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Cat. No. Product Name CAS No. Information
PC-62962

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.

Osteoporosis

Phase 2 Discontinued

PC-35143

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.

Osteoporosis

Discontinued

PC-42809

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.

Osteoporosis

Approved

PC-62964

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.

Osteoporosis

Phase 1 Discontinued

PC-61506

Ronacaleret hydrochloride

702686-96-2 A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR; stimulates parathyroid hormone (PTH) release and increases bone formation markers; act as an effective oral anabolic agent to enhance fracture healing.

Osteoporosis

Phase 2 Discontinued

PC-61505

Ronacaleret

753449-67-1 A potent calcium sensing receptor (CaSR) negative allosteric modulator with IC50 of 146 nM for hCaSR; stimulates parathyroid hormone (PTH) release and increases bone formation markers; act as an effective oral anabolic agent to enhance fracture healing.

Osteoporosis

Phase 2 Discontinued

PC-61421

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.

Osteoporosis

Phase 2 Discontinued

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