Search Result
Results for "
brain disorders
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
11
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-160505
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HCN Channel
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Neurological Disease
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RO-275 (compound 29) is a potent, selective and orally active HCN1 inhibitor with IC50 values of 0.046, 14.3, 4.6, 13.9 µM for HCN1, HCN2, HCN3, HCN4, respectively. RO-275 rescues decremented working memory. RO-275 has the potential for the research of cognitive dysfunction in brain disorder .
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- HY-148137
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Cannabinoid Receptor
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Neurological Disease
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CB1 agonist 1 (compound 22) is an agonist of CB1. CB1 agonist 1 shows affinity to CB1 receptor with an pIC50 value of 5.7. CB1 agonist 1 can be used for the research of brain disorders .
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- HY-117516
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REV-ERB
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Neurological Disease
Metabolic Disease
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SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders .
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- HY-101834
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Orexin Receptor (OX Receptor)
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Others
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ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC50s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .
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- HY-W250174
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3,5-Diiodosalicylic acid lithium salt
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Biochemical Assay Reagents
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Others
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Lithium 3,5-diiodosalicylate is a compound used in the study of bipolar disorder and other psychiatric disorders. It contains lithium and a salicylate. Lithium 3,5-diiodosalicylate works by affecting the levels of certain neurotransmitters in the brain, including dopamine and serotonin.
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- HY-17646
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AZD3241
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Glutathione Peroxidase
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Neurological Disease
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Verdiperstat (AZD3241) is a selective, irreversible and orally active myeloperoxidase (MPO) inhibitor, with an IC50 of 630 nM, and can be used in the research of neurodegenerative brain disorders.
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- HY-B0762S
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O-Acetyl-L-carnitine-d3 (hydrochloride)
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Endogenous Metabolite
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Neurological Disease
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Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
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- HY-148331
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Prolyl Endopeptidase (PREP)
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Neurological Disease
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Z-Thioprolyl-Thioproline is a bovine brain prolyl endopeptidase (PEP) inhibitor (IC50=16 µM; Ki=37 µM). Z-Thioprolyl-Thioproline is used in the study of neurological disorders such as memory disorders and cognitive disorders .
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- HY-118182
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Others
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Neurological Disease
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Tidembersat (Example 4) is a benzopyran derivative that can be used in the research of a variety of CNS disorders and traumatic brain injury .
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- HY-164506
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Others
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Neurological Disease
Cancer
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NRMA-8 is a brain-penetrant small molecule nuclear receptor modulator. NRMA-8 is promising for research of central nervous system disorders, including Alzheimer's disease, Parkinson's disease, demylenation disorders and glioblastomas .
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- HY-162660
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GPR88
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Neurological Disease
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BI-9508 is a selective and cross the blood-brain barrier GPR88 agonist. BI-9508 has the potential for the research of neurological disorders .
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- HY-W017933
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Octahydro-1H-isoindole; Perhydroisoindole; Hexahydroisoindoline
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Neurokinin Receptor
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Neurological Disease
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Octahydroisoindole (Perhydroisoindole) is a substance P antagonist that can cross the blood-brain barrier and is useful for the study of movement disorders associated with central nervous system diseases .
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- HY-B0762S1
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O-Acetyl-L-carnitine-d3-1 (hydrochloride)
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Endogenous Metabolite
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Neurological Disease
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Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
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- HY-10814
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nAChR
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Neurological Disease
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CP-810123 is a brain-permeable agonist of α7 nAChR for the research of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease .
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- HY-160168
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- HY-120332
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KH176 hydrochloride
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Reactive Oxygen Species
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Metabolic Disease
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Sonlicromanol (KH176) hydrochloride, a chemical entity derivative of Trolox, is a blood-brain barrier permeable ROS-redox modulator. Sonlicromanol (KH176) hydrochloride is used in the study for mitochondrial disorders .
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- HY-153175
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RET
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Neurological Disease
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BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus .
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- HY-101349A
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Dopamine Receptor
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Neurological Disease
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L 741742 hydrochloride is an orally active and selective antagonist of hD4 receptors. L 741742 hydrochloride has a good brain penetration. L 741742 hydrochloride can be used in study nervous system disorders, particularly schizophrenia .
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- HY-10886
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Opioid Receptor
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Neurological Disease
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MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB is used in anxiety disorders research .
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- HY-116916
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Dopamine Receptor
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Neurological Disease
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Acetophenazine, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine primarily blocks dopamine D2 receptors in the brain. Acetophenazine can be used for researching psychotic disorders such as schizophrenia and anxious depression .
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- HY-B1237A
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil hydrochloride hydrochloride is an active agent against on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes. Suloctidil hydrochloride is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders.
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- HY-146101
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iGluR
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Neurological Disease
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NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research .
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- HY-100778
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Cannabinoid Receptor
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Neurological Disease
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SMM-189 is a potent and selective cannabinoid receptor 2 (CB2) inverse agonist. SMM-189 plays an important role in neurodegenerative disorders and traumatic brain injury research .
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- HY-B1237
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Na+/K+ ATPase
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Cardiovascular Disease
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Suloctidil is a new drug that is currently being evaluated in many clinical trials for use in dementia and thrombotic disorders
Target:
Effect of suloctidil on Na+/K+ ATPase activity and on membrane fluidity in rat brain synaptosomes.
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- HY-15722
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- HY-B1262
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Dopamine Receptor
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Neurological Disease
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Acetophenazine dimaleate, a phenothiazine derivative, is an antipsychotic agent. Acetophenazine dimaleate primarily blocks dopamine D2 receptors in the brain. Acetophenazine dimaleate can be used for researching psychotic disorders such as schizophrenia and anxious depression .
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- HY-B0762
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O-Acetyl-L-carnitine hydrochloride; ALCAR hydrochloride
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Endogenous Metabolite
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Neurological Disease
Cancer
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Acetyl-L-carnitine (O-Acetyl-L-carnitine) hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders .
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- HY-136660
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mTOR
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Neurological Disease
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PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders .
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- HY-131703
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UGT
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Metabolic Disease
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UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders .
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- HY-151797
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CaMK
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Neurological Disease
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Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .
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- HY-12495A
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Biochemical Assay Reagents
Eukaryotic Initiation Factor (eIF)
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Neurological Disease
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ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
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- HY-14880B
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JNJ31001074AAC; JNJ31001074 dihydrochloride hydrate
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Histamine Receptor
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Neurological Disease
Endocrinology
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Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research .
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- HY-14880A
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JNJ-31001074 dihydrochloride
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Histamine Receptor
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Neurological Disease
Endocrinology
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Bavisant (JNJ-31001074) dihydrochloride is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research .
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- HY-14880
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JNJ-31001074
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Histamine Receptor
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Neurological Disease
Endocrinology
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Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research .
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- HY-163671
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GPR52
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Neurological Disease
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PW0729 (compound 15b) is an orphan GPR52 agonist with potential applications in GPR52 activation, signaling bias, and neuropsychiatric and neurological disorders. The brain exposure characteristics of PW0729 need to be further optimized .
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- HY-B1395
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nAChR
Histamine Receptor
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Cardiovascular Disease
Neurological Disease
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Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
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- HY-B1395A
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nAChR
Histamine Receptor
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Cardiovascular Disease
Neurological Disease
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Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
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- HY-132845
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PTC857
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α-synuclein
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Neurological Disease
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Utreloxastat (PTC857) is a compound used for the research of the disorders including α-synucleinopathies, tauopathies, Amyotrophic lateral sclerosis (ALS), traumatic brain injury, and ischemic-reperfusion related injuries (patent WO2020081879A2, example A1) .
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- HY-152171
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Monoamine Transporter
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Neurological Disease
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GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .
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- HY-18678
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PT-141
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Melanocortin Receptor
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Endocrinology
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Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders .
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- HY-59201A
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nAChR
5-HT Receptor
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Neurological Disease
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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 .
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- HY-W016145
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Apoptosis
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Metabolic Disease
Cancer
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L-Glutamic acid monosodium hydrate is a nutritional additive and flavoring agent. L-Glutamic acid monosodium hydrate can reduce obesity and induce metabolic disorders associated with oxidative stress. L-Glutamic acid monosodium hydrate induces oxidative stress,DNA damage and apoptosis in the liver and brain tissues of mice .
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- HY-B2167R
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Endogenous Metabolite
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Neurological Disease
Cancer
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Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
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- HY-139464
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Nuclear Factor of activated T Cells (NFAT)
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Neurological Disease
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Q134R, a neuroprotective hydroxyquinoline derivative that suppresses nuclear factor of activated T cell (NFAT) signaling. Q134R can across blood-brain barrier. Q134R has the potential for Alzheimer's disease (AD) and aging-related disorders research .
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- HY-108683
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Orexin Receptor (OX Receptor)
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Neurological Disease
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ACT-335827 is a selective, orally active, brain-penetrant orexin type 1 receptor antagonist. ACT-33582 acts on OXR1 and OXR2 with IC50 values of 6 nM and 417 nM, respectively. ACT-33582 can be used in studies related to neurological disorders .
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- HY-E70395
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PE; PEP
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Biochemical Assay Reagents
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Neurological Disease
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Prolyl Endopeptidase, highly active in brain and other tissues, catabolizes proline-containing peptides such as substance P, neurotensin, luteinizing hormone-releasing hormone, thyrotropin releasing hormone, bradykinin and angiotensin II. Prolyl Endopeptidase can be used for study of neuropsychiatric diseases such as stress disorder, depression, and schizophrenia .
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- HY-162693
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-68 (compound 2l) is a potent and selective AChE inhibitor, with an IC50 value of 0.040 μM. AChE-IN-68 has high blood-brain barrier permeability. AChE-IN-68 can be used for the research of neurodegenerative disorders, particularly Alzheimer’s disease .
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- HY-144610
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Opioid Receptor
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Neurological Disease
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Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC50 value of 1.14 nM and a Ki value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .
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- HY-D0884
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(S)-2-Hydroxypropanoic acid lithium
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Biochemical Assay Reagents
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Others
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L-Lactic acid (lithium) is a chemical compound belonging to the class of lithium salts. It is commonly used in the pharmaceutical industry as a mood stabilizer and antipsychotic for the improvement of bipolar disorder and schizophrenia. L-Lactic acid (lithium) works by affecting the balance of certain chemicals in the brain, which can help reduce symptoms such as mood swings, aggression, and hallucinations.
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- HY-76201
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ICRF-187 hydrochloride; ADR-529 hydrochloride; NSC-169780 hydrochloride
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Others
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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Dexrazoxane hydrochloride (ICRF-187 hydrochloride) is a heart protectant that can help preserve ovarian function and fertility. Dexrazoxane hydrochloride has antioxidant and anti-inflammatory properties, can cross the blood-brain barrier, improves motor function disorders, and offers neuroprotective effects, making it useful in the study of neurodegenerative diseases .
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- HY-13999
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Others
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Neurological Disease
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NSI-189, benzylpiperizine-aminiopyridine, is a multi-domain neurogenic compound with brain-therapeutic properties. NSI-189 can stimulate neurogenesis of human hippocampus-derived neural stem cells in vitro and stimulates neurogenesis in murine hippocampus in vivo. NSI-189 can be used for the research of psychiatric disorders .
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- HY-B1395R
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nAChR
Histamine Receptor
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Cardiovascular Disease
Neurological Disease
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Mecamylamine (hydrochloride) (Standard) is the analytical standard of Mecamylamine (hydrochloride). This product is intended for research and analytical applications. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
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- HY-11044
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Histamine Receptor
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Neurological Disease
Inflammation/Immunology
Endocrinology
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PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms . PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD) .
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- HY-103493
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Phosphodiesterase (PDE)
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Neurological Disease
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TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment .
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- HY-18078
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Phosphodiesterase (PDE)
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Neurological Disease
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PQ-10 is a potent inhibitor of Phosphodiesterase 10A (PDE10A) with IC50 andED50 of 4.6 nM and 13 mg/kg, respectively. PQ-10 induces patterns of brain glucose metabolism which can be a potential translational biomarker. PQ-10 has the potential for researching psychiatric disorders like schizophrenia .
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- HY-120741
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Phosphodiesterase (PDE)
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Neurological Disease
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PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease .
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- HY-122347A
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GW823296 maleate
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Neurokinin Receptor
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Neurological Disease
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Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .
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- HY-106301
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L-364,718; MK-329
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Cholecystokinin Receptor
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Metabolic Disease
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Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
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- HY-114452
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BTRX-246040
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Opioid Receptor
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Neurological Disease
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LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
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- HY-114452A
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BTRX-246040 tartrate
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Opioid Receptor
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Neurological Disease
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LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
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- HY-117764
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mGluR
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Neurological Disease
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LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
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- HY-13340
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VU152100
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mAChR
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Neurological Disease
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VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
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- HY-B1395S1
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Isotope-Labeled Compounds
nAChR
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Neurological Disease
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Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
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- HY-10232
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THIP
1 Publications Verification
Gaboxadol
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GABA Receptor
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Neurological Disease
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THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 µM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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- HY-168028
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mGluR
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Neurological Disease
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mGluR2 modulator 5 (Compound 11) is an orally active, selective mGluR2 negative allosteric modulator with an IC50 of 8.9 nM. Pharmacokinetic studies in rats show that mGluR2 modulator 5 can effectively cross the blood-brain barrier. It can modulate cognitive and neurological functions in mood disorders and is suitable for research in the field of neurodegenerative diseases .
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- HY-B0688
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Dapsone
1 Publications Verification
4,4′-Diaminodiphenyl sulfone; DDS
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Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
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Infection
Inflammation/Immunology
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Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-148417
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Serotonin Transporter
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Neurological Disease
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ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD) .
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- HY-N8852
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6-MeOF
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GABA Receptor
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Neurological Disease
|
6-Methoxyflavanone (6-MeOF) is an orally active flavonoid compound. 6-Methoxyflavanone has anxiolytic properties. 6-Methoxyflavanone targets unique sites on GABA-A receptors, different from traditional benzodiazepines. 6-Methoxyflavanone can be used to study anxiety disorders. 6-Methoxyflavanone readily crosses the blood brain barrier (BBB) .
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-
- HY-W424918
-
|
Others
|
Neurological Disease
|
Opromazine hydrochloride is an antipsychotic medication that exhibits sedative and antiemetic pharmacological effects, making it effective for treating psychiatric disorders such as schizophrenia and psychosis. Opromazine hydrochloride functions by reducing dopaminergic activity through the blockade of dopamine receptors in the brain. Opromazine hydrochloride has been analyzed for its metabolites in various microsomal enzymes, revealing differences in formation rates that underscore the variability of drug-metabolizing enzymes in human liver and placenta microsomes.
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-
- HY-107664
-
|
Neurotensin Receptor
|
Neurological Disease
|
SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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-
- HY-107664A
-
|
Neurotensin Receptor
|
Neurological Disease
|
SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
|
-
- HY-B0113
-
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-W001601
-
|
iGluR
|
Neurological Disease
|
Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
|
-
- HY-B0113A
-
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-P5469
-
|
Formyl Peptide Receptor (FPR)
|
Others
|
WRW4-OH is a biological active peptide. (This peptide inhibits binding of one of formyl peptide receptor-like 1 (FPRL1) agonists WKYMVm to its specific receptor. FPRL1 is an important classical chemoattractant receptor that is expressed in phagocytic cells in the peripheral blood and brain. Activation of FPRL1 is closely related to inflammatory responses in the host defense mechanism and neurodegenerative disorders.)
|
-
- HY-W001601A
-
|
iGluR
|
Neurological Disease
|
Budipine hydrochloride is an anti-parkinson agent. Budipine hydrochloride also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine hydrochloride also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine hydrochloride can be used for the research of CNS disorders include Parkinson disease .
|
-
- HY-134188
-
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
|
-
- HY-150702
-
|
MAGL
|
Neurological Disease
Inflammation/Immunology
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
|
-
- HY-118858
-
|
EAAT
|
Neurological Disease
Cancer
|
UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
|
-
- HY-106644
-
FG4963 free acid
|
5-HT Receptor
|
Neurological Disease
|
Femoxetine is a serotonin (5-HT) inhibitor with antidepressant properties. Femoxetine increases serotonin levels in the brain by preventing serotonin from being reabsorbed by nerve cells, resulting in increased concentrations of the neurotransmitter in the synaptic gap, which enhances serotonin signaling. Femoxetine can be used to study the role of serotonin in depression and other emotional disorders, and how 5-HT reuptake inhibitors affect mood and behavior .
|
-
- HY-106644A
-
FG4963
|
5-HT Receptor
|
Neurological Disease
|
Femoxetine hydrochloride is a serotonin (5-HT) inhibitor with antidepressant properties. Femoxetine hydrochloride increases serotonin levels in the brain by preventing serotonin from being reabsorbed by nerve cells, resulting in increased concentrations of the neurotransmitter in the synaptic gap, which enhances serotonin signaling. Femoxetine hydrochloride can be used to study the role of serotonin in depression and other emotional disorders, and how 5-HT reuptake inhibitors affect mood and behavior .
|
-
- HY-14280S
-
|
COMT
|
Neurological Disease
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
- HY-W018643
-
Methyl ferulate
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties . Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders . Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages .
|
-
- HY-19918A
-
|
NF-κB
Amyloid-β
nAChR
|
Neurological Disease
Inflammation/Immunology
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
|
-
- HY-106301R
-
|
Cholecystokinin Receptor
|
Metabolic Disease
|
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-B0349
-
Meclozine dihydrochloride
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
|
-
- HY-B0349A
-
Meclozine
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
|
-
- HY-B0349B
-
Meclozine dihydrochloride monohydrate
|
Histamine Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
|
-
- HY-104044A
-
BGB-290 maleate
|
Others
|
Neurological Disease
|
Pamiparib maleate (BGB-290 maleate) is a highly potent and selective PARP inhibitor with neurotoxicity-inducing activity. Pamiparib maleate can effectively penetrate the blood-brain barrier and cause cerebral hemorrhage, brain atrophy, and movement disorders in zebrafish embryos exposed. Pamiparib maleate exposure downregulates the activities of acetylcholinesterase (AChE) and adenosine triphosphatase (ATPase) and leads to upregulation of oxidative stress, which triggers apoptosis and interferes with the expression of neurodevelopment-related genes. The use of pamiparib maleate is also accompanied by downregulation of the Notch signaling pathway, while activation of the Notch signaling pathway can partially rescue neurodevelopmental toxicity. Therefore, pamiparib maleate provides a reference for evaluating its potential neurotoxicity during embryonic development .
|
-
- HY-B0688S1
-
4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
|
-
- HY-128656
-
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
|
-
- HY-144607
-
|
Opioid Receptor
|
Neurological Disease
|
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
|
-
- HY-120124
-
SUVN-G3031
|
Histamine Receptor
|
Neurological Disease
|
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders .
|
-
- HY-148502
-
|
mAChR
|
Neurological Disease
|
VU6019650 is a potent and selective orthosteric antagonist of M5 mAChR (IC50=36 nM), can be used for opioid use disorder (OUD) relief. VU6019650 can cross blood brain barrier, potentially modulates the mesolimbic dopaminergic reward circuitry. VU6019650 blocks Oxotremorine M iodide (HY-101372A) induced increases of neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area (VTA) .
|
-
- HY-B0113R
-
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0688R
-
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
Dapsone (Standard) is the analytical standard of Dapsone. This product is intended for research and analytical applications. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-W001601R
-
|
iGluR
|
Neurological Disease
|
Budipine (Standard) is the analytical standard of Budipine. This product is intended for research and analytical applications. Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
|
-
- HY-10232S
-
Gaboxadol-d4
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
|
-
- HY-B0113S1
-
H 16868-d3-1
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-B0688S2
-
4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12
|
Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-N6948S
-
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0113S4
-
H 16868-d3 sodium
|
Autophagy
Phospholipase
Proton Pump
Bacterial
Isotope-Labeled Compounds
|
Infection
Metabolic Disease
Cancer
|
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-164485
-
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
INI-4001 is a TLR7/8 agonist, with EC50 values of 1.89 μM and 4.86 μM for TLR7/8, respectively. INI-4001 induces signaling and SEAP production through TLR7 and TLR8. INI-4001 promotes the generation of high-affinity, specific antibodies against fentanyl, preventing fentanyl from crossing the blood-brain barrier, making it an effective adjuvant for fentanyl vaccines in the opioid use disorder (OUD) population .
|
-
- HY-B0113S3
-
H 16868-13C,d3
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-122608
-
SUVN-G3031 free base
|
Histamine Receptor
|
Neurological Disease
|
Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders .
|
-
- HY-158030
-
|
HDAC
|
Neurological Disease
|
HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu 2+-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue .
|
-
- HY-14280
-
|
COMT
|
Neurological Disease
Cancer
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-14280A
-
|
COMT
|
Neurological Disease
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-147352
-
|
iGluR
|
Neurological Disease
|
NMDA receptor potentiator-1 (Compound 1368) is a subunit selective NMDA receptor potentiator with IC50s of 4 μM and 5 μM against NR2C and NR2D expression, respectively .
|
-
- HY-14280R
-
|
COMT
|
Neurological Disease
Cancer
|
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-151129
-
|
nAChR
|
Neurological Disease
|
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-107669
-
|
nAChR
|
Neurological Disease
|
nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-117046A
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
|
-
- 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-117993
-
|
Others
|
Neurological Disease
|
MIND4 is a novel thiozoline that was found to inhibit the deacetylase SIRT2 and to have neuroprotective activity in in vitro brain slices and Drosophila models of Huntington's disease (HD). A systems biology approach revealed another SIRT2-independent property of MIND4, namely as an inducer of nuclear factor erythroid 2 p45-derived factor 2 (NRF2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) that lacks SIRT2 inhibitory activity. MIND compounds induce NRF2 activation responses in both neuronal and non-neuronal cells and reduce the generation of reactive oxygen and nitrogen intermediates. These agent-like thiozolines offer exciting opportunities for the development of multi-target agents with potential synergistic therapeutic benefits for HD and related disorders.
|
-
- HY-12708
-
Chlorpromazine
Maximum Cited Publications
57 Publications Verification
|
Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
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Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
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- HY-B0407A
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Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
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HY-L028
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901 compounds
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The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 901 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
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HY-L0123V
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30,300 compounds
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The incidence and significance of central nervous system diseases are increasing at an alarming rate all over the world. Although substantial research efforts have been applied to develop new CNS-active drugs, only a few CNS disorders are addressed satisfactorily, while the remaining ones pose significant clinical challenges. Blood-brain barrier (BBB) permeability is one of the most important limiting factors in the design and development of novel CNS-targeted pharmaceuticals for the treatment of neurological disorders.
Carefully selected from the HTS Compound Collection to meet the parameters optimized for high BBB-permeability, our CNS Focused Screening Library comprising over 30,300 structurally-diverse and potentially CNS-active screening compounds. This original Screening Compound Library is aimed at supporting CNS drug design projects and HTS efforts in search for novel neurotherapeutics.
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Cat. No. |
Product Name |
Type |
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- HY-W250174
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3,5-Diiodosalicylic acid lithium salt
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Biochemical Assay Reagents
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Lithium 3,5-diiodosalicylate is a compound used in the study of bipolar disorder and other psychiatric disorders. It contains lithium and a salicylate. Lithium 3,5-diiodosalicylate works by affecting the levels of certain neurotransmitters in the brain, including dopamine and serotonin.
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- HY-12495A
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Cell Assay Reagents
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ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
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- HY-D0884
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(S)-2-Hydroxypropanoic acid lithium
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Biochemical Assay Reagents
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L-Lactic acid (lithium) is a chemical compound belonging to the class of lithium salts. It is commonly used in the pharmaceutical industry as a mood stabilizer and antipsychotic for the improvement of bipolar disorder and schizophrenia. L-Lactic acid (lithium) works by affecting the balance of certain chemicals in the brain, which can help reduce symptoms such as mood swings, aggression, and hallucinations.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-112173
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- HY-18678
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PT-141
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Melanocortin Receptor
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Endocrinology
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Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders .
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- HY-P5469
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Formyl Peptide Receptor (FPR)
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Others
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WRW4-OH is a biological active peptide. (This peptide inhibits binding of one of formyl peptide receptor-like 1 (FPRL1) agonists WKYMVm to its specific receptor. FPRL1 is an important classical chemoattractant receptor that is expressed in phagocytic cells in the peripheral blood and brain. Activation of FPRL1 is closely related to inflammatory responses in the host defense mechanism and neurodegenerative disorders.)
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-B0762
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- HY-W018643
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- HY-W017933
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- HY-B2167R
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
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Endogenous Metabolite
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Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0762S
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Acetyl-L-carnitine-d3 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
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- HY-B0762S1
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Acetyl-L-carnitine-d3-1 (hydrochloride) is the deuterium labeled Acetyl-L-carnitine hydrochloride. Acetyl-L-carnitine hydrochloride is a blood-brain permeable acetyl ester of the amino acid L-carnitine found in the body. Acetyl-L-carnitine hydrochloride is often used as a dietary supplement, and exibits anti-stress-related psychiatric disorders[1].
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- HY-14280S
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Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
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- HY-B0113S1
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Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-B1395S1
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Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
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- HY-B0688S1
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Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
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- HY-10232S
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THIP-d4 (Gaboxadol-d4) is the deuterium labeled THIP (HY-10232). THIP (Gaboxadol) is a selective extrasynaptic GABAA receptors (eGABARs) agonist (with blood-brain barrier permeability), shows an EC50 value of 13 μM for δ-GABAAR. THIP induces strong tense GABAA-mediated currents in layer 2/3 neurons, but shows on effect on miniature IPSCs. THIP can be used in studies of sleep disorders .
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- HY-B0688S2
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Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-N6948S
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Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S4
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Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S3
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Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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