calcification

Halopemide is a potent inhibitor of PLD (IC50 = 220 and 310 nM for human PLD1 and PLD2). Halopemid is an antagonist of dopamine receptors. Halopemid can be used in psychotropic research.

Etidronic acid (HEDP) is a diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.

Sodium etidronate (Didronel) is a synthetic therapeutic diphosphonate analog of endogenous pyrophosphate. As a member of the family of drugs known as bisphosphonates, Sodium etidronate differs from endogenous pyrophosphate in its resistance to enzymatic hydrolysis. This agent adsorbs to hydroxyapatite cells and reduces the number of osteoclasts, thereby inhibiting abnormal bone resorption. Etidronate may also directly stimulate bone formation by osteoblasts.

Calindol hydrochloride is a potent orthosteric modulator (EC50: 132 nM) of the putative calcium-calcium-sensitive receptor (CaSR), inhibits Pi-induced VC, and delays the progression of calcification in vascular smooth muscle cells.

Upacicalcet (AJT-240) is an intraventricular calcium mimetic, a SHPT available for human hemodialysis, that inhibits excessive parathyroid hormone (PTH) secretion by directly acting on parathyroid cell membrane calcium-sensitive receptors, thereby lowering blood levels of PTH.Upacicalcet is an orthosteric modulator of calcium-sensitive receptors and prevents adenine-induced secondary vascular calcification and bone disease in a rat model of adenine-induced secondary hyperparathyroidism.

Clodronate disodium tetrahydrate (Clastoban) inhibits bone resorption and soft tissue calcification.

(2R)-Octyl-α-hydroxyglutarate is a modified derivative of the D-isomer of 2-hydroxyglutarate. (2R)-Octyl-α-hydroxyglutarate can improve adenine-induced arterial calcification in rats and inhibit pancreatic tissue damage, making it suitable for research on vascular calcification (VC) and acute pancreatitis.

TNAP-IN-1 is a specific inhibitor of tissue-nonspecific alkaline phosphatase (TNAP) and is utilized in studying diseases related to soft tissue calcification.

2-Thio-UTP is a selective P2Y2 receptor (purinergic receptor) agonist (EC50 = 50 nM) capable of inhibiting calcification potential, α-smooth muscle actin expression, and pro-fibrotic gene expression in valvular interstitial cells (VICs). It may be employed in studies of calcific aortic valve stenosis (CAVS).

Hexasodium phytate is used potentially to treat vascular calcification and calciphylaxis.

L-Lysine acetate is an essential amino acid for humans. Owing to its unique biological properties, it can be used in mechanistic investigations and research related to vascular calcification (VC) and acute pancreatitis.

Lysine monohydrate is one of the essential amino acids for humans and can be used in basic and experimental studies related to vascular calcification (VC) and acute pancreatitis.

POV-PC is an oxidized phospholipid that inhibits VSMC growth under high serum conditions and induces apoptosis under low serum conditions. POVPC reduces NO production and expression of CD31 and endothelial NOS, triggering ferroptosis in vascular smooth muscle cells, promoting vascular calcification.

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

Fetuin (from Fetal Bovine Serum) is a glycoprotein purified from foetal bovine serum, primarily employed as an additive in cell culture to promote cell adhesion and growth. Fetuin is the protein product of the AHSG gene, naturally occurring in serum and extracellular fluids. It inhibits calcification and cysteinopeptidases, antagonises TGF-β, reduces insulin sensitivity, and more.

2,3-Diphospho-D-glyceric acid pentasodium salt is a highly anionic polyphosphorus compound located within the concave center of red blood cells, where it decreases oxygen affinity by binding to hemoglobin. This endogenous compound selectively inhibits vascular calcification (VC) and effectively postpones the formation of crystalline calpain particles (CPP). Additionally, it inhibits calcification in the mouse vascular smooth muscle cell line (MOVAS) without eliciting cytotoxic effects [1].

Efmirenpase alfa is an Fc-ENPP1 fusion protein (comprising a human IgG1 Fc domain linked to a modified human ENPP1). Compared to natural human ENPP1, Efmirenpase alfa exhibits an extended half-life and greater receptor affinity. It is being investigated as an enzyme replacement therapy for ENPP1 deficiency conditions, such as arterial calcification and hypophosphatemic rickets.

Spironolactone-d6-1 is a deuterium-labeled version of Spironolactone. Spironolactone functions as an aldosterone antagonist, targeting mineralocorticoid receptors (IC50=24 nM) and androgen receptors (IC50=77 nM). It promotes podocyte autophagy (autophagy) and modulates pain. The compound improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II-induced inflammation. It also decreases aldosterone-induced vascular and soft tissue calcification via PIT1-dependent signaling, and mitigates vascular dysfunction in type II diabetic mice by decreasing oxidative stress and restoring NO/GC signaling. At low concentrations, Spironolactone and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca2+ channels to exert antihypertensive effects.

1-Methyl-2-undecyl-4(1H)-quinolone, along with dihydroevocarpine and evodiamine, should serve as chemical markers for the quality control of Evodia rutaecarpa (Juss.) Benth. This compound selectively inhibits type B MAO (MAO-B) activity with an IC(50) value of 15.3 microM using the substrate kynuramine, while not inhibiting type A MAO (MAO-A) activity. It can mitigate high phosphate-induced calcification in human aortic valve interstitial cells (HAVICs) by inhibiting phosphate cotransporter (PiT-1) gene expression and exhibits moderate antiangiogenic activity against human tumor cells.

Carbonic Anhydrase, Human (EC 4.2.1.1), is a zinc metalloenzyme that catalyzes the hydration of carbon dioxide to form carbonic acid. It plays a role in various essential physiological processes, such as maintaining pH and carbon dioxide homeostasis, transporting bicarbonate and carbon dioxide, biosynthetic reactions, bone resorption, calcification, and tumorigenesis.

Carbonic Anhydrase I, Human (EC 4.2.1.1), is a zinc metalloenzyme that catalyzes the hydration of carbon dioxide to form carbonic acid. This enzyme plays a crucial role in various physiological processes, including maintaining pH and carbon dioxide homeostasis, transporting bicarbonate and carbon dioxide, facilitating biosynthetic reactions, bone resorption, calcification, and tumor progression.