eNOS
eNOS (NOS3) generates endothelial nitric oxide (NO), a vasoprotective signal that regulates vascular tone, blood pressure, platelet aggregation, leukocyte adhesion, and vascular homeostasis[1][2]. Mechanistically, Akt/PKB activates eNOS through Ser1177 phosphorylation, while agonist-stimulated endothelial cells integrate Ser1177 activation with Thr495 regulation to control NO output[3]. In disease models, eNOS loss or inhibition reduces endothelial NO signaling and increases blood pressure, as shown in eNOS-deficient mice and L-arginine/NOS inhibitor studies[4][5][6]. Compared with related isoforms, eNOS is mostly expressed in endothelial cells, nNOS mediates neuronal signaling, and iNOS produces high-output NO during inflammatory activation[1]. For experimental applications, L-NMMA, L-NIO, and L-NAME inhibit NOS activity and provide pharmacological tools to test endothelial NO-dependent vascular responses[6].
References:
- [1]. Förstermann U, et al. Nitric oxide synthases: regulation and function. Eur Heart J. 2012 Apr;33(7):829-37, 837a-837d. [Content Brief]
- [2]. Förstermann U, et al. Endothelial nitric oxide synthase in vascular disease: from marvel to menace. Circulation. 2006 Apr 4;113(13):1708-14. [Content Brief]
- [3]. Fleming I, et al. Phosphorylation of Thr(495) regulates Ca(2+)/calmodulin-dependent endothelial nitric oxide synthase activity. Circ Res. 2001 Jun 8;88(11):E68-75. [Content Brief]
- [4]. Huang PL, et al. Hypertension in mice lacking the gene for endothelial nitric oxide synthase. Nature. 1995 Sep 21;377(6546):239-42. [Content Brief]
- [5]. Shesely EG, et al. Elevated blood pressures in mice lacking endothelial nitric oxide synthase. Proc Natl Acad Sci U S A. 1996 Nov 12;93(23):13176-81. [Content Brief]
- [6]. Rees DD, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo. Br J Pharmacol. 1990 Nov;101(3):746-52. [Content Brief]
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eNOS Related Products (40)
Related Products (40)
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1,4-PBIT dihydrobromide
0 ImagesSynonyms: 1,4-PB-ITU dihydrobromide
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AVE-9488
0 ImagesAVE-9488 is an eNOS enhancer with the activity of protecting the heart from ischemia-reperfusion injury. AVE-9488 can upregulate eNOS expression, increase NO production, reduce myocardial ischemia-reperfusion injury, and reduce the level of reactive oxygen species.
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MRS2768 tetrasodium salt
0 ImagesMRS2768 tetrasodium salt is a potent, selective, and metabolically stable P2Y2 receptor agonist with an EC50 of 1.89 μM for the human P2Y2 receptor. MRS2768 tetrasodium salt activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 tetrasodium salt inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 tetrasodium salt activates eNOS to increase NO secretion in endothelial cells. MRS2768 tetrasodium salt drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 tetrasodium salt exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 tetrasodium salt can be applied to investigate P2Y2-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.
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eNOS activator-1
0 ImagesCat. No.: HY-189214eNOS activator-1 is an orally active, blood-brain barrier permeable endothelial nitric oxide synthase (eNOS) activator. eNOS activator-1 upregulates eNOS mRNA expression, enhances endogenous NO biosynthesis, and activates the eNOS signaling pathway to maintain blood-brain barrier integrity. eNOS activator-1 upregulates the protein expression levels of PI3K, AKT, p-PI3K, and p-AKT. eNOS activator-1 reduces oxidative stress levels by decreasing lipid peroxidation and restoring antioxidant enzyme activities. eNOS activator-1 upregulates the expression of tight junction proteins ZO-1 and occludin, increases Cav-1 expression, and inhibits MMP-9-mediated blood-brain barrier disruption. eNOS activator-1 can be used in the research of ischemic stroke.
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δ-Viniferin
0 ImagesCat. No.: HY-N3841ACAS No.: 681293-15-2δ-Viniferin is a COX-1/COX-2 inhibitor (with an IC50 of 5 µM for both enzymes). δ-Viniferin induces the expression of SIRT1, catalase and HO-1, promotes the phosphorylation of eNOS, and stimulates nitric oxide (NO) production. δ-Viniferin is applicable to research related to atherosclerosis, downy mildew, Gram-positive bacterial infections, inflammation, infections, cardiovascular diseases and diabetes.
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MRS2768
0 ImagesCat. No.: HY-108649CAS No.: 1047980-83-5MRS2768 is a potent, selective, and metabolically stable P2Y2 receptor agonist with an EC50 of 1.89 μM for the human P2Y2 receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y2-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.
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S-Isopropylisothiourea hydrobromide
0 ImagesS-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) is a blood-brain barrier (BBB) penetrant NOS inhibitor with IC50 values of 0.66, 0.75 and 0.29 μM against mouse spinal cord, cerebellar, bovine aortic and porcine endothelial cell NOS. S-Isopropylisothiourea exhibits a significant blood pressure-raising effect without damaging the perfusion of vital organs and can also inhibit the late-phase pain response induced by formalin. S-Isopropylisothiourea hydrobromide is used in the researchs for hemorrhagic shock and pain response based on NOS.
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Malvidin-3-glucoside chloride (Standard)
0 ImagesCat. No.: HY-125740RCAS No.: 7228-78-6Synonyms: Malvidin-3-O-glucoside chloride (Standard); Oenin chloride (Standard)Malvidin-3-glucoside (Malvidin-3-O-glucoside; Oenin) chloride (Standard) is the analytical standard of Malvidin-3-glucoside chloride (HY-125740). This product is intended for research and analytical applications. Malvidin-3-glucoside chloride is an orally active inhibitor of the NF-κB pathway, which blocks inflammatory responses induced by TNF-α, reduces IκB-α degradation and p65 nuclear translocation, and upregulates endothelial nitric oxide synthase eNOS to increase NO production. Malvidin-3-glucoside chloride exerts anti-inflammatory and antioxidant effects by inhibiting pro-inflammatory molecules such as MCP-1, ICAM-1, and IL-6, and regulating intestinal microorganisms and metabolites, while protecting endothelial cells and improving intestinal microecological dysbiosis under inflammatory conditions. Malvidin-3-glucoside chloride can be used to study chronic inflammatory-related diseases such as atherosclerosis and inflammatory bowel disease, and has the potential to prevent vascular inflammation and improve intestinal health.
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Triflusal-d3
0 ImagesCat. No.: HY-B0531SCAS No.: 2748541-63-9Triflusal-d3 is deuterium labeled Triflusal (HY-B0531). Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
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YPX-C-05
0 ImagesYPX-C-05 is an orally active HDAC inhibitor and vasodilator. YPX-C-05 inhibits HDAC enzymatic activity, increases histone H4 acetylation, activates the PI3K/Akt pathway, promotes Akt and eNOS phosphorylation, enhances eNOS activity, and boosts nitric oxide production. YPX-C-05 increases Tetrahydrobiopterin (HY-107383) levels, restores serum nitric oxide levels, reduces endothelin-1 levels, and improves endothelial function. YPX-C-05 reduces vascular remodeling and exerts antihypertensive effects in hypertensive Mus musculus mice. YPX-C-05 can be used for the research of hypertension.
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Guanidino ethyl disulfide
0 ImagesGuanidino ethyl disulfide (GED) (Compound 23) is a NO Synthase (NOS) inhibitor with EC50s of 110, 630 and 180 μM for iNOS, eNOS and bNOS, respectivly. Guanidino ethyl disulfide effectively inhibits nitrite production in J774.2 macrophages. Guanidino ethyl disulfide can be used for circulatory shock, inflammation and neurological diseases research.
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Triflusal (Standard)
0 ImagesTriflusal (Standard) is the analytical standard of Triflusal (HY-B0531). This product is intended for research and analytical applications. Triflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
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4-Methoxybenzyl alcohol (Standard)
0 ImagesSynonyms: P-Methoxy-benzyl alcoho (Standard); (4-Methoxyphenyl)methanol (Standard)4-Methoxybenzyl alcohol (Standard) (P-Methoxy-benzyl alcoho (Standard); (4-Methoxyphenyl)methanol (Standard)) is the analytical standard of 4-Methoxybenzyl alcohol (HY-W015777). This product is intended for research and analytical applications. 4-Methoxybenzyl alcohol (P-Methoxy-benzyl alcoho; (4-Methoxyphenyl) methanol) is a naturally derived volatile aromatic compound. 4-Methoxybenzyl alcohol upregulates the phosphorylation level of PI3K/Akt pathway proteins, downregulates the expression of pro-inflammatory factors, increases the content of tight junction proteins occludin and claudin-5, and alleviates structural damage to the blood-brain barrier. 4-Methoxybenzyl alcohol improves the decrease in viability and NO level of cerebral microvascular endothelial cells induced by oxygen-glucose deprivation/reperfusion, and reduces the release of lactate dehydrogenase. 4-Methoxybenzyl alcohol serves as a substrate in the two-phase persulfate-mediated electro-oxidation system, where it is directionally oxidized to p-anisaldehyde. 4-Methoxybenzyl alcohol acts as a substrate for wild-type fungal aryl alcohol oxidase. 4-Methoxybenzyl alcohol can be used in studies related to ischemic stroke, as well as in research across various fields such as chemical synthesis, including the synthesis of fragrances and flavorings.
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Efadirelaxin alfa
0 ImagesCat. No.: HY-P992108CAS No.: 3061442-66-5Synonyms: RELAX10Efadirelaxin alfa (RELAX10) is a highly selective agonist of relaxin/insulin-like family peptide receptor RXFP1. After subcutaneous administration in animal experiments, Efadirelaxin alfa exhibits a significantly prolonged terminal half-life (7 days in mice, 3.75 days in rats), and shows no activity against related receptors such as RXFP2 and RXFP3. Efadirelaxin alfa has significant anti-cardiac hypertrophy and anti-fibrotic effects. Efadirelaxin alfa effectively attenuates and reverses cardiac hypertrophy and collagen deposition by regulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa improves cardiac systolic function without causing fluctuations in blood pressure or heart rate, demonstrating favorable safety. Efadirelaxin alfa is currently mainly used in studies related to heart failure.
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nNOS-IN-7
0 ImagesCat. No.: HY-120340CAS No.: 1895092-16-6
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TP508
0 ImagesCat. No.: HY-P0316CAS No.: 121341-81-9TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
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