Search Result
Results for "
arterial smooth muscle
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Nombre del producto |
Target |
Áreas de investigación |
Chemical Structure |
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- HY-B0464
-
|
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PGE synthase
NO Synthase
Reactive Oxygen Species (ROS)
DNA Methyltransferase
COX
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Cardiovascular Disease
Inflammation/Immunology
Cancer
|
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Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
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- HY-A0033
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Darifenacin
Maximum Cited Publications
7 Publications Verification
UK-88525
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mAChR
p38 MAPK
Akt
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Neurological Disease
Metabolic Disease
Cancer
|
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Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
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- HY-A0012
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UK-88525 hydrobromide
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mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
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Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
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- HY-16693
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Glutaminase
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Cardiovascular Disease
Others
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LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease .
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- HY-B1107
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Nafronyl oxalate salt
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5-HT Receptor
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Cardiovascular Disease
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Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT2 receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT2 receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia .
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- HY-B0464A
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DNA Methyltransferase
Reactive Oxygen Species (ROS)
COX
NO Synthase
PGE synthase
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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Hydralazine is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
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- HY-P1636
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Thrombin
YAP
Calcium Channel
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Metabolic Disease
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Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
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- HY-11095
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mGluR
CaSR
PI3K
Akt
mTOR
Autophagy
Apoptosis
Bcl-2 Family
Caspase
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Cardiovascular Disease
Neurological Disease
|
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NPS 2390 is an allosteric antagonist of calcium-sensing receptor (CaSR) and mGluR1/5. NPS 2390 inhibits the PI3K/Akt/mTOR signaling pathway, reduces hypoxia-induced intracellular calcium elevation, decreases the expression of autophagy (autophagy) proteins, regulates the expression of phenotypic marker proteins, and inhibits the proliferation of pulmonary artery smooth muscle cells. NPS 2390 attenuates the endogenous apoptosis (apoptosis) pathway, increases the expression level of Bcl-2, downregulates the expression levels of Bax, cytochrome c and caspase-3, alleviates cerebral edema and improves neurological function in rat models. NPS 2390 can be used in studies related to hypoxic pulmonary hypertension, traumatic brain injury, stroke and pain .
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- HY-155106
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PKG
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Cardiovascular Disease
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SMA4 is a selective PKG1α activator with basal EC50 value of 29 μM. SMA4 facilitates phosphorylation of the known PKG1 substrate, vasodilator-stimulated phosphoprotein (VASP), and inhibits human pulmonary arterial smooth muscle cells (hPASMC) proliferation. SMA4 can be used for cardiovascular disease research .
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- HY-W153159
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Adrenergic Receptor
|
Inflammation/Immunology
|
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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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- HY-B0464S1
-
|
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Isotope-Labeled Compounds
PGE synthase
NO Synthase
Reactive Oxygen Species (ROS)
DNA Methyltransferase
COX
|
Cancer
|
|
Hydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
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-
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- HY-B0464S
-
|
|
Isotope-Labeled Compounds
PGE synthase
NO Synthase
Reactive Oxygen Species (ROS)
DNA Methyltransferase
COX
|
Cardiovascular Disease
|
|
Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
|
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- HY-W507009
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|
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Endogenous Metabolite
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Cardiovascular Disease
|
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L-Arginyl-L-alanine is a dipeptide, is a vascular smooth muscle-derived relaxing factor. L-Arginyl-L-alanine increases the smooth muscle levels of cyclic GMP and nitrite in endothelium-denuded arterial rings .
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- HY-119291
-
|
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Phosphodiesterase (PDE)
|
Others
|
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RA642 is a compound with vasodilatory and hypertensive effects, with the activity of increasing arterial blood pressure, enhancing cerebral blood flow, reducing cerebrovascular resistance and peripheral resistance, and having a papaverine-like relaxant effect on smooth muscle in anesthetized animals.
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- HY-172522
-
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Biochemical Assay Reagents
|
Cardiovascular Disease
|
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(±)11(12)-DiHET can be converted to a metabolite – 7,8-dihydroxy-hexadecadienoic acid (DHHD). (±)11(12)-DiHET is able to produce relaxation in porcine coronary artery rings. (±)11(12)-DiHET can be studied in research about arterial smooth muscle metabolism .
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- HY-W436495
-
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6,15-Diketo-13,14-dihydro-PGF1α
|
Drug Metabolite
|
Metabolic Disease
|
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6,15-Diketo-13,14-dihydro prostaglandin F1α (6,15-Diketo-13,14-dihydro-PGF1α) is a metabolite of prostacyclin (PGI2). 6,15-Diketo-13,14-dihydro prostaglandin F1α enhances intracellular cAMP and cholesterol metabolism in bovine arterial smooth muscle cells .
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- HY-171469
-
|
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Potassium Channel
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Cardiovascular Disease
|
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SKP-451 is an ATP-sensitive potassium (K +) channel agonist. SKP-451 activates the ATP-sensitive K + channels, promotes the efflux of K +, causes membrane hyperpolarization, and inhibits the influx of Ca 2+, thereby relaxing the vascular smooth muscle. SKP-451 relaxs the canine coronary artery, rabbit basilar artery, and vertebral artery. SKP-451 also reduces the mean arterial blood pressure of conscious spontaneously hypertensive rats (SHR). SKP-451 is promising for research of cardiovascular diseases .
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- HY-A0012R
-
|
UK-88525 hydrobromide (Standard)
|
Reference Standards
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
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- HY-B0464R
-
|
|
Reference Standards
PGE synthase
NO Synthase
Reactive Oxygen Species (ROS)
DNA Methyltransferase
COX
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Cardiovascular Disease
Inflammation/Immunology
Cancer
|
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Hydralazine (hydrochloride) (Standard) is the analytical standard of Hydralazine (hydrochloride). This product is intended for research and analytical applications. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
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- HY-114986
-
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6-keto-Prostaglandin E1
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β-glucuronidase
|
Cardiovascular Disease
|
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6-Keto-PGE1 (6-keto-Prostaglandin E1) is a biologically active derivative of PGE1. 6-Keto-PGE1 inhibits adenosine diphosphate-induced platelet aggregation. 6-Keto-PGE1 reduces cardiac afterload, decreases the accumulation of plasma myocardial depressant factor (MDF), lowers arterial blood pressure, dilates vascular beds, inhibits the vasoconstrictive response of vascular smooth muscle, and increases pulmonary compliance. 6-Keto-PGE1 directly stabilizes isolated cat liver lysosomes and significantly reduces the release of β-glucuronidase and cathepsin D. 6-Keto-PGE1 prolongs the survival time of traumatized rats and exerts protective effects through hemodynamic and cytoprotective actions. 6-Keto-PGE1 reduces central airway resistance. 6-Keto-PGE1 can be used in studies related to traumatic shock .
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- HY-182573
-
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
|
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RWJ-58259 is a selective PAR-1 inhibitor with an IC50 value of 0.15 μM. RWJ-58259 binds selectively to PAR-1, blocks the binding of tethered ligands, interferes with calcium mobilization and PAR-1-related cellular functions, and exhibits no PAR-1 agonist activity or thrombin proteolytic inhibitory activity. RWJ-58259 inhibits thrombin-induced platelet aggregation, calcium signaling and vascular smooth muscle cell proliferation, reduces neointimal thickness and arterial stenosis, and alleviates vascular occlusion and platelet deposition. RWJ-58259 can be used in the research of thrombotic diseases and vascular injury associated with acute coronary intervention .
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- HY-183644
-
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Lysyl Oxidase
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Cardiovascular Disease
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LNO 9 is an orally active LOXL2 inhibitor and NO donor, with an IC50 of 0.17 μM against human LOXL2. LNO 9 competitively binds to the LTQ cofactor of LOXL2 to form an irreversible complex, thereby inhibiting collagen oxidation and abnormal cross-linking. LNO 9 releases nitric oxide (NO) to increase cGMP levels in pulmonary artery smooth muscle cells. LNO 9 inhibits hypoxia-induced collagen modification and possesses vasodilatory activity. LNO 9 ameliorates right ventricular hypertrophy and pulmonary artery medial thickness in rat models induced by hypoxia and Monocrotaline (HY-N0750), and can be used for research on pulmonary hypertension .
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- HY-182616
-
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β-glucuronidase
Glycosidase
Phosphatase
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Inflammation/Immunology
|
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CH-123 is an orally active lipid-lowering agent. CH-123 inhibits the elevated activities of β-glucuronidase, β-galactosidase, N-acetyl-β-glucosaminidase and acid phosphatase in aortic smooth muscle cells and hepatocytes. CH-123 reduces serum total lipid and cholesterol levels, as well as intracellular cholesterol content in aortic smooth muscle cells. CH-123 significantly inhibits lysosomal enzyme activity. CH-123 can be used in the research of atherosclerosis .
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- HY-183907
-
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Calcium Channel
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Cardiovascular Disease
|
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Cicletanine is a voltage-dependent Ca 2+ channel inhibitor. Cicletanine inhibits α-adrenoceptor-mediated Ca 2+ release pathway, and shows vasodilatory effects on isolated vascular smooth muscle. Cicletanine directly stimulates lysosomal and cytoplasmic cholesteryl ester hydrolase activity. Cicletanine can be used for the research of hypertension .
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-
| Cat. No. |
Nombre del producto |
Target |
Research Area |
-
- HY-P1636
-
|
|
Thrombin
YAP
Calcium Channel
|
Metabolic Disease
|
|
Hirudin (54-65) is a thrombin antagonist and YAP suppressor with anticoagulatory properties.Hirudin (54-65) blocks thrombin's anion binding site, acts on soluble and thrombus-bound thrombin.Hirudin (54-65) suppresses thrombin-induced profibrotic YAP activity, reduces YAP expression, nuclear translocation, and downstream effector signaling in vascular endothelial cells.Hirudin (54-65) ameliorates obstructive cholestasis, attenuates liver fibrosis symptoms, fibrosis-associated angiogenesis, and endothelial-to-mesenchymal transition.Hirudin (54-65) reduces liver inflammation and tissue hypoxia.Hirudin (54-65) promotes extracellular calcium influx through L-type calcium channels in canine coronary artery smooth muscle, mediates contraction.Hirudin (54-65) induces endothelium-independent contraction of canine coronary arterial segments; this response is not affected by indomethacin pretreatment.Hirudin (54-65) can be used for the research of liver obstructive cholestasis, liver fibrosis .
|
| Cat. No. |
Nombre del producto |
Category |
Target |
Chemical Structure |
-
- HY-W153159
-
|
|
Structural Classification
Alkaloids
Monophenols
Other Alkaloids
Gramineae
Phenols
Plants
Hordeum distichon L.
Source Classification
|
Adrenergic Receptor
|
|
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 .
|
-
| Cat. No. |
Nombre del producto |
Chemical Structure |
-
- HY-B0464S1
-
|
|
|
Hydralazine-d5 (hydrochloride) is deuterium-labeled Hydralazine (hydrochloride) (HY-B0464). Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
|
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-
- HY-B0464S
-
|
|
|
Hydralazine-d4 hydrochloride is the deuterium labeled Hydralazine hydrochloride. Hydralazine hydrochloride is an orally active, blood-brain barrier-permeable DNA methyltransferase inhibitor with vasodilatory, arterial smooth muscle relaxant and hypotensive activities. Hydralazine hydrochloride reactivates silenced tumor suppressor genes via mediating DNA demethylation, while exerting neuroprotective and anti-inflammatory properties. Hydralazine hydrochloride inhibits NOS-2 (iNOS) and COX-2, and reduces the production of NO and PGEE2; meanwhile, Hydralazine hydrochloride scavenges reactive oxygen species and inhibits macrophage activation. Hydralazine hydrochloride alleviates motor dysfunction, neuropathic inflammatory pain, and formalin-induced somatic and emotional pain responses. In addition, Hydralazine hydrochloride directly induces DNA strand breaks and sister chromatid exchange, exhibiting certain mutagenic characteristics. Hydralazine hydrochloride has been widely used in studies on hypertension, various cancers (such as cervical cancer, leukemia), spinal cord injury and the mechanisms of inflammatory pain .
|
-
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