841 Results for "

peripherally

" in MedChemExpress (MCE) Product Catalog:
Products (841)

841 Results for "peripherally" in MCE Product Catalog:

Cat. No.: HY-W027553
CAS No.: 62732-44-9
Synonyms: NIK-247 free base; Amiridine free base
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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Cat. No.: HY-W153159
CAS No.: 13062-76-5
N-Methyltyramine hydrochloride is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine hydrochloride blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine hydrochloride promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine hydrochloride relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine hydrochloride can be used in studies related to gastrointestinal diseases .
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Cat. No.: HY-W153897
CAS No.: 370-98-9
N-Methyltyramine is an orally active α2-adrenoreceptor antagonist with an IC50 value of 5.53 μM against rat targets. N-Methyltyramine blocks α2-adrenoreceptors, while inhibiting lipolysis, hyperactivity responses and small intestinal peristalsis in mice. N-Methyltyramine promotes gastrin release and pancreatic juice secretion, upregulates appetite, blood pressure, myocardial contraction frequency and contraction intensity, and increases renal blood flow, renal vascular resistance and mean peripheral arterial resistance. N-Methyltyramine relaxes mouse small intestinal smooth muscle and undergoes biotransformation in vivo to produce adrenaline. N-Methyltyramine can be used in studies related to gastrointestinal diseases .
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Cat. No.: HY-W583212
CAS No.: 14354-67-7
Synonyms: ZnMP
Zn (II) Mesoporphyrin IX (ZnMP) is a heme oxygenase inhibitor with photochemical substrate activity. Zn (II) Mesoporphyrin IX specifically inhibits the activity of bone marrow heme oxygenase. In vitro, Zn (II) Mesoporphyrin IX inhibits the growth of erythroid and myeloid progenitor cells in rabbit bone marrow, and blocks the rhG-CSF-induced mobilization of these progenitor cells into the peripheral blood, exhibiting toxicity to hematopoietic growth and progenitor cell production in rabbits. Zn (II) Mesoporphyrin IX undergoes irreversible photochemical decomposition conforming to first-order kinetic characteristics when irradiated with UV-B in 95% ethanol solution. Zn (II) Mesoporphyrin IX can be used in hematopoietic regulation research, but its photolability and toxic effects on the hematopoietic system require attention .
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Cat. No.: HY-L149
7,999 compounds

A membrane protein is a protein molecule that is attached to or associated with the membrane of a cell or an organelle. Membrane proteins can be classified into two groups based on how the protein is associated with the membrane: integral membrane proteins and peripheral membrane proteins. In humans, about 30% genome encodes membrane proteins. Membrane proteins perform a variety of functions vital to the survival of organisms, for example, signal transduction, molecules or ion transportation, enzymatic catalysis, and intercellular communication. Membrane proteins also play important roles in drug discovery. As reported, more than 60% of current drug targets are membrane proteins.

MCE supplies a unique collection of 7,999 compounds targeting a variety of membrane proteins. MCE Membrane Protein-targeted Compound Library can be used for membrane protein-focused screening and drug discovery.

Cat. No.: HY-101036R
CAS No.: 87-67-2
Choline bitartrate (Standard) is the analytical standard of Choline bitartrate (HY-101036). This product is intended for research and analytical applications. Choline bitartrate is an orally active methylxanthine-derived choline salt of theophylline. Choline bitartrate exhibits weak antihistaminic and anticholinergic activities and can enhance the effects of histamine and acetylcholine. Choline bitartrate relaxes bronchial smooth muscle, dilates coronary and peripheral blood vessels, increases urine output and electrolyte excretion, stimulates central nervous system motor activity, and induces transient hypotension following a pressor phase. Choline bitartrate modulates sleep architecture by increasing wakefulness time and reducing slow-wave sleep, without altering the frequency or severity of nocturnal hypoxemia, apnea, or hypopnea events. Choline bitartrate is used in studies of bronchospasm, nocturnal asthma, and chronic asthma .
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Cat. No.: HY-106224AS
Synonyms: Hypocretin-1-13C6,15N (human, rat, mouse) TFA
Orexin A- 13C6, 15N (human, rat, mouse) (Hypocretin-1- 13C6, 15N (human, rat, mouse)) TFA is the 13C- and 15N-labeled Orexin A (human, rat, mouse) (HY-106224). Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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Cat. No.: HY-107111R
CAS No.: 932373-87-0
Research Areas:  

Neurological Disease

GSK1034702 (Standard) is the analytical standard of GSK1034702 (HY-107111). This product is intended for research and analytical applications. GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .
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Cat. No.: HY-121186
CAS No.: 42864-78-8
Purity:  98.98%
Synonyms: SOM3355
Bevantolol hydrochloride (SOM3355) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol hydrochloride blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol hydrochloride reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol hydrochloride is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
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Cat. No.: HY-132184S
CAS No.: 1881277-30-0
Synonyms: 5,6-EET-d11; (±)5,6-EpETrE-d11
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid is one of the four major epoxyeicosatrienoic acid (EET) isomers metabolized from Arachidonic acid (HY-109590). 5,6-Epoxyeicosatrienoic acid induces peripheral vasodilation and lowers blood pressure by inhibiting T-type calcium channels (Cav3.2: IC50 = 0.54 μM). 5,6-Epoxyeicosatrienoic acid causes vasoconstriction in hypoxic pulmonary blood vessels via activating Rho kinase in a membrane depolarization-dependent manner. 5,6-Epoxyeicosatrienoic acid induces mechanical pain by activating TRPA1. 5,6-Epoxyeicosatrienoic acid can be used in studies related to hypoxic pulmonary vasoconstriction, mechanical hyperalgesia and hypertension.
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Cat. No.: HY-14229R
CAS No.: 1197300-24-5
Synonyms: CCDC (Standard)
TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
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Cat. No.: HY-155297
CAS No.: 55248-23-2
Synonyms: FLA-136
Target:  

Histamine Receptor

Research Areas:  

Cardiovascular Disease

Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
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Cat. No.: HY-179047
CAS No.: 3040320-18-8
SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 +T cells. SMU-L11-R shows potential in colorectal cancer studies .
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Cat. No.: HY-182060
CAS No.: 3064814-26-9
PDE4B/D-IN-5 (Compound P32) is a peripherally restricted, oral active inhibitor of PDE4B and PDE4D with extremely low blood-brain barrier penetration, with IC50 values of 3.4 nM and 2.2 nM, respectively. PDE4B-IN-8 inhibits the production of TNF-α. PDE4B/D-IN-5 significantly reduces the Bax/Bcl2 ratio, and alleviates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. PDE4B/D-IN-5 can be used for the research of acute lung injury .
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Cat. No.: HY-187618
CAS No.: 1508276-29-6
Target:  

TRP Channel

Research Areas:  

Metabolic Disease

GRC-17536 is a TRPA1 antagonist with selective inhibition of TRPA1-mediated calcium influx .GRC-17536 binds to TRPA1 binding site 2 to inhibit channel activity .GRC-17536 reduces irritant-induced cough responses and citric acid-induced cough responses .GRC-17536 exhibits antitussive activity .GRC-17536 has poor pharmacokinetic and bioavailability properties, leading to discontinued development after a Phase IIa study .GRC-17536 can be used for the research of painful diabetic polyneuropathy, peripheral diabetic neuropathy, asthma, and chronic cough .
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Cat. No.: HY-19689
CAS No.: 90043-86-0
Synonyms: NIK-247; Amiridine
Ipidacrine (NIK-247; Amiridine) hydrochloride is orally active and blood-brain-barrier-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 hydrochloride has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine hydrochloride is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine hydrochloride is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine hydrochloride 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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Cat. No.: HY-A0249
CAS No.: 59170-23-9
Synonyms: SOM3355 free base
Bevantolol (SOM3355 (free base)) is a selective β1-adrenergic receptor antagonist, with an IC50 of 35 nM for β1-adrenergic receptor and an IC50 of 60 nM for VMAT2. Bevantolol blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease .
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Cat. No.: HY-B0551AR
CAS No.: 7081-53-0
Doxapram hydrochloride hydrate (Standard) is the analytical standard of Doxapram hydrochloride hydrate (HY-B0551A). This product is intended for research and analytical applications. Doxapram hydrochloride hydrate is a respiratory stimulant. Doxapram hydrochloride hydrate increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram hydrochloride hydrate inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram hydrochloride hydrate significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram hydrochloride hydrate can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity.
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Cat. No.: HY-B0551S
Doxapram-d8 is deuterated labeled Doxapram (HY-B0551). Doxapram is a respiratory stimulant. Doxapram increases breathing rate and depth by acting on the brain's respiratory centers and peripheral chemoreceptors. Doxapram inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50s of 410 nM, 37 μM, 9 μM, respectively. Doxapram inhibits the Ca²⁺-activated potassium current (IC50 ≈ 13 μM) and Ca²⁺-independent potassium current (IC50 ≈ 20 μM) in type I cells of the carotid body. Doxapram significantly prolongs the effective refractory period of the atrium and has an anti-arrhythmic effect. Doxapram can be used for the study of respiratory depression such as post-anesthesia respiratory depression, chronic obstructive pulmonary disease and apnea of prematurity.
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Cat. No.: HY-B1016R
CAS No.: 15421-84-8
Synonyms: AR-12008 (Standard)
Trapidil (Standard) (AR-12008 (Standard)) is the analytical standard of Trapidil (HY-B1016R). This product is intended for research and analytical applications. Trapidil (AR-12008) is an orally active vasodilator and antiplatelet agent. Trapidil antagonizes platelet-derived growth factor (PDGF), inhibits phosphodiesterase, thromboxane A2 synthesis and pro-inflammatory cytokine production. Trapidil promotes prostacyclin biosynthesis, reduces lipid peroxidation, regulates nitric oxide metabolism, and inhibits cell proliferation and migration. Trapidil exerts tissue-protective effects, regulates bone turnover, and inhibits pyroptosis via the GPX3/Nrf2 pathway. Trapidil is applicable to research related to renal ischemia-reperfusion injury, chronic stable angina, restenosis, meningioma, diabetic cardiomyopathy and peripheral nerve crush injury.
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