- HY-109654R
-
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Reactive Oxygen Species
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Metabolic Disease
|
Ensulizole (Standard) is the analytical standard of Ensulizole. This product is intended for research and analytical applications. Ensulizole is a sulfonated UV absorber and can intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation .
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- HY-119069
-
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Dopamine Receptor
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Neurological Disease
|
FAUC 3019 is a partial agonist of dopamine D(4) receptors and has the activity of promoting penile erection. FAUC 3019 has a strong stimulatory effect on penile erection in male rats at low concentrations. The biological activity of FAUC 3019 makes it a promising compound candidate .
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- HY-106437
-
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GABA Receptor
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Neurological Disease
|
ELB-139 is a progesterone analogue. ELB-139 is a GABAA receptor partial agonist. ELB-139 has anxiolytic and anticonvulsant activity. ELB-139 induces increase of extracellular 5-HT in the striatum and the medial prefrontal cortex of rats .
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- HY-15056
-
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TRP Channel
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Inflammation/Immunology
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AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted .
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- HY-14546S1
-
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- HY-12752
-
Trimeprazine
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Histamine Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
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Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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- HY-15831
-
-
- HY-120669
-
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Sodium Channel
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Metabolic Disease
|
PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 μM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively .
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- HY-148247
-
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Free Fatty Acid Receptor
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Metabolic Disease
|
BI-2081 is a GPR40 (FFAR1) partial agonist (EC50: 4 nM). BI-2081 induces glucose depending insulin secretion and reduces the plasma glucose concentration. BI-2081 can be used in the research of metabolic diseases, in particular diabetes type 2 .
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- HY-P99321
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BMS 224819; Chi220; Anti-Human CD40 Recombinant Antibody
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TNF Receptor
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Inflammation/Immunology
Cancer
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Teneliximab (BMS-224819) is a chimeric monoclonal antibody, blocks the CD40-CD40L interaction. Teneliximab (BMS-224819) has partial agonist activity resulting in some signaling through CD40 and peripheral B cell depletion .
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- HY-154829A
-
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Neuropeptide FF Receptor
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Inflammation/Immunology
|
AC-099 hydrochloride (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 hydrochloride attenuates spinal nerve ligation-induced hypersensitivity in rats .
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- HY-154829
-
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Neuropeptide FF Receptor
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Inflammation/Immunology
|
AC-099 (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 attenuates spinal nerve ligation-induced hypersensitivity in rats .
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- HY-137350
-
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Leukotriene Receptor
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Inflammation/Immunology
|
12-epi-LTB4 is an agonist for BLT1 and BLT2. 12-epi LTB4 exhibits a partial agonistic activity against mBLT1 and mBLT2, and induces phosphorylation of extracellular signal-regulated kinase in primary mouse keratinocytes .
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- HY-123335
-
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Somatostatin Receptor
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Others
|
L-796,778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796,778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM .
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- HY-122681
-
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Opioid Receptor
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Neurological Disease
|
SR-16435 is a nociceptin/orphanin FQ (NOP)/μ-opioid receptor partial agonist, with high binding affinity (NOP receptor Ki=7.49; μ-Opioid receptor Ki=2.70). SR-16435 can relieve pain .
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- HY-112071A
-
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Adrenergic Receptor
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Endocrinology
|
Prenalterol hydrochloride is a partial adrenal agonist with functional β1-receptor specificity and positive inotropic effects. Prenalterol hydrochloride is effective in suppressing acute heart failure, low output syndrome after myocardial infarction, shock, and reducing orthostatic hypotension in Shy-Drager syndrome .
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- HY-121053A
-
WY-50324 hydrochloride; SEB-324 hydrochloride
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5-HT Receptor
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Neurological Disease
|
Adatanserin hydrochloride is a high affinity, selective and partial agonist for the 5-HT1A receptor with a Ki of 1 nM. Adatanserin hydrochloride is a moderate affinity 5-HT2 receptor antagonist with a Ki of 73 nM. Adatanserin hydrochloride shows significant anxiolytic and antidepressant activity in an animal conflict model .
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- HY-P1316
-
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Opioid Receptor
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Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
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- HY-P1316A
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
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- HY-120879
-
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Dopamine Receptor
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Neurological Disease
|
PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay .
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- HY-138879
-
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nAChR
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Neurological Disease
|
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties .
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- HY-116565
-
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease .
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- HY-121736
-
AGI-026
|
Isocitrate Dehydrogenase (IDH)
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Neurological Disease
|
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
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- HY-151811
-
|
Opioid Receptor
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Neurological Disease
|
NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
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- HY-106056
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D 16726
|
Others
|
Cancer
|
Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
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-
- HY-131821
-
Thymidine-5'-O-monophosphorothioate
|
P2Y Receptor
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Others
|
5'-TMPS (Thymidine-5'-O-monophosphorothioate) is a selective partial agonist of P2Y6R and an antagonist of P2Y14R. Additionally, 5'-TMPS acts as a positive regulator of angiogenesis, exhibiting pro-angiogenic effects
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- HY-107803
-
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Estrogen Receptor/ERR
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Neurological Disease
|
Geranium oil serves as a partial agonist for estrogen receptor (ER), enhancing both the cytotoxicity induced by Tamoxifen (TMX) (HY-13757A) in GT1-7 cells and the adverse effects of TMX on the central nervous system. Geranium oil can be utilized in the research of neurological disorders such as dementia .
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- HY-10020S
-
CP 526555-15N3 Hydrochloride
|
nAChR
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
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- HY-106660
-
|
Dopamine Receptor
|
Neurological Disease
|
BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
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- HY-114085
-
|
Dopamine Receptor
|
Neurological Disease
|
BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
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- HY-143239
-
|
PPAR
|
Metabolic Disease
|
PPARα/γ agonist 1 (compound 5b) is a potent and dual PPARα/γ partial agonist with EC50 values of 28 nM and 69 nM for PPARα and PPARγ, respectively. PPARα/γ agonist 1 is a promising prototype for dyslipidemia and diabetes research .
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-
- HY-19490A
-
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
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- HY-W329175
-
SKF-104557
|
Dopamine Receptor
|
Neurological Disease
|
N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at human D2 and D3 receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor .
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- HY-162827
-
|
RAR/RXR
Apoptosis
|
Cancer
|
RAR/RXR agonist-1 (compound 7) is a chlorinated retinoic acid isomer, a selective RARα agonist and a partial RXRα agonist. RAR/RXR agonist-1 can activate RXRα and induce G2/M arrest and apoptosis in cancer cells .
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- HY-169116
-
|
Dopamine Receptor
|
Neurological Disease
|
D5R agonist 1 (Compound 5j) is a selective, orally active and BBB penetrable D5R partial agonist (EC50: 269.7 nM). D5R agonist 1 enhances the cognition in the Scopolamine (HY-N0296)-induced amnesia model .
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- HY-B0032
-
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-HT1A receptor with an IC50 of 6.75 nM.
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- HY-17401
-
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor .
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- HY-P0227
-
|
Melanocortin Receptor
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Metabolic Disease
|
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
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- HY-B0032A
-
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-HT1A receptor with an IC50 of 6.75 nM.
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-
- HY-117290
-
|
Factor Xa
|
Cardiovascular Disease
|
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .
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- HY-114978
-
|
mGluR
PERK
|
Neurological Disease
|
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
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- HY-121053
-
WY-50324; SEB-324
|
5-HT Receptor
|
Neurological Disease
|
Adatanserin (WY-50324) is a high affinity, selective and partial agonist for the 5-HT1A receptor with a Ki of 1 nM. Adatanserin is a moderate affinity 5-HT2 receptor antagonist with a Ki of 73 nM. Adatanserin shows significant anxiolytic and antidepressant activity in an animal conflict model .
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- HY-162728
-
|
Opioid Receptor
|
Neurological Disease
|
RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC50 value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .
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- HY-107743
-
NalBzoH
|
Opioid Receptor
|
Neurological Disease
|
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect .
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- HY-B0061
-
SM-3997 citrate
|
5-HT Receptor
|
Neurological Disease
|
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
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- HY-P3343A
-
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Estrogen Receptor/ERR
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Cancer
|
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells .
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- HY-116565A
-
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease .
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- HY-149481
-
|
Dopamine Receptor
|
Neurological Disease
|
D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders .
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- HY-107556
-
|
Histamine Receptor
|
Neurological Disease
|
VUF 5681 dihydrobromide is a neutral antagonist of histamine H3 receptor. VUF 5681 dihydrobromide also has partial agonist function of H3 receptor. VUF 5681 dihydrobromide blocks the effects of Thioperamide (HY-12206). VUF 5681 dihydrobromide is used in central nervous system disease research .
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- HY-18138
-
|
5-HT Receptor
|
Neurological Disease
|
PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .
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- HY-117799
-
|
5-HT Receptor
|
Endocrinology
|
LY426965 is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
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- HY-120223
-
|
Adrenergic Receptor
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Metabolic Disease
|
BMS-196085 is an orally active, potent and selective full agonist against human β3 adrenergic receptor with a Ki value of 21 nM. BMS-196085 also has partial agonist activity at the β1 receptor. BMS-196085 is promising for research of obesity and type-II diabetes .
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- HY-116445
-
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Dopamine Receptor
Others
|
Neurological Disease
|
UNC9975 is a D2R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research .
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-
- HY-108057
-
RG3487 free base
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
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-
- HY-168629
-
|
FXR
|
Metabolic Disease
|
FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD + CCl4-(HY-Y0298) induced metabolic dysfunction-associated steatohepatitis mice .
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-
- HY-B0280
-
CVT 303; RS 43285-003
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
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- HY-10559
-
APD125
|
5-HT Receptor
|
Neurological Disease
Cancer
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
- HY-128855
-
|
mAChR
|
Neurological Disease
|
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine 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-N6869
-
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-B1264
-
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-103524
-
(-)-Valerenic Acid
|
GABA Receptor
5-HT Receptor
|
Neurological Disease
|
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
|
-
- HY-144289
-
|
Glucokinase
|
Metabolic Disease
|
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
|
-
- HY-14153AS
-
SDZ-HTF-919-13C,d3; HTF-919-13C,d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
|
-
- HY-119873
-
REV 5320
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-B0030R
-
|
iGluR
Bacterial
Antibiotic
|
Infection
Neurological Disease
Cancer
|
D-Cycloserine (Standard) is the analytical standard of D-Cycloserine. This product is intended for research and analytical applications. D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
|
-
- HY-155706
-
|
Opioid Receptor
Dopamine Receptor
|
Inflammation/Immunology
|
MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
|
-
- HY-158183
-
|
Chloride Channel
|
Others
|
NMD670 is an orally active partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. NMD670 increases muscle excitability in response to movement commands, enhances neuromuscular transmission, restores muscle function and improves muscle mobility. NMD670 has a favorable safety profile and improves muscle function in rats in a MG rat model .
|
-
- HY-135432
-
APD334 arginine
|
LPL Receptor
|
Inflammation/Immunology
|
Etrasimod arginine is an orally available S1P receptor modulator that is a potent full agonist of the S1P1 receptor and has partial agonist activity at S1P4. Etrasimod arginine reduces inflammation in a CD4 +CD45RB high T cell-transferred mouse colitis model .
|
-
- HY-117799A
-
|
5-HT Receptor
|
Endocrinology
|
LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders .
|
-
- HY-117575
-
|
5-HT Receptor
|
Neurological Disease
|
WAY-100135 is a serotonergic compound belonging to the phenylpiperazine family, utilized in scientific research for its role as a strong antagonist of the 5-HT1A receptor and a partial agonist of the 5-HT1D receptor, with minimal activity at the 5-HT1B receptor.
|
-
- HY-19733
-
ITI-007 tosylate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Cancer
|
Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .
|
-
- HY-125905
-
VHL ligand 3; E3 ligase Ligand 19
|
Ligands for E3 Ligase
|
Cancer
|
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4 .
|
-
- HY-108057A
-
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki 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 Ki value of 1.2 nM .
|
-
- HY-P0205A
-
[Sar1,Ala8] Angiotensin II acetate hydrate
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-P0205
-
[Sar1,Ala8] Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-107656
-
|
mAChR
|
Neurological Disease
|
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
|
-
- HY-121855
-
Glycerol 1-monoelaidate; α-Monoelaidin
|
Biochemical Assay Reagents
|
Others
|
Monoeladin is an ester derivative of glycerin and oleic acid, which are commonly found in various vegetable and animal fats. Monoeladin has unique chemical properties that make it an important intermediate in the biosynthesis of other lipid molecules, especially in the formation of triglycerides and phospholipids. It also plays a role in food science as a partial replacement for saturated fat, which has been linked to an increased risk of heart disease.
|
-
- HY-122112
-
|
Sigma Receptor
|
Cancer
|
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
|
-
- HY-14558R
-
|
5-HT Receptor
|
Neurological Disease
|
Tandospirone (Standard) is the analytical standard of Tandospirone. This product is intended for research and analytical applications. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms .
|
-
- HY-121974
-
|
Others
|
Neurological Disease
|
SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain .
|
-
- HY-123689A
-
ALKS-33 hydrochloride; RDC-0313 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
Samidorphan hydrochloride is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-B0489R
-
|
mAChR
nAChR
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
|
-
- HY-15414
-
Vortioxetine
Maximum Cited Publications
9 Publications Verification
Lu AA 21004
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
Cancer
|
Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
|
-
- HY-G0021
-
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-100822
-
(+)-HA-966
|
iGluR
|
Neurological Disease
|
(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist/antagonist of glycine site of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine . (R)-(+)-HA-966 can cross the blood-brain barrier and has the potential for neuropathic and acute pain .
|
-
- HY-P0205B
-
[Sar1,Ala8] Angiotensin II TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-B0731
-
SM-9018
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-111254
-
|
PPAR
|
Metabolic Disease
|
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain .
|
-
- HY-B0032AS
-
SM-13496-d8
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Lurasidone-d8 is deuterium labeled Lurasidone. 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-HT1A receptor with an IC50 of 6.75 nM.
|
-
- HY-105115
-
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
|
-
- HY-17637
-
ITI-007
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Cancer
|
Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used for the study of schizophrenia and bipolar depression .
|
-
- HY-P2625S
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-123689
-
ALKS-33; RDC-0313
|
Opioid Receptor
|
Neurological Disease
|
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-12752A
-
Trimeprazine hemitartrate
|
Histamine Receptor
Influenza Virus
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Alimemazine hemitartrate (Trimeprazine hemitartrate) is an antagonist of the histamine (HA) receptor that can be taken orally and also acts as a partial agonist at other GPCR receptors. Alimemazine hemitartrate has effects that include anti-serotonin, antispasmodic, antihistamine, sedation, hypnotic, antiviral, and anti-nausea properties. Alimemazine hemitartrate promotes the growth of pancreatic β-cells in mice and improves diabetes in mice .
|
-
- HY-16718
-
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
|
-
- HY-19505
-
|
GABA Receptor
|
Neurological Disease
|
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties .
|
-
- HY-17401S
-
CVT 303-dd8 dihydrochloride; RS 43285-d8
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
|
-
- HY-101300
-
LD 3098 hydrochloride
|
Adenosine Receptor
|
Neurological Disease
|
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full?α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) .
|
-
- HY-129707
-
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 hemicalcium inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents .
|
-
- HY-117829
-
UNC9994
1 Publications Verification
|
Dopamine Receptor
5-HT Receptor
Histamine Receptor
Arrestin
|
Neurological Disease
|
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
|
-
- HY-16718A
-
PF-00251802 hydrochloride
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
|
-
- HY-Y1365
-
|
Biochemical Assay Reagents
|
Metabolic Disease
Cancer
|
Gelatins is a non-toxic, non carcinogenic, biodegradable, and non irritating natural polymer derived from partial hydrolysis of collagen. Due to its strong liquid absorption and swelling ability, Gelatins has excellent hemostatic properties and can be used as a matrix material for the reduction, growth, and stability of metal nanoparticles. Gelatins can also be used for tumor cell culture and tumor therapy [1][2][3].
|
-
- HY-149387
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-149386
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-P2625S1
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-14262S1
-
EMD 68843-d8; SB659746A-d8
|
5-HT Receptor
Serotonin Transporter
Isotope-Labeled Compounds
|
Neurological Disease
|
Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
|
-
- HY-B0032AR
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Lurasidone (Standard) is the analytical standard of Lurasidone. This product is intended for research and analytical applications. 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-HT1A receptor with an IC50 of 6.75 nM.
|
-
- HY-B0032R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Lurasidone (Hydrochloride) (Standard) is the analytical standard of Lurasidone (Hydrochloride). This product is intended for research and analytical applications. 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-HT1A receptor with an IC50 of 6.75 nM.
|
-
- HY-162835
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a PROTAC-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) .
|
-
- HY-126932
-
|
Estrogen Receptor/ERR
|
Cancer
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three TR ER+ breast cancer cell cultures in 3D. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites, mimicking the actions of E2 .
|
-
- HY-W654010
-
SM-13496-d8-1 hydrochloride
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). 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-HT1A receptor with an IC50 of 6.75 nM .
|
-
- HY-A0007
-
N-0923 Hydrochloride
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki 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-15414A
-
Lu AA21004 hydrobromide
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
Cancer
|
Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
|
-
- HY-B0280S2
-
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
Ranolazine-d3 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-B0280S1
-
|
Isotope-Labeled Compounds
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
Ranolazine-d8 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-15780S
-
OPC-34712-d8
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Brexpiprazole-d8 is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].
|
-
- HY-14547
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia .
|
-
- HY-B0280S
-
CVT 303-d5; RS 43285-003-d5
|
Isotope-Labeled Compounds
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
|
-
- HY-14547A
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia .
|
-
- HY-15394A
-
N-0437
|
Adrenergic Receptor
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
Endocrinology
|
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis 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-12752BS
-
Trimeprazine-d6 hydrochloride
|
Histamine Receptor
Isotope-Labeled Compounds
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
|
-
- HY-101586A
-
Lu 25-109 maleate
|
mAChR
|
Neurological Disease
|
Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats .
|
-
- HY-105056
-
Ro 16-6028
|
GABA Receptor
|
Neurological Disease
|
Bretazenil (Ro 16-6028) is a partial agonist at the gamma-aminobutyric acid A (GABAA) receptor-linked benzodiazepine site. Bretazenil is potent benzodiazepine examined, exhibiting an IC50 (concentration at which half-maximal inhibition of specific [35S]TBPS binding occurs) of 6.1 nM. Bretazenil shows an EC50 of 10 nM for recombinant α1β1γ2. Anticonvulsant effects .
|
-
- HY-108506
-
BIA 2-005; GP 47779
|
Sodium Channel
|
Neurological Disease
|
Licarbazepine (BIA 2-005; GP 47779)?is a?voltage-gated sodium channel?blocker?with?anticonvulsant?and?mood-stabilizing?effects .
|
-
- HY-108506R
-
|
Sodium Channel
|
Neurological Disease
|
Licarbazepine (Standard) is the analytical standard of Licarbazepine. This product is intended for research and analytical applications. Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects .
|
-
- HY-B0072
-
-
- HY-A0087
-
|
Biochemical Assay Reagents
PPAR
Estrogen Receptor/ERR
Cytochrome P450
|
Others
|
Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes .
|
-
- HY-B0731A
-
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-P1318
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1318A
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-19686
-
TVX Q 7821 free base
|
5-HT Receptor
|
Neurological Disease
|
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function .
|
-
- HY-P1726A
-
|
Melanocortin Receptor
|
Cancer
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
|
-
- HY-147757
-
|
PPAR
|
Metabolic Disease
|
PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively .
|
-
- HY-B0280R
-
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
Ranolazine (Standard) is the analytical standard of Ranolazine. This product is intended for research and analytical applications. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP) . Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor . Antianginal agent.
|
-
- HY-103524R
-
(-)-Valerenic Acid (Standard)
|
5-HT Receptor
GABA Receptor
|
Neurological Disease
|
Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABAA receptors. Valerenic acid is also a partial agonist of the 5-HT5a receptor. Valerenic acid mediates anxiolytic activity via GABAA receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .
|
-
- HY-N6869R
-
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-19686A
-
TVX Q 7821
|
5-HT Receptor
|
Neurological Disease
|
Ipsapirone hydrochloride (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone hydrochloride (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function .
|
-
- HY-B1264R
-
|
NO Synthase
Adrenergic Receptor
|
Cardiovascular Disease
|
Celiprolol (hydrochloride) (Standard) is the analytical standard of Celiprolol (hydrochloride). This product is intended for research and analytical applications. Celiprolol (REV 5320) is a potent, cardioselective and orally active β1-andrenoceptor r antagonist with partial β2 agonist activity, with Ki values of 0.14-8.3 μM. Celiprolol has antihypertensive and antianginal activity, and can be used for the research of cardiovascular disease such as high blood pressure .
|
-
- HY-15394
-
N-0437 hydrochloride
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis 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-100848
-
|
EGFR
|
Cancer
|
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .
|
-
- HY-133152
-
DM-3411
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM .
|
-
- HY-119486A
-
(Rac)-PF-06649751; (Rac)-CVL-751
|
Dopamine Receptor
Arrestin
|
Neurological Disease
|
(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
|
-
- HY-115644
-
|
Melanocortin Receptor
|
Inflammation/Immunology
|
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties .
|
-
- HY-P2090
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
|
-
- HY-125626
-
8-iso-15-keto PGF2α
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a partial agonist for Thromboxane receptor (TP), which exhibits a vasoconstrictor efficacy with a pD2 of 5.8. 8-iso-15-keto Prostaglandin F2α mediates a weak relaxation of rats aorta rings at high concentration .
|
-
- HY-134269
-
7-Deaza-8-bromo-cADPR; 7-Deaza-8-bromo-cyclic ADP ribose
|
Calcium Channel
|
Neurological Disease
|
8-Br-7-CH-cADPR (7-Deaza-8-bromo-cADPR) is a potent cADPR antagonist. 8-Br-7-CH-cADPR shows partial inhibition of calcium elevation caused by sTIR dimerization. 8-Br-7-CH-cADPR significantly decreases Paclitaxel (HY-B0015)-induced axon degeneration .
|
-
- HY-U00033
-
|
Others
|
Neurological Disease
|
Iomazenil is a benzodiazepine receptor antagonist with partial inverse agonist activity. Iomazenil can assess the binding potential of central benzodiazepine receptors in the cerebral cortex and may reflect neuronal function in viable tissue. Iomazenil use is associated with improved cognitive function in adult patients with ischemic cerebral pathology after indirect revascularization surgery. Iomazenil demonstrated restoration of benzodiazepine receptor binding potential in the affected hemisphere after surgery on brain SPECT imaging .
|
-
- HY-75502
-
N-0923; (-)-N 0437
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
Endocrinology
|
Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
|
-
- HY-N2025
-
|
PPAR
Glucosidase
|
Metabolic Disease
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-12397
-
|
VD/VDR
|
Endocrinology
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character .
|
-
- HY-19411
-
|
nAChR
|
Neurological Disease
|
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus .
|
-
- HY-P2090A
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
|
-
- HY-10063
-
TC-1734; ACD3480
|
nAChR
|
Neurological Disease
|
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
|
-
- HY-G0021S
-
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
|
-
- HY-105689
-
|
RAR/RXR
|
Others
|
AGN 192870 is a RAR neutral antagonist with Kds of 147, 33, and 42 nM for RARα, RARβ, and RARγ, respectively. AGN 192870 shows IC50s of 87 and 32 nM for RARαand RARγ, respectively. AGN 192870 shows RARβ partial agonism . AGN 192870 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-111385
-
|
Dopamine Receptor
5-HT Receptor
Arrestin
|
Neurological Disease
|
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
|
-
- HY-G0021S1
-
Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
|
-
- HY-148922
-
|
PPAR
|
Metabolic Disease
|
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
|
-
- HY-A0007R
-
N-0923 Hydrochloride (Standard)
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki 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-15414R
-
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
Cancer
|
Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
|
-
- HY-B0731R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone (hydrochloride) (Standard) is the analytical standard of Perospirone (hydrochloride). This product is intended for research and analytical applications. Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-123689S
-
ALKS-33-d4; RDC-0313-d4
|
Isotope-Labeled Compounds
|
Neurological Disease
|
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
|
-
- HY-123689S1
-
ALKS-33-d5; RDC-0313-d5
|
Isotope-Labeled Compounds
Opioid Receptor
|
Neurological Disease
|
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
|
-
- HY-115861
-
|
Others
|
Neurological Disease
|
UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies .
|
-
- HY-G0021R
-
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-15414AS
-
Lu AA21004-d8 hydrobromide
|
Isotope-Labeled Compounds
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
|
-
- HY-15414S
-
Lu AA 21004 d8
|
Isotope-Labeled Compounds
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
|
-
- HY-125751
-
|
Dopamine Receptor
|
Neurological Disease
|
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole .
|
-
- HY-120423
-
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Cannabinoid Receptor
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Neurological Disease
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AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability . AM-6538 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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- HY-10019S
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CP 526555-d4
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Isotope-Labeled Compounds
nAChR
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Neurological Disease
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Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
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- HY-15394S
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N-0437-d7 hydrochloride
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Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
Endocrinology
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(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-114678
-
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5-HT Receptor
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Neurological Disease
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LY302148 is a receptor ligand for 5-HT1F. Compared to the Emax of 5-HT, LY302148 behaves as a partial agonist for the 5-HT1F receptor. In the [ 35S]GTPγS binding assay targeting human 5-HT1F receptors, LY302148 exhibits good potency with an EC50 value of 5.23 nM. LY302148 can be used in the research of migraine .
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- HY-B0229
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BW-311C90; 311C90
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5-HT Receptor
Endogenous Metabolite
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Neurological Disease
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Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with Kis of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine .
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- HY-120045A
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Opioid Receptor
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Neurological Disease
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DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .
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- HY-15780
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OPC-34712
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
|
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-10233
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Lu 02-030 hydrochloride; THIP hydrochloride
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GABA Receptor
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Neurological Disease
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Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
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- HY-133152S
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DM-3411 d8
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Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
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Neurological Disease
|
Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
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- HY-14330
-
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Dopamine Receptor
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Neurological Disease
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ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-103409
-
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Dopamine Receptor
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Neurological Disease
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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- HY-101198
-
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Histamine Receptor
Apoptosis
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Neurological Disease
Cancer
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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 (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .
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- HY-136207
-
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nAChR
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Neurological Disease
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TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect .
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- HY-130344
-
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Dopamine Receptor
Sigma Receptor
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Neurological Disease
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SKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression .
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- HY-B1562
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(±)-Bopindolol
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Adrenergic Receptor
Renin
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
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- HY-B1562C
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(±)-Bopindolol fumarate
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Adrenergic Receptor
Renin
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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Bopindolol ((±)-Bopindolol) fumarate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol fumarate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol fumarate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol fumarate is a proagent of Pindolol (HY-B0982). Bopindolol fumarate can be used for essential and renovascular hypertension research.
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- HY-15780A
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OPC-34712 hydrochloride
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
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Neurological Disease
|
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-15394S1
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N-0437-d3 hydrochloride
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Isotope-Labeled Compounds
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Endocrinology
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(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-75502R
-
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Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
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Neurological Disease
Endocrinology
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Rotigotine (Standard) is the analytical standard of Rotigotine. This product is intended for research and analytical applications. Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .
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- HY-120498
-
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5-HT Receptor
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Neurological Disease
|
RS-64459-193 is a 5-HT1A receptor partial agonist with a Ki of 24.9 nM. RS-64459-193 also shows high affinity for 5-HT2C, 5-HT2A and 5-HT7 with pKi values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is almost devoid of activity at the m 5-HT3 receptor .
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- HY-15414S1
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Lu AA 21004-d6
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Serotonin Transporter
5-HT Receptor
Isotope-Labeled Compounds
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Neurological Disease
Cancer
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Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
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- HY-13967B
-
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Free Fatty Acid Receptor
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Metabolic Disease
|
AMG 837 calcium hydrate is a potent, orally bioavailable and partial agonist of GPR40/FFA1. AMG 837 calcium hydrate inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 calcium hydrate could enhance insulin secretion and lower glucose levels in rodents . AMG 837 (calcium hydrate) 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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- HY-100186
-
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Androgen Receptor
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Cardiovascular Disease
Others
Metabolic Disease
Inflammation/Immunology
Endocrinology
Cancer
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GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness .
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- HY-14565
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ABT-089
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nAChR
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Neurological Disease
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Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
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- HY-103412
-
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Dopamine Receptor
Sigma Receptor
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Neurological Disease
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SKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression .
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- HY-150030
-
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Cannabinoid Receptor
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Neurological Disease
|
CB1/2 agonist 4 is a full CB1 agonist and CB2 partial agonist with EC50 values of 15.09 nM and 1.16 nM, respectively. CB1/2 agonist 4 also has hCB1 and hCB2 receptor affinities with Ki values of 1.1 nM and 4.2 nM, respectively. CB1/2 agonist 4 has a significant antinociceptive activity, and also can activate cannabinoid and TRPV1 receptor with values of IC50 and EC50 is 0.8 μM and 0.12 μM, respectively .
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- HY-B1562B
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(±)-Bopindolol (malonate)
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Adrenergic Receptor
Renin
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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Bopindolol ((±)-Bopindolol) malonate is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol malonate is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol malonate has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol malonate is a proagent of Pindolol (HY-B0982). Bopindolol malonate can be used for essential and renovascular hypertension research.
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- HY-P2797
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AMCase, Serratia marcescens
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Bacterial
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Metabolic Disease
Inflammation/Immunology
|
Chitinase, Serratia marcescens (EC 3.2.1.14) has partial lysozyme activity and is widely found in bacteria, fungi, animals and some plants. Chitinase belongs to the glycosyl hydrolase family. Chitinase catalyzes chito-oligosaccharide hydrolysis. Chitinases also can serve as prognostic biomarkers of disease progression. Chitinase can be used in the research of pathogenesis of various human fibrotic and inflammatory disorders, particularly those of the lung (idiopathic pulmonary fibrosis, chronic obstructive pulmonary disease, sarcoidosis, and asthma) and the gastrointestinal tract (inflammatory bowel diseases (IBDs) and colon cancer) .
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- HY-132190
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1-O-Hexa-decyl-2-acetyl-sn-glycero-3-phospho(N,N,N-trimethyl)-hexanolamine
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Platelet-activating Factor Receptor (PAFR)
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Cardiovascular Disease
|
Hexanolamino PAF C-16 (1-O-hexadecyl-2-acetyl-sn-glycero-3-phospho (N,N,N trimethyl) hexanolamine) is a Platelet-activating Factor Receptor (PAFR) Modulator with partial agonist activity. Hexanolamino PAF C-16 induces platelet aggregation and macrophage production but fails to increase [Ca2+]i in platelets, suggesting that PAF receptors may interact with PAF receptors through Ca 2+-dependent and -independent pathways. Related to platelet aggregation .
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- HY-N2025R
-
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PPAR
Glucosidase
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Metabolic Disease
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
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- HY-B0229S
-
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- HY-121029
-
KRP-104
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Histone Methyltransferase
|
Metabolic Disease
|
Bisegliptin (KRP-104) is a small molecule compound with antidiabetic activity. Bisegliptin is metabolized mainly by converting the cyano group to the carboxylic acid form, and DPP-4 plays a partial role in its metabolism. The carboxylic acid metabolite of bisegliptin can be detected both in vivo and in vitro. In rat experiments, the plasma concentration of the carboxylic acid metabolite of bisegliptin was affected by other DPP inhibitors, showing the complexity of its metabolic process. The amide intermediate of bisegliptin was detected both in vivo and in vitro, and its conversion rate was significantly faster than that of the parent compound when incubated with DPP-4 .
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- HY-168241
-
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Cholinesterase (ChE)
5-HT Receptor
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Infection
|
Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .
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- HY-111052
-
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GABA Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
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- HY-108039
-
HE 3286; NE-3107
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NF-κB
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis . Bezisterim 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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- HY-100552
-
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5-HT Receptor
|
Neurological Disease
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
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- HY-157425
-
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5-HT Receptor
|
Neurological Disease
|
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
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- HY-160887
-
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5-HT Receptor
|
Neurological Disease
|
FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
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- HY-121579
-
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Others
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Others
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L-764406 is a non-thiazolidinedione (TZD)-type PPARg nuclear receptor ligand with high affinity. L-764406 has significant binding ability to PPARg (IC50=70 nM). L-764406 exhibited partial agonist activity and induced expression of the adipocyte-specific gene aP2 in chimeric receptors expressing the PPARg LBD and the corresponding reporter gene, as well as in 3T3-L1 cells. In contrast, L-764406 showed no activity in cells transfected with chimeric receptors containing PPARa or PPARd LBDs .
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- HY-18957C
-
BGB-283 hydrochloride
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Others
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Cancer
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
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- HY-W009009
-
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GABA Receptor
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Neurological Disease
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2 .
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- HY-15780S1
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OPC-34712-d8-1
|
Dopamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
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- HY-130311
-
2-Monolinolein; 2-Monolinoleoylglycerol
|
Cannabinoid Receptor
|
Neurological Disease
|
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
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- HY-15780R
-
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5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
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- HY-W052508
-
N-Desalkylquetiapine
|
5-HT Receptor
|
Neurological Disease
|
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
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- HY-138879B
-
(1S,5R)-CP-601927
|
nAChR
|
Neurological Disease
|
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
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- HY-100554
-
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
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- HY-121900
-
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PPAR
|
Metabolic Disease
Endocrinology
|
LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
|
-
- HY-19842
-
CVT 3619
|
Adenosine Receptor
|
Cardiovascular Disease
Metabolic Disease
|
GS-9667 (CVT 3619), a novel N 6-5'-substituted adenosine analog, is a selective, partial agonist of the A1 adenosine receptor (A1AdoR). GS-9667 binds to adipocyte membranes with high (KH=14 nM) and low (KL=5.4 μM) affinities. GS-9667 reduces cyclic AMP content and release of nonesterified fatty acids from epididymal adipocytes with IC50 values of 6 nM and 44 nM, respectively. GS-9667 inhibits lipolysis and has the potential for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA) .
|
-
- HY-101341
-
|
5-HT Receptor
|
Neurological Disease
|
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
|
-
- HY-N0049
-
|
Parasite
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- HY-109112
-
RP5063
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
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 (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=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-W027553
-
NIK-247 free base
|
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Neurological Disease
Metabolic Disease
|
Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-108548
-
Rp-8-Bromo-PET-cGMPS
|
Others
|
Inflammation/Immunology
|
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
|
-
- HY-115857
-
|
Others
|
Neurological Disease
|
SH-053-S-CH3-2'F is a selective positive allosteric modulator that produces mild to partial agonistic activity at α(1) GABA(A) receptors. SH-053-S-CH3-2'F showed anxiety-relieving effects at a dose of 30 mg/kg. SH-053-S-CH3-2'F completely avoids the memory impairment commonly caused by benzodiazepine site agonists. SH-053-S-CH3-2'F shows strong selectivity at GABA(A) receptors, which could potentially be used to develop more selective anti-anxiety drugs .
|
-
- HY-18137
-
|
5-HT Receptor
|
Neurological Disease
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
|
-
- HY-162083
-
|
Cannabinoid Receptor
5-HT Receptor
|
Neurological Disease
|
CB2R/5-HT1AR agonist 1 (Compound 2o) is an orally active partial agonist of the CB2 receptor (EC50=479.6 nM). CB2R/5-HT1AR agonist 1 is a full agonist of 5-HT1A receptor (EC50=2.7 μM). CB2R/5-HT1AR agonist 1 exhibits anti-anxiety and anti-depressive effects. CB2R/5-HT1AR agonist 1 possesses favorable pharmacokinetic properties .
|
-
- HY-N0049R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- HY-109112R
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. 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 (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=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 .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-Y0850O
-
PVA (Mw 31000-50000, 87-89% hydrolyzed); Poly(Ethenol) (Mw 31000-50000, 87-89% hydrolyzed)
|
Drug Delivery
|
Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) is a synthetic polymer derived from polyvinyl acetate through partial or complete hydroxylation .
|
-
- HY-Y1365
-
|
Thickeners
|
Gelatins is a non-toxic, non carcinogenic, biodegradable, and non irritating natural polymer derived from partial hydrolysis of collagen. Due to its strong liquid absorption and swelling ability, Gelatins has excellent hemostatic properties and can be used as a matrix material for the reduction, growth, and stability of metal nanoparticles. Gelatins can also be used for tumor cell culture and tumor therapy [1][2][3].
|
-
- HY-154924
-
S-NADP
|
Biochemical Assay Reagents
|
Thio-NADP (S-NADP) is a nicotinic acid adenine dinucleotide phosphate (NAADP) inhibitor. Thio-NADP activates partial Ca 2+ release .
|
-
- HY-121855
-
Glycerol 1-monoelaidate; α-Monoelaidin
|
Drug Delivery
|
Monoeladin is an ester derivative of glycerin and oleic acid, which are commonly found in various vegetable and animal fats. Monoeladin has unique chemical properties that make it an important intermediate in the biosynthesis of other lipid molecules, especially in the formation of triglycerides and phospholipids. It also plays a role in food science as a partial replacement for saturated fat, which has been linked to an increased risk of heart disease.
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2625
-
|
GCGR
|
Metabolic Disease
|
GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM) .
|
-
- HY-P5535
-
OCE-205
|
Vasopressin Receptor
|
Inflammation/Immunology
|
Invopressin (Compound 42) is a vasopressin V1A receptor partial agonist (EC50: 1.0 nM). Invopressin can be used for research of cirrhosis, including bacterial peritonitis, HRS2 and refractory ascites .
|
-
- HY-P5516
-
|
Peptides
|
Others
|
SNNF(N-Me)GA(N-Me)IL is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence)
|
-
- HY-P5517
-
|
Peptides
|
Others
|
SNNF(N-Me)GA(N-Me)ILSS is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence)
|
-
- HY-P3617
-
|
Peptides
|
Metabolic Disease
|
Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca 2+ pump in liver plasma membranes independently of adenylate cyclase activation .
|
-
- HY-106234
-
-
- HY-P3563
-
|
Endothelin Receptor
|
Cardiovascular Disease
|
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC50 of 1.5 nM .
|
-
- HY-P5358
-
|
Protease Activated Receptor (PAR)
|
Others
|
YFLLRNP is a biological active peptide. (a partial agonist of PAR-1. YFLLRNP selectively active G12/13 signaling pathway without activating Gq or Gi pathways at low concentrations. YFLLRNP (60 μM))
|
-
- HY-P10325
-
-
- HY-P7060
-
TPPT
|
iGluR
|
Neurological Disease
|
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
|
-
- HY-P1294
-
|
CRFR
|
Neurological Disease
|
α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-P1294A
-
|
CRFR
|
Neurological Disease
|
α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist with KB of ~100 nM. α-Helical CRF(9-41) TFA is also a partial agonist of CRF1 receptor with an EC50 of 140 nM .
|
-
- HY-P10377
-
|
Neuropeptide FF Receptor
|
Metabolic Disease
|
GUB03385 is a long-acting PrRP31 analogue. GUB03385 is a potent dual agonist for GPR10 (full agonist, EC50: 0.4 nM) and NPFF2R (partial agonist, EC50: 20 nM). GUB03385 has anti-obesity effect .
|
-
- HY-P1316
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for µ-, κ- or δ-opioid receptors .
|
-
- HY-P1316A
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRWK-NH2 is a potent and selective partial agonist for the nociceptin receptor (NOP), [ 3H]Ac-RYYRWK-NH2 binds to rat cortical membranes ORL1 with a Kd of 0.071 nM, but has no affinity for μ-, κ- or δ-opioid receptors .
|
-
- HY-P5515
-
|
Peptides
|
Others
|
F(N-Me)GA(N-Me)IL is a biological active peptide. (Double N-methylated derivatives of amyloidogenic and cytotoxic partial IAPP sequence were found to be devoid of β-sheet structure, amyloidogenicity and cytotoxicity, The derivatives were able to interact with the native sequences and inhibit amyloid formation)
|
-
- HY-P0227
-
|
Melanocortin Receptor
|
Metabolic Disease
|
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
|
-
- HY-P3343A
-
|
Estrogen Receptor/ERR
|
Cancer
|
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells .
|
-
- HY-P0205A
-
[Sar1,Ala8] Angiotensin II acetate hydrate
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) acetate hydrate is an octapeptide analog of angiotensin II. Saralasin acetate hydrate is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin acetate hydrate can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-P0205
-
[Sar1,Ala8] Angiotensin II
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) is an octapeptide analog of angiotensin II. Saralasin is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-P0205B
-
[Sar1,Ala8] Angiotensin II TFA
|
Angiotensin Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
Saralasin ([Sar1,Ala8] Angiotensin II) TFA is an octapeptide analog of angiotensin II. Saralasin TFA is a competitive angiotensin II receptor antagonist with a Ki value of 0.32 nM for 74% of the binding sites, and has partial agonist activity as well. Saralasin TFA can be used for the research of renovascular hypertension, renin-dependent (angiotensinogenic) hypertension .
|
-
- HY-P2625S
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-P2625S1
-
|
Isotope-Labeled Compounds
|
Metabolic Disease
|
GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
|
-
- HY-P1318
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1318A
-
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
|
-
- HY-P1726A
-
|
Melanocortin Receptor
|
Cancer
|
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
|
-
- HY-P2090
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
|
-
- HY-P2090A
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
|
-
- HY-P2055
-
|
Peptides
|
Endocrinology
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99794
-
BAY 1213790
|
Factor Xa
|
Cardiovascular Disease
|
Osocimab (BAY 1213790), an anti-FXIa antibody (Ki=2.4 nM; EC50=0.2 nM). FXI inhibition may reduce the risk of thrombosis. Osocimab inhibits thrombin generation, and prolongs activated partial thromboplastin time. Osocimab exhibits anticoagulant effects .
|
-
- HY-P99321
-
BMS 224819; Chi220; Anti-Human CD40 Recombinant Antibody
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Teneliximab (BMS-224819) is a chimeric monoclonal antibody, blocks the CD40-CD40L interaction. Teneliximab (BMS-224819) has partial agonist activity resulting in some signaling through CD40 and peripheral B cell depletion .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0175
-
-
-
- HY-N1951
-
-
-
- HY-N11464
-
-
-
- HY-N8505
-
-
-
- HY-N2364
-
-
-
- HY-B0030
-
-
-
- HY-117526
-
-
-
- HY-N0175R
-
-
-
- HY-B0489A
-
-
-
- HY-N7687
-
-
-
- HY-B0489
-
-
-
- HY-107803
-
-
-
- HY-N6869
-
-
-
- HY-B0030R
-
-
-
- HY-B0489R
-
|
Alkaloids
Structural Classification
Areca catechu L.
Other Alkaloids
Source classification
Palmae
Plants
|
mAChR
nAChR
|
Arecoline (hydrobromide) (Standard) is the analytical standard of Arecoline (hydrobromide). This product is intended for research and analytical applications. Arecoline hydrobromide, a naturally occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline hydrobromide exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline hydrobromide also can induce oxidative stress .
|
-
-
- HY-N6869R
-
|
Structural Classification
Microorganisms
other families
Terpenoids
Source classification
Diterpenoids
Plants
|
Antibiotic
PPAR
Bacterial
Fungal
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
-
- HY-N2025
-
-
-
- HY-B0229
-
-
-
- HY-N2025R
-
|
Structural Classification
Flavonoids
Flavones
Source classification
Bignoniaceae
Plants
Oroxylum indicum (Linn.) Bentham ex Kurz
|
PPAR
Glucosidase
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
-
- HY-N0049
-
-
-
- HY-N0049R
-
|
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-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14261S
-
|
Vilazodone-d8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
|
-
-
- HY-126057S
-
|
(R)-Praziquantel-d11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].
|
-
-
- HY-14546S1
-
|
Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM[1][2].
|
-
-
- HY-15831
-
|
L-838417-d9 is the deuterium labeled L-838417. L-838417 is a subtype-selective GABAA positive allosteric modulator, acting as a partial agonist at α2, α3 and α5 subtypes[1].
|
-
-
- HY-10019S1
-
|
Varenicline- 15N, 13C,d2 is 15N and deuterated labeled Varenicline (HY-10019). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50=250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
|
-
-
- HY-10019AS1
-
|
Varenicline-d4 hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .
|
-
-
- HY-B0982S
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Pindolol-d7 (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33 nM)[1][2].
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- HY-Y1176S
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Isonipecotic acid-d9 is the deuterium labeled Isonipecotic acid[1]. Isonipecotic acid is a GABAA receptor partial agonist[2].
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- HY-10020S
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Varenicline-15N3 Hydrochloride (CP 526555-15N3 Hydrochloride) is the 15N labeled isotope of Varenicline hydrochloride (HY-10020). Varenicline (CP 526555) is an orally active partial agonist of α4β2 nicotinic acetylcholine receptor (α4β2 nAChR, IC50 = 250 nM), which is the principal mediator of nicotine dependence. Varenicline is also a partial agonist of α6β2 nAChR and a full agonist of α6β2 nAChR. Varenicline blocks the direct agonist effects of nicotine on nAChR while stimulates nAChR in a more moderate way, being widely used as an aid of smoking cessation .
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- HY-14153AS
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Tegaserod- 13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
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- HY-B0032AS
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Lurasidone-d8 is deuterium labeled Lurasidone. 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-HT1A receptor with an IC50 of 6.75 nM.
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- HY-P2625S
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GLP-2(3-33) (Leu- 13C6, 15N) is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
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- HY-17401S
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Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor[3].
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- HY-P2625S1
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GLP-2(3-33) (Leu- 13C6, 15N) TFA is 13C and 15N labeled GLP-2(3-33) (HY-P2625). GLP-2(3-33), generated naturally by dipeptidylpeptidase IV (DPPIV), acts as a partial agonist on GLP-2 receptor (EC50=5.8 nM).
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- HY-14262S1
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Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
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- HY-W654010
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Lurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). 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-HT1A receptor with an IC50 of 6.75 nM .
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- HY-B0280S2
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Ranolazine-d3 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
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- HY-B0280S1
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Ranolazine-d8 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
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- HY-15780S
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Brexpiprazole-d8 is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].
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- HY-B0280S
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Ranolazine-d5 is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
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- HY-12752BS
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Alimemazine-d6 hydrochloride (Trimeprazine-d6 hydrochloride) is the deuterium labeled Alimemazine (HY-12752). Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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- HY-G0021S
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N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].
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- HY-G0021S1
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N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist[1][2][3].
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- HY-123689S
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Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
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- HY-123689S1
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Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .
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- HY-15414AS
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Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
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- HY-15414S
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Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
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- HY-10019S
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Varenicline-d4 is deuterium labeled Varenicline. Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively[1]. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment[2].
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- HY-15394S
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(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-133152S
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Brexpiprazole S-oxide-d8 is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].
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- HY-15394S1
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(Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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- HY-15414S1
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Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
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- HY-B0229S
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Zolmitriptan-d6 is deuterium labeled Zolmitriptan. Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with Kis of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine[1][2].
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- HY-15780S1
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Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
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Cat. No. |
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Classification |
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- HY-103476
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Azide
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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 . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-128855
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Alkynes
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Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine 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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- HY-108039
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HE 3286; NE-3107
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Alkynes
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Bezisterim (HE 3286; NE-3107) is a synthetic derivative of a natural anti-inflammatory steroid, β-AET. Bezisterim is an orally active partial NF-κB inhibitor. HE3286 reduces proinflammatory signals, including IL-6 and matrix metallopeptidase 3. Bezisterim freely penetrates the blood brain barrier in mice. Bezisterim can be used for the research of the ulcerative colitis, arthritis, experimental autoimmune encephalomyelitis . Bezisterim 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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Cat. No. |
Product Name |
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Classification |
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- HY-Y0850O
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PVA (Mw 31000-50000, 87-89% hydrolyzed); Poly(Ethenol) (Mw 31000-50000, 87-89% hydrolyzed)
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Polymers
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Polyvinyl alcohol (Mw 31000-50000, 87-89% hydrolyzed) is a synthetic polymer derived from polyvinyl acetate through partial or complete hydroxylation .
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- HY-Y1365
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Emulsifiers
Disintegrants
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Gelatins is a non-toxic, non carcinogenic, biodegradable, and non irritating natural polymer derived from partial hydrolysis of collagen. Due to its strong liquid absorption and swelling ability, Gelatins has excellent hemostatic properties and can be used as a matrix material for the reduction, growth, and stability of metal nanoparticles. Gelatins can also be used for tumor cell culture and tumor therapy [1][2][3].
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