bone loss

BCI hydrochloride ((E)-BCI hydrochloride) is a selective dual-specificity phosphatase 6 (DUSP6) inhibitor that inhibits RANKL-mediated osteoclastogenesis and attenuates oophorectomy-induced bone loss.BCI hydrochloride has anti-inflammatory activity, reduces reactive oxygen species (ROS) production, and partially reverses AE-induced bone loss. BCI hydrochloride has anti-inflammatory activity and can reduce reactive oxygen species (ROS) production, partially reverse AE-induced cytotoxicity, and increase ERK activity, which can be used to study inflammatory diseases.

Droloxifene (3-Hydroxytamoxifen), a tamoxifen derivative, is an oral active and selective estrogen receptor modulator.Droloxifene induced p53 expression and apoptosis in McF-7 cells.Fluroxifene has anti-estrogen and anti-implantation effects.Fluroxifene prevented bone loss in ovariectomized rats.

Astramembrangenin (Cycloastragenol (Astramembrangenin)) is a triterpenoid saponin compound and a hydrolysis product of the main active ingredient in Astragalus membranaceus. Cycloastragenol (CAG) may have a novel therapeutic role in depression

Sciadopitysin may prevent the development of diabetic osteopathy, it exerts its therapeutic effects via upregulation of mitochondrial biogenesis.Sciadopitysin shows protective effects on antimycin A-induced toxicity in osteoblastic MC3T3-E1 cells, it may

Cimicifugoside H1 shows the protective function to cerebral neuron during cerebral ischemia.

6-Raloxifene-β-D-glucopyranoside is a benzothiophene glucuronidated at the 6' position. It is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss, resorption, and lowering lipid

Otenaproxesul (ATB 346) is a novel hydrogen sulphide-releasing derivative of naproxen with markedly reduced toxicity.

PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.

CXM102 is an activator of autophagy. This compound induces autophagy in aged BMSCs, rejuvenating them and promoting their preferential differentiation into osteoblasts. CXM102 enhances the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. In middle-aged male mice, it stimulates bone anabolic metabolism, reduces marrow adipocytes, delays bone loss, lowers serum inflammation levels, reduces organ fibrosis, and extends lifespan.

E0924G is an orally active PPARδ agonist with an EC50 of 2.82 μM. It enhances the upregulation of osteoprotegerin (OPG) expression, with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibits F-actin ring formation in RAW264.7 macrophages. Additionally, E0924G modulates bone density and bone loss in models of ovariectomy (OVX) and age-related osteoporosis.

Raloxifene (LY139481) is a selective estrogen receptor modulator that exhibits both estrogen agonist and antagonist activities at certain sites, with antiviral activity against viruses like Ebola, influenza, and HCV, useful for studying viral infections.

SPA0355 is a thiourea derivative with antioxidant and anti-inflammatory properties. It inhibits RANKL (receptor activator of nuclear factor κB ligand)-induced osteoclastogenesis in primary bone marrow-derived macrophages and suppresses the activation of MAPKs, Akt, and NF-κB pathways. Furthermore, SPA0355 enhances osteoblast differentiation by increasing alkaline phosphatase activity and mineralized nodule formation. It protects ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it a potential candidate for studying postmenopausal osteoporosis.

BT-Amide is an orally active Pyk2 kinase (Pyk2kinase) inhibitor with an IC50 of 44.69 nM. It prevents glucocorticoid-induced bone loss and demonstrates bone-protective activity in C57BL 6 mice.

L-006235 is a potent and reversible inhibitor of cathepsin K with IC50 of 0.25 nM.

Thonzonium bromide is a mono-cationic surfactant that is structurally similar to Farnesol as an antimicrobial agent. It inhibits proton transport in a dose-dependent manner (EC50=69 μM). It inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo.

GSK 650394 is an inhibitor of serum- and glucocorticoid-regulated kinases (SGK) that inhibits SGK1 and SGK2 (IC50=62 103 nM). GSK 650394 has antitumor activity and also inhibits osteoclast differentiation and prevents bone loss.

ABD-295 is an antiresorptive agent, osteoclast inhibitor, and biphenylsulfide derivative. ABD-295 has potent inhibitory effects on osteoclastic bone resorption in vitro. ABD-295 prevents ovariectomy-induced bone loss in vivo.

M-5011 is a non-steroidal anti-inflammatory drug and immunomodulator potentially for the treatment of inflammation and pain. M-5011 had an effective antinociceptive activity (ED50 value) of 0.63 mg kg. M-5011 partially inhibits the generalized bone loss a

CGP77675 hydrate is an orally active, potent inhibitor of Src family kinases. It inhibits the phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively), as well as Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. CGP77675 hydrate may be useful for treating diseases associated with elevated bone loss and has anticancer activity [1].

Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6]

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

Kinsenoside ((+)-Kinsenoside) shows significant antihepatotoxic, and anti-inflammatory activities. Kinsenoside could be useful for repairing beta cells in pancreatic islet injury as well as improving its function, it could promote the glucose tolerance of acute glucose increase in both diabetic and normal healthy rats. Kinsenoside inhibits osteoclastogenesis from macrophages by attenuating RANKL-induced NF-κB and NFATc1 activities, which in turn, prevents bone loss from OVX mice.

Miroestrol is a potent phytoestrogen compound with multifaceted biological effects. It induces a mammogenic effect and demonstrates neuroprotective properties, along with the ability to prevent bone loss in ovariectomized mice. Additionally, Miroestrol has been shown to reduce the risk of cancer [4].