Search Result
Results for "
peripherally active
" in MedChemExpress (MCE) Product Catalog:
20
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0484
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Buflomedil hydrochloride, a vasodilator agent, is an orally active α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. Buflomedil hydrochloride can be used for the study of peripheral circulatory disorders .
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-
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- HY-110206
-
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Cannabinoid Receptor
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Metabolic Disease
|
AM6545 is a highly selective, brain-free (peripherally active) CB1 receptor antagonist (Ki=1.7 nM). AM6545 inhibits endocannabinoid signaling by competitively antagonizing CB1 receptors, inhibiting CB1-mediated appetite stimulation and inflammatory responses without affecting cAMP levels. AM6545 significantly reduces food intake and body weight in mice, while improving metabolic syndrome-related renal impairment (such as proteinuria, fibrosis) and insulin resistance. AM6545 can be used in the study of obesity and its complications .
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-
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- HY-106538
-
-
-
- HY-116239
-
-
-
- HY-B0233
-
PN 200-110
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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-
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- HY-B0484A
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Buflomedil, a vasodilator agent, is an orally active α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. Buflomedil can be used for the study of peripheral circulatory disorders .
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-
-
- HY-B0484R
-
|
Adrenergic Receptor
|
Cardiovascular Disease
|
Buflomedil hydrochloride (Standard) is the analytical standard of Buflomedil hydrochloride (HY-B0484). This product is intended for research and analytical applications. Buflomedil hydrochloride (Standard), a vasodilator agent, is an orally active α1A-adrenoceptor antagonist with Kis of 4.06 µM and 6.84 µM for α1A-AR and α1B-AR, respectively. Buflomedil hydrochloride can be used for the study of peripheral circulatory disorders .
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-
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- HY-113826
-
|
Lipoxygenase
|
Others
|
L-656224 is an orally active, potent and selective inhibitor of leukotriene biosynthesis in intact rat and human leukocytes and CXBG mastocytoma cells (IC50 values, 18-240 nM) and of human leukocyte and porcine leukocyte 5-lipoxygenase (IC50, 4 x 10 -7 M). L-656224 is promising for research of asthma and peripheral analgesic agents .
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-
-
- HY-157527
-
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
|
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
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-
-
- HY-101733
-
-
-
- HY-B1895
-
-
-
- HY-119605
-
|
GABA Receptor
|
Neurological Disease
|
DAA-1097 is an orally active and selective agonist for the peripheral benzodiazepine receptor (PBR). DAA-1097 has anxiolytic effects .
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-
-
- HY-105266
-
-
-
- HY-107384
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EMD-61753
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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-
-
- HY-107384A
-
EMD-61753 hydrochloride
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
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-
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- HY-B0233S1
-
PN 200-110-d6
|
Calcium Channel
Autophagy
|
Neurological Disease
|
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
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-
-
- HY-B0233R
-
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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-
-
- HY-B0233S2
-
PN 200-110-d7
|
Calcium Channel
Autophagy
Isotope-Labeled Compounds
|
Cardiovascular Disease
Neurological Disease
|
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
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-
- HY-106147
-
|
Opioid Receptor
|
Neurological Disease
|
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system .
|
-
-
- HY-15283
-
Clopidogrelum
|
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
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-
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- HY-129787
-
|
Cannabinoid Receptor
|
Neurological Disease
|
PF-03550096 is an orally active synthetic cannabinoid (CB) that selectively targets peripheral CB2 receptors with a Ki value of 7.9 nM. PF-03550096 has analgesic activity .
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-
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- HY-106147B
-
|
Opioid Receptor
|
Neurological Disease
|
Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system .
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-
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- HY-B0233S
-
|
Calcium Channel
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].
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-
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- HY-B0259A
-
|
Potassium Channel
|
Cardiovascular Disease
|
Indapamide hemihydrate is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide hemihydrate is also can reduce left ventricular hypertrophy .
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-
-
- HY-B0259
-
|
Potassium Channel
|
Cardiovascular Disease
|
Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
|
-
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- HY-123239
-
|
GPR55
|
Neurological Disease
|
KLS-13019 is an orally active GPR55 receptor antagonist and a structural analogue of cannabidiol (CBD). It can prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rats .
|
-
-
- HY-B1895R
-
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
Levodropropizine (Standard) is the analytical standard of Levodropropizine. This product is intended for research and analytical applications. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
|
-
-
- HY-116477
-
|
FAAH
|
Neurological Disease
Inflammation/Immunology
|
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier) .
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-
-
- 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 .
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-
-
- HY-B0347
-
|
Calcium Channel
Reactive Oxygen Species
Caspase
Apoptosis
|
Cardiovascular Disease
|
Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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-
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- HY-125881
-
|
LPL Receptor
|
Inflammation/Immunology
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile .
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-
-
- HY-112707
-
|
Cannabinoid Receptor
5-HT Receptor
|
Neurological Disease
|
AM9405 is a novel peripherally active cannabinoid type 1 (CB1) and serotonin type 3 receptor agonist. AM9405 inhibits twitch contraction of the ileum and the colon with IC50s of 45.71 and 0.076 nM, respectively.
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-
-
- HY-B1895S1
-
-
-
- HY-108328
-
PF-04937319
|
Glucokinase
|
Neurological Disease
Metabolic Disease
|
Nerigliatin (PF-04937319) is a orally active glucokinase activator (GKA) with EC50 value of 154.4 μM. Nerigliatin maintains glucose-lowering efficacy. Nerigliatin causes peripheral nerve degeneration. Nerigliatin can be used in type 2 diabetes research.
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-
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- HY-108353
-
-
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- HY-118284
-
|
P2Y Receptor
|
Cardiovascular Disease
|
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease .
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-
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- HY-N7514
-
|
5-HT Receptor
|
Neurological Disease
|
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice .
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-
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- HY-108353A
-
-
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- HY-N12141
-
|
Apoptosis
|
Inflammation/Immunology
|
Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome .
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-
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- HY-B0259S3
-
|
Isotope-Labeled Compounds
Potassium Channel
|
Cardiovascular Disease
|
Indapamide-d6 is a deuterated labeled Indapamide . Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
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-
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- HY-B0468
-
Isoproterenol hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
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-
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- HY-15283R
-
|
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
Clopidogrel (Standard) is the analytical standard of Clopidogrel. This product is intended for research and analytical applications. Clopidogrel is an orally active platelet inhibitor that targets P2Y12 receptor. Clopidogrel is used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
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-
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- HY-B0259S
-
|
Isotope-Labeled Compounds
Potassium Channel
|
Cardiovascular Disease
|
(rac)-Indapamide-d3 is a labelled racemic Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy[1][4].
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-
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- HY-122968
-
NSD-1065
|
Endogenous Metabolite
|
Neurological Disease
|
Brocresine (NSD-1065) is an orally active histidine decarboxylase inhibitor and inhibits the formation of histamine from histidine. Brocresine is also a L-amino acid decarboxylase inhibitor with both a peripheral and central action. Brocresine inhibits gastric secretory response to administration of exogenous gastrin .
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-
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- HY-B0347S3
-
|
Calcium Channel
Caspase
Reactive Oxygen Species
Apoptosis
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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-
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- HY-B0347R
-
|
Calcium Channel
Reactive Oxygen Species
Caspase
Apoptosis
|
Cardiovascular Disease
|
Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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-
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- HY-B0347S1
-
|
Apoptosis
Caspase
Calcium Channel
Reactive Oxygen Species
|
Cardiovascular Disease
|
Lacidipine- 13C8 is the deuterium labeled Lacidipine[1]. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[2][3].
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-
-
- HY-17034B
-
MPV785
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
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-
-
- HY-B1382A
-
1,2,2,6,6-Pentamethylpiperidine hydrochloride
|
nAChR
|
Cardiovascular Disease
Neurological Disease
|
Pempidine (1,2,2,6,6-Pentamethylpiperidine) hydrochloride is an orally active ganglionic blocking agent used in the treatment of hypertension. Pempidine hydrochloride blocks the effects of intravenously administered addictive drugs and peripheral vagal nerve stimulation on blood pressure, and reduces the output of acetylcholine .
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-
-
- HY-16723A
-
(R)-TV 45070; (R)-XEN402
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
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- HY-17034
-
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Medetomidine is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine has sedative and analgesic effects. Medetomidine can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
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- HY-B0259R
-
|
Potassium Channel
|
Cardiovascular Disease
|
Indapamide (Standard) is the analytical standard of Indapamide. This product is intended for research and analytical applications. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
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-
- HY-N6857
-
|
NF-κB
|
Inflammation/Immunology
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
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- HY-B0259S1
-
|
Isotope-Labeled Compounds
Potassium Channel
|
Cardiovascular Disease
|
Indapamide- 13C,d3 is 13C and deuterium labeled Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
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- HY-B0362A
-
Phentolamine methanesulfonate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
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-
- HY-N4115
-
Su 3118
|
Monocarboxylate Transporter
|
Cardiovascular Disease
Cancer
|
Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine .
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- HY-B0464A
-
|
Reactive Oxygen Species
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Hydralazine is a orally active antihypertensive agent, reduces peripheral resistance directly by relaxing the smooth muscle cell layer in arterial vessel. Hydralazine has antioxidant activity, as well as inhibits reactive oxygen species (ROS) release and O2 ·- generation with an IC50 value of 9.53 mM and 1.19 mM, respectively .
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- HY-B0164A
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine dihydrochloride is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
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-
- HY-18977
-
KML29
2 Publications Verification
|
MAGL
|
Metabolic Disease
Inflammation/Immunology
|
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH .
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- HY-B0164
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
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-
- HY-127026S
-
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
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-
- HY-144126
-
|
LPL Receptor
|
Inflammation/Immunology
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS) .
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- HY-B0468S
-
Isoproterenol-d7 hydrochloride
|
Isotope-Labeled Compounds
Endogenous Metabolite
Adrenergic Receptor
|
Cardiovascular Disease
|
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- HY-17406
-
Ro 40-7592
|
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
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-
- HY-N3931
-
|
Others
|
Cardiovascular Disease
|
Gardneramine is an orally active alkaloid that acts like papaverine. Gardneramine has peripheral vascular diastolic effect, direct inhibition on myocardium and central inhibition. Gardneramine showed antihypertensive, vasodilatation and atrial inhibition effects in rabbit, dog and guinea pig models, respectively. Gardneramine also inhibits the movement of smooth muscle organs such as the stomach and intestines .
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-
- HY-150728
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .
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-
- HY-B0715
-
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-B0468R
-
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
Isoprenaline (hydrochloride) (Standard) is the analytical standard of Isoprenaline (hydrochloride). This product is intended for research and analytical applications. Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
- HY-B1451
-
TA-6366
|
Angiotensin-converting Enzyme (ACE)
MMP
|
Cardiovascular Disease
Metabolic Disease
|
Imidapril hydrochloride (TA-6366) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril hydrochloride suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril hydrochloride can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research .
|
-
- HY-B0010B
-
(±)Formoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
|
Formoterol ((±)Formoterol) is an orally active β2-selective agonist. Formoterol potently relaxes the peripheral airways through stimulating the beta 2-adrenoceptors selectively as is the case in the central airways and that it significantly inhibits IgE-mediated slow reactive substance of anaphylaxis (SRS-A) release through beta-adrenoceptor stimulation .
|
-
- HY-B1343
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
|
-
- HY-146662
-
|
PGE synthase
|
Inflammation/Immunology
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .
|
-
- HY-N6857R
-
|
NF-κB
|
Inflammation/Immunology
|
Armepavine (Standard) is the analytical standard of Armepavine. This product is intended for research and analytical applications. Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades .
|
-
- HY-107322
-
Mepirodipine hydrochloride; YM-09730-5
|
Calcium Channel
|
Cardiovascular Disease
|
Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-B1451A
-
TA-6366 free base
|
Angiotensin-converting Enzyme (ACE)
MMP
|
Cardiovascular Disease
Metabolic Disease
|
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research .
|
-
- HY-12717AS
-
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
Phentolamine-d4 (hydrochloride) is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction[1][2][3].
|
-
- HY-156961
-
|
JAK
|
Inflammation/Immunology
|
GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases .
|
-
- HY-149484
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BChE-IN-15 (Compound 6d) is an AChE/BChE inhibitor, with IC50s of 20 nM and 220 nM respectively. AChE/BChE-IN-15 binds to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active sites of AChE and BChE. AChE/BChE-IN-15 can be used for research of Alzheimer’s disease .
|
-
- HY-17034BS1
-
MPV785-13C,d3
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
|
Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
|
-
- HY-17583
-
-
- HY-B0362AR
-
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Phentolamine (mesylate) (Standard) is the analytical standard of Phentolamine (mesylate). This product is intended for research and analytical applications. Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
|
-
- 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-B0164R
-
|
Histamine Receptor
|
Inflammation/Immunology
|
Mizolastine (Standard) is the analytical standard of Mizolastine. This product is intended for research and analytical applications. Mizolastine is an orally active, high affinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
|
-
- HY-17391
-
|
Adenosine Receptor
|
Endocrinology
|
Pamabrom is a diuretic that acts on the opioid receptor-nitric oxide (NO) -cyclic guanosine monophosphate (cGMP) -K + channel pathway. Pamabrom exerts peripheral antinociceptive activity by activating this pathway. The mechanism involves activating opioid receptors, promoting the release of nitric oxide, and then influencing cyclic guanosine monophosphate and K channels to produce an analgesic effect. Pamabrom is orally active and is mainly used in the research and treatment of premenstrual syndrome and primary dysmenorrhea[1].
|
-
- HY-B0715S
-
BL-191-d6; PTX-d6; Oxpentifylline-d6
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
|
-
- HY-17406S1
-
Ro 40-7592-d4
|
Isotope-Labeled Compounds
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
|
-
- HY-B0715S2
-
BL-191-d5; PTX-d5; Oxpentifylline-d5
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
|
-
- HY-17406R
-
Ro 40-7592 (Standard)
|
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
Tolcapone (Standard) is the analytical standard of Tolcapone. This product is intended for research and analytical applications. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
|
-
- HY-B0715R
-
BL-191 (Standard); PTX (Standard); Oxpentifylline (Standard)
|
HIV
Autophagy
Phosphodiesterase (PDE)
|
Cardiovascular Disease
Cancer
|
Pentoxifylline (Standard) is the analytical standard of Pentoxifylline. This product is intended for research and analytical applications. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-B0715S3
-
BL-191-d3; PTX-d3; Oxpentifylline-d3
|
Isotope-Labeled Compounds
Autophagy
Phosphodiesterase (PDE)
HIV
|
Cardiovascular Disease
Cancer
|
Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
|
-
- HY-N15424
-
|
Apoptosis
Bcl-2 Family
|
|
Himachalol, a sesquiterpene, is an orally active antispasmodic and anticancer constituent found in the wood of Cedrus deodara. Himachalol has anti-proliferative activity against the melanoma cells, and induces apoptosis (decreases Bcl-2 level and increases Bax level). Himachalol has systemic hypotension and peripheral vasodilation effect. Himachalol inhibits Carbachol-induced spasm of the intestine. The LD50 of Himachalol in mice is 265 mg/kg (p.o.) and 247 mg/kg (i.p.) .
|
-
- HY-A0081
-
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-13106
-
EMA401; PD-126055; (S)-EMA400
|
Angiotensin Receptor
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-119980B
-
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-13106A
-
EMA401 sodium; PD-126055 sodium
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
Olodanrigan (EMA401) sodium is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. Olodanrigan sodium is under development as a neuropathic pain therapeutic agent. Olodanrigan sodium analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons .
|
-
- HY-119980
-
|
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-168214
-
|
Potassium Channel
|
Neurological Disease
|
Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally active agonist for KV7.2/7.3 channel (KCNQ2/3) with an EC50 of 1.03 μM. Kv7.2/Kv7.3 agonist 1 exhibits analgesic efficacy in mice chronic constriction injury (CCI) model and mice Streptozotocin (HY-13753)-induced diabetic peripheral neuropathic pain (DPNP) model, with ED50 of 12.02 and 9.63 mg/kg .
|
-
- HY-155995
-
MK-905
|
Biochemical Assay Reagents
|
Cancer
|
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
|
-
- HY-119980BS
-
|
Isotope-Labeled Compounds
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Neurological Disease
Cancer
|
Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980A
-
|
Dopamine Receptor
Sodium Channel
SARS-CoV
|
Infection
Neurological Disease
Cancer
|
Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-119980S
-
|
Isotope-Labeled Compounds
Sodium Channel
Dopamine Receptor
SARS-CoV
|
Others
|
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-14280A
-
|
COMT
|
Neurological Disease
Cancer
|
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-A0081R
-
|
Dopamine Receptor
SARS-CoV
Sodium Channel
|
Neurological Disease
Cancer
|
Fluphenazine (dihydrochloride) (Standard) is the analytical standard of Fluphenazine (dihydrochloride). This product is intended for research and analytical applications. Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
|
-
- HY-136208
-
|
Opioid Receptor
|
Neurological Disease
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
|
-
- 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-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-13224A
-
|
Endogenous Metabolite
|
Cancer
|
AZD4877 hydrochloride is a synthetic dynein inhibitor with potential anti-tumor activity. AZD4877 selectively inhibits the microtubule dynein KSP (also known as kinesin-5 or Eg5), which may lead to inhibition of mitotic spindle assembly. The action of AZD4877 may activate the spindle assembly checkpoint, leading to cell cycle arrest at the mitotic stage. AZD4877 may induce cell death in actively dividing tumor cells. AZD4877 may be less likely to cause peripheral neuropathy associated with microtubule-targeted compounds as it is not involved in post-mitotic processes. AZD4877 is essential for the formation of bipolar spindles and the proper segregation of sister chromosomes .
|
-
- 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 .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- 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.)
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0233S1
-
|
Isradipine-d6 is the deuterium labeled Isradipine[1]. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[2][3][4].
|
-
-
- HY-B0233S2
-
|
Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease .
|
-
-
- HY-B0233S
-
|
Isradipine-d3 (PN 200-110-d3) is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease[1][2][3].
|
-
-
- HY-B1895S1
-
|
Levodropropizine-d5 ((S)-(-)-Dropropizine-d5) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
|
-
-
- HY-B0259S3
-
|
Indapamide-d6 is a deuterated labeled Indapamide . Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
|
-
-
- HY-B0259S
-
|
(rac)-Indapamide-d3 is a labelled racemic Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy[1][4].
|
-
-
- HY-B0347S3
-
|
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
-
- HY-B0347S1
-
|
Lacidipine- 13C8 is the deuterium labeled Lacidipine[1]. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[2][3].
|
-
-
- HY-B0259S1
-
|
Indapamide- 13C,d3 is 13C and deuterium labeled Indapamide. Indapamide is an orally active sulphonamide diuretic agent, that can reduce blood pressure by decreasing vascular reactivity and peripheral vascular resistance. Indapamide is also can reduce left ventricular hypertrophy .
|
-
-
- HY-127026S
-
|
Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
|
-
-
- HY-B0468S
-
|
Isoprenaline-d7 (hydrochloride) is a deuterated labeled Isoprenaline (hydrochloride) . Isoprenaline (Isoproterenol) hydrochloride is a non-selective, orally active β-adrenergic receptor agonist. Isoprenaline has potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities. Isoprenaline can be used for the research of bradycardia and bronchial asthma .
|
-
-
- HY-12717AS
-
|
Phentolamine-d4 (hydrochloride) is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction[1][2][3].
|
-
-
- HY-17034BS1
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Medetomidine-13C,d3 (hydrochloride) is a deuterated labeled Medetomidine (hydrochloride) . Medetomidine hydrochloride is an orally active α2-adrenoceptor agonist (Ki: 1.08 nM). Medetomidine hydrochloride has sedative and analgesic effects. Medetomidine hydrochloride can cause peripheral vasoconstriction through the activation of α2 adrenoceptors on blood vessels .
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- HY-B0715S
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Pentoxifylline-d6 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
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- HY-17406S1
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Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
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- HY-B0715S2
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Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
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- HY-B0715S3
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Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation .
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- HY-119980BS
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Fluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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- HY-119980S
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Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
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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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