bone density

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

Imperatorin (8-Isopentenyloxypsoralene) is a modulator of p38, ERK pathway. Imperatorin increases BMP-2 expression (mRNA) and increases bone density volume and mineralization in vivo.

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

Soy Isoflavone is extracted from the seeds of leguminous plants. The isoflavones in soybeans are natural phytoestrogens, which have good medicinal value and can reduce the incidence of breast cancer in women, relieve menopausal symptoms, and increase bone density.

1. Poncirin (Isosakuranetin-7-neohesperidoside) shows a significant in vitro inhibitory effect on the growth of the human gastric cancer cells, SGC-791, in a dose-dependent manner. 2. Poncirin prevents adipogenesis, enhances osteoblast differentiation in mesenchymal stem cellsincreased bone mineral density, and improves trabecular microarchitecture likely reflect increases bone formation and decreases bone resorption in GIO mice.

Eldecalcitol possesses a potent inhibitory effect on bone resorption and induces a significant increase in bone mineral density. Eldecalcitol is an orally active analogue of active vitamin D. It also is used in the treatment of osteoporosis .

PCSK9-IN-29 serves as a lipid-lowering agent that enhances the expression of low-density lipoprotein receptor (LDLR) protein and reduces PCSK9 protein expression in hepG2 cells. Additionally, in crab-eating macaques on a high-fat diet, it lowers serum LDL-C, TC, and liver enzyme ALT levels, reduces body weight and fat, and boosts bone mineral content. PCSK9-IN-29 is useful for studies involving non-alcoholic fatty liver disease and obesity.

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.

PDE7A-IN-1 (Compound 26) is an orally active PDE7A inhibitor with an IC50 value of 3.7 nM. By inhibiting sclerostin, PDE7A-IN-1 significantly enhances bone mineral density, making it suitable for studies on osteoporosis and related bone metabolic disorders.

Ranelic acid is an organic acid capable of chelating metal cations. Strontium ranelate, the strontium salt of Ranelic acid, is utilized to treat osteoporosis and increase bone mineral density.

CW 008 is an activator of the cAMP/PKA/CREB pathway. It promotes osteogenic differentiation of human bone marrow derived mesenchymal stem cells in vitro and increases bone mass and bone volume density in ovariectomized mice.

3-epi-25-hydroxy Vitamin D3 is the C-3 epimer of 25-hydroxy vitamin D3. Dietary administration of 3-epi-25-hydroxy vitamin D3 (0.5 and 1 IU g) decreases levels of serum parathyroid hormone (PTH) in male, but not female, weanling rats.

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

Pparδ agonist 5 is a selective, orally active PPARδ agonist with an EC50 of 0.335 μM and better selectivity than GW0742. Pparδ agonist 5 has a beneficial effect on the improvement of bone density and microarchitecture in vivo.

Incadronate, also known as Cimadronate and YM-175, is a bone resorption inhibitor. Incadronate disodium inhibits macrophage migration to site of inflammation in vivo and proliferation and causes apoptosis in cancer cells in vitro. Incadronate disodium is a bone density conservation, antitumor and anti-inflammatory agent.

pTH (1-37) (human), a fragment of parathyroid hormone (PTH), promotes cAMP formation and enhances alkaline phosphatase activity. Additionally, it fosters growth, elevates bone calcium content, and augments bone mineral density (BMD) in uremic animals. This compound shows promise for osteoporosis research [1] [2] [3].

The compound AVSEHQLLHDKGKSIQDLRRRFFLHHLI-{Aib}-EIHTAYRFGG facilitates bone ossification and has potential applications in the study of conditions associated with osteogenic insufficiency or diminished bone mineral density (BMD), including osteoporosis [1].

VnP-16, a synthetic peptide fragment mirroring amino acids 270-281 of vitronectin (a multifunctional glycoprotein involved in cell attachment, migration, and spreading), promotes attachment and spreading of isolated human osteogenic cells. This effect is reversible with β1 integrin siRNA knockdown when VnP-16 is applied at 9.1 µg/cm2 on cell plates. The compound enhances osteogenesis in human skin-derived mesenchymal precursors and MC3T3-E1 mouse calvarial osteoblast precursors. Furthermore, in vivo studies show VnP-16 mitigates IL-1α-induced bone loss, reduces calvarial osteoclast numbers in mice, increases bone mineral density, and lessens trabecular bone loss in a mouse model of ovariectomy-induced bone loss.

Calcitonin, eel is a peptide hormone that plays a crucial role in maintaining calcium balance within the body. It is extensively utilized in the scientific investigation of postmenopausal osteoporosis, a condition characterized by decreased bone density and an increased risk of fractures in women after menopause.

C-telopeptide, a cross-linked peptide from type I collagen, is released during bone resorption and shows a correlation with bone mineral density (BMD).

Elcatonin (Carbocalcitonin), a synthetic analog of eel calcitonin, enhances bone mineral density, inhibits bone resorption, and exhibits a central analgesic effect [1].