Osteoporosis|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Bone is a rigid tissue that performs several key functions: it supports the body; it provides a point of attachment for tendons; it protects the internal organs; it produces blood cells; and it stores key minerals such as calcium and phosphorus. Throughout life, bone is remodeled by the activity of osteoblasts and osteoclasts. Osteoblasts are responsible for the synthesis of bone, while osteoclasts resorb bone tissue. A carefully controlled balance of these activities underlies bone remodeling and an imbalance can result in disorders such as osteoporosis, which weakens bones.

Osteoblasts and Osteoclasts

Osteoblasts and osteoclasts are derived from different cell precursors - mesenchymal and hematopoietic stem cells (MSCs and HSCs), respectively. Differentiation of HSCs to osteoclasts involves a number of cytokines such as bone morphogenetic protein (BMP) and TNF-α. Rho kinase (ROCK) inhibition may also stimulate osteoblast differentiation. Osteoblasts and osteoclasts are responsible for bone repair and growth, as well as the maintenance of bone density.

Metabolic Bone Disease

Loss of bone density normally occurs after the age of 35, and is a natural part of ageing. Bone turnover is regulated by a number of factors, including estrogen, nitric oxide and calcium-regulated calcium channels. However, bone loss may also be a result of metabolic bone disease, a term that describes a number of disorders resulting from mineral abnormalities in bone tissue. These include osteoporosis, Paget's disease of bone, osteomalacia and rickets.

Osteoporosis is relatively common, particularly in post-menopausal women, and can result in an increased likelihood of bone fracture. Osteomalacia and rickets describe deficiencies in bone mineralization in adults and children, respectively. Paget's disease of bone results from increased bone resorption by osteoclasts, followed by rapid, disorganized bone deposition by osteoblasts. The resulting tissue is larger and weaker than normal bone.

Cat. No.	Product Name	CAS No.	Information
H6137	Alendronate sodium hydrate	121268-17-5	Alendronate sodium hydrate (Alendronate;MK 217;G-704650 Adronat) is a bisphosphonate that acts as a specific inhibitor of osteoclastmediated bone resorption, inhibits osteoclast protein-tyrosine phosphatase (PTPepsilon) with IC50 of 2 uM; also inhibits the activities of other bacterially expressed PTPs such as PTPsigma and CD45, suppresses in vitro formation of multinucleated osteoclasts from osteoclast precursors and in vitro bone resorption by isolated rat osteoclasts with IC50 of 10 uM; also is also inhibits farnesyl disphosphate synthase with IC50 of 1.7 uM.
H5990	Calcifediol monohydrate	63283-36-3	The major circulating metabolite of vitamin D3; it is produced in the liver and is the best indicator of the body's vitamin D stores; it is effective in the treatment of RICKETS and OSTEOMALACIA, both in azotemic and non-azotemic patients; also has mineralizing properties.
H5663	MK-0773	606101-58-0	A potent, selective androgen receptor modulator (SARM) with binding IC50 of 6.6 nM; displays no binding to other nuclear receptors ( GR, IC50> 2 uM) and 5α-reductase (IC50>10 uM); improves muscle function while minimizing effects on other tissues.
H5657	LGD-2226	328947-93-9	LGD-2226 (LGD2226) is an orally active, selective androgen receptor modulator (SARM) with binding Ki of 1 nM, >1000-fold selectivity over GR,PR, MR and ER; LGD2226 is fully active in cell-based models of bone and muscle, exhibits anabolic activity on muscle and bone with reduced impact on prostate growth in rodent models; LGD2226 is also efficacious in a sex-behavior model in male rats measuring mounts, intromissions, ejaculations, and copulation efficiency.
H5034	Relacatib	362505-84-8	Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively; displays 39-300-fold selectivity over other cathepsins; inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 of 45 nM and 70 nM, respectively; inhibits bone resorption both in vitro in human tissue and in vivo in cynomolgus monkeys.
H5032	ONO-5334	868273-90-9	A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively; shows less or no potentcy for human cathepsin S/L/B/C (Ki=0.83/1.7/32/2500 nM); inhibits human osteoclasts bone resorption in vitro at a concentration more than 100 fold lower than that of alendronate; reduces plasma calcium level increased by PTHrP in thyroparathyroidectomized rats, decreases serum and urine C-telopeptide of type I collagen level.
H5031	Odanacatib	603139-19-1	A potent, selective, reversible and orally active cathepsin K inhibitor with IC50 of 0.2 nM; displays >300-fold selectivity over cathepsin B, L, S, F, and V; demonstrates the potentiation for the treatment of osteoporosis and other skeletal disorders associated with excessive bone remodeling.
H5024	L 873724	603139-12-4	L 873724 is a potent and selective non-basic cathepsin K inhibitor with IC50 of 0.2 nM, shows no significant potency against Cat B, L, and S (IC50= 5239, 264, and 178 nM); demonstrates excellent pharmacokinetics and efficacy in an ovariectomized (OVX) rhesus monkey model.
H5989	Calcifediol	19356-17-3	The major circulating metabolite of vitamin D3; it is produced in the liver and is the best indicator of the body's vitamin D stores; it is effective in the treatment of RICKETS and OSTEOMALACIA, both in azotemic and non-azotemic patients; also has mineralizing properties.
H3054	Strontium ranelate	135459-87-9	A strontium(II) salt of ranelic acid that stimulates CaSR and leads to the differentiation of pre-osteoblast to osteoblast, increases the bone formation; also stimulates osteoblasts to secrete osteoprotegerin in inhibiting osteoclasts formed from pre-osteoclasts in relation to the RANKL system; a medication for osteoporosis treatment.

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