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Results for "

Vascular remodeling

" in MedChemExpress (MCE) Product Catalog:

28

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1

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1

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5

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2

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2

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0561
    Spironolactone
    Maximum Cited Publications
    7 Publications Verification

    SC9420

    		 Mineralocorticoid Receptor Androgen Receptor Autophagy Calcium Channel Cardiovascular Disease Metabolic Disease Endocrinology Cancer
    Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
    Spironolactone
  • HY-P0003
    Nesiritide

    Brain Natriuretic Peptide-32 human; BNP-32

    		 Natriuretic Peptide Receptor (NPR) Calcium Channel Cardiovascular Disease
    Nesiritide (Brain Natriuretic Peptide-32 human) is a recombinant human B-type natriuretic peptide. Nesiritide is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide shows vasodilatory, diuretic, and natriuretic activities. Nesiritide is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
    Nesiritide
  • HY-11103
    Sitaxsentan sodium
    2 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan sodium
  • HY-N1437
    Hydroxycitric acid
    1 Publications Verification

    		 Apoptosis Ferroptosis mTOR DNA/RNA Synthesis Keap1-Nrf2 Ribosomal S6 Kinase (RSK) NF-κB ATP Citrate Lyase AMPK Cardiovascular Disease Metabolic Disease Cancer
    Hydroxycitric acid is an orally active, multi-target, multi-bioactive organic acid. activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Hydroxycitric acid activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Hydroxycitric acid activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation .
    Hydroxycitric acid
  • HY-109163
    Treprostinil palmitil

    INS-1009

    		 Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Treprostinil palmitil is a long-acting inhaled pulmonary vasodilator prodrug of Treprostinil (HY-100441), formulated in a lipid nanoparticle (LNP). Treprostinil palmitil can inhibit pulmonary vascular remodeling induced by Su/Hx challenge in rats. Treprostinil palmitil can induce cough. Treprostinil palmitil demonstrates a sustained presence in the lungs with reduced systemic exposure and prolonged inhibition of hypoxia-induced pulmonary vasoconstriction in vivo. Treprostinil palmitil can be studied in research for pulmonary arterial hypertension and interstitial lung disease .
    Treprostinil palmitil
  • HY-W338584
    Hydroxycitric acid tripotassium
    1 Publications Verification

    		 Keap1-Nrf2 Ferroptosis Apoptosis mTOR NF-κB ATP Citrate Lyase AMPK Ribosomal S6 Kinase (RSK) DNA/RNA Synthesis Cardiovascular Disease Metabolic Disease Endocrinology Cancer
    Tripotassium hydroxycitrate is an orally active, multi-target, multi-bioactive organic acid. Tripotassium hydroxycitrate activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Tripotassium hydroxycitrate activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Tripotassium hydroxycitrate activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation .
    Hydroxycitric acid tripotassium
  • HY-120295
    A-192621
    2 Publications Verification

    		 Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology
    A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
    A-192621
  • HY-141867
    Z-FF-FMK

    Z-Phe-Phe-FMK

    		 Cathepsin MEK Caspase DNA/RNA Synthesis Apoptosis Cardiovascular Disease Neurological Disease
    Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
    Z-FF-FMK
  • HY-15472
    PRX-08066

    		5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase Cardiovascular Disease Neurological Disease Cancer
    PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .
    PRX-08066
  • HY-P3012
    Cathepsin G

    		Cathepsin ERK p38 MAPK PKC Protease Activated Receptor (PAR) MMP Inflammation/Immunology
    Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases .
    Cathepsin G
  • HY-76520
    Sitaxsentan

    IPI 1040; TBC-11251

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan
  • HY-162888
    WQ-C-401

    		PDGFR ERK Cardiovascular Disease
    WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
    WQ-C-401
  • HY-10383
    J-104132

    		Endothelin Receptor Cardiovascular Disease Metabolic Disease
    J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3].
    J-104132
  • HY-P3227
    Cyclo(Ala-Arg-Gly-Asp-Mamb)

    XJ735

    		 Integrin Inflammation/Immunology
    Cyclo(Ala-Arg-Gly-Asp-Mamb) is a selective RGD peptide antagonist and has the potential for Pulmonary arterial hypertension research .
    Cyclo(Ala-Arg-Gly-Asp-Mamb)
  • HY-B0561S4
    Spironolactone-d6-1

    		Isotope-Labeled Compounds Mineralocorticoid Receptor Androgen Receptor Autophagy Calcium Channel Cardiovascular Disease Metabolic Disease Cancer
    Spironolactone-d6-1 is the deuterium labeled Spironolactone (HY-B0561). Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
    Spironolactone-d6-1
  • HY-N1115
    Tubotaiwine

    (+)-Tubotaiwine; NSC 306222; Tubotaiwin

    		 Others Cardiovascular Disease
    Tubotaiwine ((+)-Tubotaiwine), an alkaloid, has beneficial effect on cadmium (Cd) induced hypertension in rats. Tubotaiwine regulates systolic, diastolic and mean arterial blood pressure of the Cd exposed rats. Tubotaiwine reduces arterial stiffness, inhibits of oxidative stress and increases vascular remodeling .
    Tubotaiwine
  • HY-101682
    SCH 42495

    		Neprilysin Cardiovascular Disease
    SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester proagent of SCH 42354 .
    SCH 42495
  • HY-101682A
    SCH 42495 racemate

    		Neprilysin Cardiovascular Disease
    SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester proagent of SCH 42354 .
    SCH 42495 racemate
  • HY-173360
    PDE10A-IN-5

    		Phosphodiesterase (PDE) Cardiovascular Disease
    PDE10A-IN-5 (Compound A30) is an inhibitor of phosphodiesterase 10A (PDE10A) with oral activity, and its IC50 value is 3.5 nM. PDE10A-IN-5 exerts the activity of inhibiting pulmonary vascular remodeling by inhibiting PDE10A and activating the cyclic adenosine monophosphate (cAMP)-associated signaling pathway, and can be used for research in the field of pulmonary arterial hypertension .
    PDE10A-IN-5
  • HY-W700639
    Tolafentrine

    		Phosphodiesterase (PDE) Neurological Disease
    Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes .
    Tolafentrine
  • HY-159484
    Hsp110/sGC-modulator-1

    		HSP Guanylate Cyclase Cardiovascular Disease
    Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
    Hsp110/sGC-modulator-1
  • HY-P0003A
    Nesiritide acetate

    Brain Natriuretic Peptide-32 human acetate; BNP-32 acetate

    		 Natriuretic Peptide Receptor (NPR) Calcium Channel Cardiovascular Disease
    Nesiritide (Brain Natriuretic Peptide-32 human) acetate is a recombinant human B-type natriuretic peptide. Nesiritide acetate is a NPRs agonist, with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V1/2 activation/inactivation of the L-type calcium channel. Nesiritide acetate shows vasodilatory, diuretic, and natriuretic activities. Nesiritide acetate is used in cardiovascular diseases such as heart failure and vascular remodeling after arterial injury .
    Nesiritide acetate
  • HY-168178
    Hsp110-STAT3 PPI-IN-2

    		HSP STAT Cardiovascular Disease
    Hsp110-STAT3 PPI-IN-2 (compound 10b) is a Hsp110-STAT3 interaction disruptor. Hsp110-STAT3 PPI-IN-2 can be used in pulmonary arterial hypertension (PAH) related research .
    Hsp110-STAT3 PPI-IN-2
  • HY-11103R
    Sitaxsentan sodium (Standard)

    IPI 1040 sodium (Standard); TBC11251 sodium (Standard)

    		 Endothelin Receptor Reference Standards TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan sodium is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan sodium (Standard)
  • HY-15472A
    PRX-08066 maleate

    		5-HT Receptor p38 MAPK TGF-β Receptor FGFR Apoptosis Caspase Cardiovascular Disease Neurological Disease Cancer
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET) .
    PRX-08066 maleate
  • HY-76520S
    Sitaxsentan-13C6

    IPI 1040-13C6 ; TBC-11251-13C6

    		 Isotope-Labeled Compounds Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan- 13C6 (IPI 1040- 13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan-13C6
  • HY-180585
    LOXL2/sGC modulator-2

    		Monoamine Oxidase Guanylate Cyclase PKG Collagen Cardiovascular Disease
    LOXL2/sGC modulator-2 (Compound 9k) is a selective and orally active lysyl oxidase-like 2 (LOXL2) and soluble guanylate cyclase (sGC) dual-target regulator. LOXL2/sGC modulator-2 shows inhibitory activity for LOXL2 with an IC50 of 0.1 μM and can activate sGC. LOXL2/sGC modulator-2 can ameliorate vascular remodeling and reduce pulmonary artery pressure. LOXL2/sGC modulator-2 can downregulate PKG1, PCNA, α-SMA, collagen I and fibronectin levels. LOXL2/sGC modulator-2 can be used for the research of pulmonary arterial hypertension .
    LOXL2/sGC modulator-2
  • HY-182306
    VEGFR-2 ligand-2

    		VEGFR Cardiovascular Disease
    VEGFR-2 ligand-1, Sorafenib (HY-10201) derivative, is a vascular endothelial growth factor receptor 2 (VEGFR2) ligand. VEGFR-2 ligand-1 binds to the ATP-binding pocket of VEGFR2, forms hydrophobic contacts and hydrogen bonds with key binding-site residues. VEGFR-2 ligand-1 can be used for the research angiogenesis-related pathologies .
    VEGFR-2 ligand-2

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