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Results for "

vascular remodeling

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Androgen Receptor (1) Apoptosis (3) Autophagy (1) Calcium Channel (3) Caspase (2) Endothelin Receptor (2) ERK (1) FGFR (2) Guanylate Cyclase (1) HSP (2) Integrin (1) Mineralocorticoid Receptor (1) Natriuretic Peptide Receptor (NPR) (2) Neprilysin (2) p38 MAPK (2) PDGFR (1) Phosphodiesterase (PDE) (2) Prostaglandin Receptor (1) STAT (1) TGF-β Receptor (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (14) Endocrinology (3) Inflammation/Immunology (2) Metabolic Disease (2) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Targets Recommended: VEGFR VAP-1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0561

Spironolactone 5+ Cited Publications 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 .

HY-120295

A-192621 1 Publications Verification	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology
A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ET_B) receptor antagonist with an IC₅₀ of 4.5 nM and a K_i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET_A (IC₅₀ of 4280 nM and K_i 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 .

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 .

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 .

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 K_i 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].

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 .

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 .

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 .

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 .

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 K_d values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide acetate regulates V_1/2 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 .

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 K_d values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Nesiritide regulates V_1/2 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 .

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 .

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 .

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 K_i 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) .

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 K_i 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) .

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 .

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 .

Cat. No.	Product Name

HY-L045

Oxygen Sensing Compound Library	3,451 compounds
Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression. Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival. HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation. MCE offers a unique collection of 3,451 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Oxygen Sensing Compound Library

3,451 compounds

Oxygen homeostasis regulation is the most fundamental cellular process for adjusting physiological oxygen variations, and its irregularity leads to various human diseases, including cancer. Hypoxia is closely associated with cancer development, and hypoxia/oxygen-sensing signaling plays critical roles in the modulation of cancer progression.

Hypoxia-inducible factor 1 (HIF-1) is a transcription factor that functions as a master regulator of oxygen homeostasis. A variety of HF-1 target genes have been identified thus far which encode proteins that play key roles in critical developmental and physiological processes including angiogenesis/vascular remodeling, erythropoiesis, glucose transport, glycolysis, iron transport, and cell proliferation/survival.

HIF-1 is a heterodimeric transcription factor consisting of a constitutively expressed β-subunit and an oxygen-regulated α-subunit. The unique feature of HIF-1 is the regulation of HIF-1α expression and activity based upon the cellular O₂ concentration. Under normoxic conditions, hydroxylation of HIF-1α on these different proline residues is essential for HIF proteolytic degradation by promoting interaction with the von Hippel-Lindau tumor-suppressor protein (pVHL) through hydrogen bonding to the hydroxyproline-binding pocket in the pVHL β-domain. As oxygen levels decrease, hydroxylation of HIF decreases; HIF-1α then no longer binds pVHL, and becomes stabilized, allowing more of the protein to translocate to the cell’s nucleus, where it acts as a transcription factor, upregulating (often within minutes) the production of proteins that stimulate blood perfusion in tissues and thus tissue oxygenation.

MCE offers a unique collection of 3,451 oxygen sensing related compounds targeting HIF/HIF Prolyl-Hydroxylase, MAPK/ERK, PI3K/AKT signaling pathways, etc. MCE Oxygen Sensing Compound Library is a useful tool to study hypoxia, oxidative stress and discover new anti-cancer drugs.

Cat. No.	Product Name	Target	Research Area