ONO-5334

Names

[ Name ]:
ONO-5334

[Synonym ]:
2H-Pyran-4-propanoic acid, β-[(cycloheptylcarbonyl)amino]tetrahydro-α-oxo-, 2-[(2Z,4R)-3,4-dimethyl-2-thiazolidinylidene]hydrazide, (βS)-
N-[(1S)-3-{(2Z)-2-[(4R)-3,4-Dimethyl-1,3-thiazolidin-2-ylidene]hydrazino}-2,3-dioxo-1-(tetrahydro-2H-pyran-4-yl)propyl]cycloheptanecarboxamide
MFCD28139071

Biological Activity

[Description]:

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

[References]

References 1. Ochi Y, et al. Bone. 2011 Dec;49(6):1351-6. 2. Ochi Y, et al. Bone. 2014 Aug;65:1-8. doi: 10.1016/j.bone.2014.04.023. 3. Ochi Y, et al. J Bone Miner Metab. 2014 Nov;32(6):645-52. 4. Nagase S, et al. Br J Clin Pharmacol. 2012 Dec;74(6):959-70. View Related Products by Target Cathepsin Osteoporosis

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₂₁H₃₄N₄O₄S

[ Molecular Weight ]:
438.584

[ Exact Mass ]:
438.230072

[ LogP ]:
1.34

[ Index of Refraction ]:
1.644

Related Compounds

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