smooth muscle cell

LDN-27219 is a potent hTGase inhibitor with IC50 of 0.6 uM.

Regrelor disodium (INS 50589) is a P2Y12 receptor antagonist that prevents thrombosis, effectively inhibits vascular smooth muscle cell contraction, curbs cell proliferation, and reduces inflammation.

(R)-Naroparcil is an isomer of Naroparcil. Naroparcil, a 4-methylumbelliferyl beta-D-xyloside analog, is associated with vascular smooth muscle cell proliferation and inhibits thrombus formation in the Wessler slough model.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Hydralazine hydrochloride (Apresoline) is the hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume, and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells.

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

ML-7 hydrochloride (ML-7 HCl) is a cell-permeable, reversible, effective, ATP-competitive, and specific inhibitor of myosin light chain kinase (Ki: 300 nM); also inhibits smooth-muscle myosin light chain kinase, PKA, and PKC.

Polydatin (Piceid), the glycoside of Resveratrol, is originally isolated from the Chinese herb Polygonum cuspidatum. The compound can inhibit platelet aggregation and elevate the ratios of LDL-C HDL-C and TC HDL-C. In the myocardial cell, white blood cell, vascular smooth muscle cell, and endothelial cell, Polydatin can inhibit ICAM-1 expression, elevate Ca2+, weaken white blood cell-endothelial cell adhesion, and activate KATP channels.

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is an S enantiomer of blebbistatin. It is a potent and selective myosin II inhibitor with IC50 ranging from 0.5 to 5 μM.

Clorgyline (M&B 9302), an irreversible and selective MAO-A inhibitor with the advantages of oral activity and blood-brain barrier permeability, has an antidepressant effect by structurally altering the enzyme through the formation of intermediate radical cations, and reduces 1% fbs-stimulated VSMC (vascular smooth muscle cell) growth.

Dexloxiglumide, an active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). It is a selective antagonist of cholecystokinin type A (CCKA) receptors.

Collagenase, Type VIII, has the capability to hydrolyze Type VIII collagen, and may be utilized in the study of atherosclerosis development. Type VIII collagen serves as a regulator of endothelial cell differentiation and angiogenesis, acts as a substrate for the adhesion and migration of cells such as smooth muscle cells, and may accumulate in atherosclerosis. Following the activation by endotoxins, the expression of Collagenase, Type VIII can reduce the production of Type VIII collagen, potentially inhibiting the progression of atherosclerosis.

Kanglexin is an orally active novel anthraquinone compound. It inhibits NLRP3 inflammasome activation and pyroptosis, offering cardioprotective benefits. By stimulating the FGFR1 ERK signaling pathway, Kanglexin promotes angiogenesis and accelerates wound healing in diabetes. Additionally, it has lipid-lowering effects and inhibits vascular smooth muscle cell dedifferentiation, making it a potential compound for studying hyperlipidemia, fatty liver, and atherosclerosis.

BKCa activator-1 (Compound 51b) is an orally active activator of BKCa calcium-activated potassium channels with an EC50 of 2.82 μM. It promotes K+ efflux, leading to cell membrane hyperpolarization and inhibition of smooth muscle contraction. In a spontaneous hypertensive rat (SHR) model, it alleviates urinary incontinence and exhibits antitussive effects in a guinea pig cough model.

TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries.

BK 129 is a local anesthetic with relaxant properties. BK 129 inhibits Ca2+ entry into the smooth muscle cell and Ca2+ release from sarcoplasmic reticulum.

DL-threo dihydrosphingosine is a cell-permeable inhibitor of the extracellular signal-regulated kinase (ERK) signalling cassette in mammalian cells. DL-threo dihydrosphingosine is effective against both growth factor- and G-protein-dependent activation of

FK-739 is an angiotensin type 1 receptor antagonist. FK 739 inhibits the specific binding of [125I]-angiotensin II to rat aortic smooth muscle cell membrane (IC50 = 8.6 nM) without displacing the specific binding of [125I]-angiotensin II to bovine cerebel

Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

I-BOP is an agonist (KD=0.61 nM) at the thromboxane A2 receptor (TP). I-BOP promotes cell proliferation by activating the PI3K pathway in vascular smooth muscle.

Migrastatin is a bacterial metabolite that has been found inStreptomyceswith antimuscarinic and anticancer activities.1,2It binds to M1-5muscarinic acetylcholine receptors (Kis = >200, 200, 31, 43, and >200 μM, respectively) and inhibits calcium mobilization induced by carbamoylcholine in SK-N-SH cells (IC50= 28 μM), as well as in primary rat bladder smooth muscle cells.1Migrastatin inhibits the migration of EC17 esophageal cancer cells in a wound healing assay (IC50= 10 μg/ml) and 4T1 mouse mammary carcinoma cells in a chamber cell migration assay (IC50= 29 μM).2It enhances cytotoxicity induced by vinblastine in vincristine-resistant P388/VCR cells.3

Neuromedin C is a bombesin-like neuropeptide that stimulates uterine smooth muscle contraction and the release of gastrin , somatostatin, and amylase in rats. Neuromedin C is a truncated form of gastrin-releasing peptide corresponding to the GRP amino acids 18-27. It inhibits GRP and bombesin binding to rat pancreatic membranes (IC50s = 0.4 and 2.2 nM, respectively), which can be reduced by sodium chloride and guanylyl imidodiphosphate . Neuromedin C induces scratching and mast cell degranulation in mice when administered intradermally at doses ranging from 1 to 300 nmol/site, which is inhibited by the BB2 bombesin receptor agonist RC-3095 and reduced in mast cell-deficient mice. Neuromedin C (3.2 nmol/kg, i.p.) reduces rat glucose consumption by approximately 50% for up to one hour.

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).