Osteoporosis

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

Avanafil (TA1790) is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.

Balicatib (AAE581) is a potent and selective inhibitor of cathepsin K, used in trials studying the treatment of osteoporosis.

Teriparatide acetate (Forteo) is a PHT agonist, with an IC50 of 2 nM in HEK293 cells.Teriparatide acetate is a recombinant form of parathyroid hormone. It is an effective anabolic (i.e., bone growing) agent used to treat some forms of osteoporosis. Intermittent use of Teriparatide acetate activates osteoblasts more than osteoclasts, which leads to an overall increase in bone.

1. Tiliroside (Tribuloside) shows anticarcinogenic activity. 2. Tiliroside shows hepatoprotective activity. 3. Tiliroside shows antioxidant and anti-inflammatory activity, can inhibit neuroinflammation in neurodegenerative disorders. 4. Tiliroside has anti-diabetic effect, are at least partially mediated through inhibitory effects on carbohydrate digestion and glucose uptake in the gastrointestinal tract. 5. Tiliroside and gnaphaliin are antioxidants against in vitro Cu(2+)-induced LDL oxidation in the same order of magnitude compared to that of the reference drug, probucol. 6. Tiliroside enhances fatty acid oxidation via the enhancement adiponectin signaling associated with the activation of both AMP-activated protein kinase and peroxisome proliferator-activated receptor α and ameliorates obesity-induced metabolic disorders.

Alfacalcidol (Etalpha) (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication.

Alendronic Acid (alendronate) is a nonhormonal medication used for osteoporosis, osteogenesis imperfecta, and several other bone diseases.

Denosumab is a monoclonal antibody given subcutaneously that inhibits osteoclast activity by targeting the RANK ligand

Neoeriocitrin is a natural product isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.

N-(3-Methoxybenzyl)-(9Z,12Z,15Z)-octadecatrienamide (Macamide Impurity 14) induces osteogenic differentiation and subsequent bone formation of mesenchymal stem cells by activating the canonical Wnt β-catenin signaling pathway, making it useful for osteoporosis research.

Anti-osteoporosis agent-11 (compound 3k) is an anti-osteoporosis compound targeting osteoclasts. It exhibits its most prominent effect by inhibiting osteoclast differentiation, with an IC50 value of 0.36 μM. Additionally, Anti-osteoporosis agent-11 suppresses osteoclast formation, bone resorption, and the expression of osteoclast-specific genes by blocking the RANKL-induced mitogen-activated protein kinase (MAPK) and NF-κB signaling pathways.

Anti-osteoporosis agent-10 is an inhibitor of osteoporosis that suppresses the formation of osteoclasts with an IC50 of 0.042 μM. It also exhibits antagonistic activity towards PPARγ, with an EC50 value of 0.75 μM.

Anti-osteoporosis agent-1 (comp 4aa) is a potent RPA (replication protein A) inhibitor with an IC50 value of 18 μM [1].

Anti-osteoporosis agent-4 (Compound 11h) suppresses the differentiation of primary osteoclasts and attenuates RANKL-induced osteoclastogenesis, effectively inhibiting osteoclast formation with an IC50 value of 358.29 nM, and impedes the activation of the PI3K AKT and IκBα NF-κB signaling pathways [1].

Compound 133, also known as Anti-osteoporosis agent-7, is a potential anti-osteoporosis agent that exhibits significant inhibition of osteoclast formation.

Anti-osteoporosis agent-2 (Compound 10) inhibits RANKL-induced osteoclast differentiation [1].

Compound 11, also known as Anti-osteoporosis agent-3, is a derivative of PMSA that serves as an anti-osteoporosis agent. It effectively inhibits osteoclastogenesis in vitro with an IC50 value of 322.9 nM. Additionally, this compound prevents the formation of F-action belts and bone resorption [1].

Anti-osteoporosis agent-9 (compound 5b) is an N-cyclopropyl-4-((sulfonylpiperazin-1-yl)methyl)benzamide derivative that exhibits anti-osteoclast activity.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

ONO-5334 is a selective, orally active and potent histone K inhibitor with anti-SAR-COV-2 and anti-bone resorption activity for the study of osteoporosis.

WY-47766 (OST-766) is a small molecule proton pump inhibitor that can be used to study postmenopausal osteoporosis.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1 2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

Praeruptorin B (Praeruptorin D), a compound found in the roots of Peuced, is an inhibitor of sterol regulatory element-binding proteins (SREBPs) that attenuates the metastatic ability of human renal cancer cells by targeting CTSC and CTSV expression, and can be used in the study of osteoporosis.

E197 is an anti-osteoporotic compound, a Dock5 inhibitor, which can be used in the study of osteoporosis.