A2487-5mg | Odanacatib (MK-0822) [603139-19-1] Quimigen Portugal

Background

Odanacatib (MK-0822) is a potent, orally active and selective inhibitor of Cathepsin K with IC50 value of 0.20 nM [1],

Cathepsin K is expressed predominantly in osteoclasts and degrades the collagen matrix componentsofbone. It plays a central role in mediating bone resorption. And the inhibitor of cathepsin K, Odanacatib, is in development for the treatment of osteoporosis. Based on preclinical evidence and available clinical data from dose-ranging phase IIB trials, odanacatib appears to reduce bone resorptionwhile somewhat preserving bone formation in postmenopausal

Women. Currently, Odanacatib is undergoing evaluation for fracture risk reduction in a phase III trial with ＞16000 patients with postmenopausal osteoporosis [2].

References:
[1] S. Aubrey Stoch, Stefan Zajic, Julie A. Stone, Deborah L. Miller, Lucas van Bortel, Kenneth C. Lasseter, Barnali Pramanik, Caroline Cilissen, Qi Liu, Lida Liu, Boyd B. Scott, Deborah Panebianco, Yu Ding, Keith Gottesdiener & John A. Wagner. Odanacatib, a selective cathepsin K inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics –results from single oral dose studies in healthy volunteers. British Journal of Clinical Pharmacology. 2012, 75, (5): 1240-1254.
[2] Matt S. Anderson, Isaias Noel Gendrano, Chengcheng Liu, Steven Jeffers,

Chantal Mahon, Anish Mehta, Kate Mostoller, Stefan Zajic, Denise Morris, Jessie Lee, and S. Aubrey Stoch. Odanacatib, a selective Cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. Endocrine Research. 2014, 99(2):552–560.

Chemical Properties

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	525.56
Cas No.	603139-19-1
Formula	C₂₅H₂₇F₄N₃O₃S
Solubility	insoluble in EtOH; insoluble in H2O; ≥17.7 mg/mL in DMSO
Chemical Name	(2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
SDF	Download SDF
Canonical SMILES	CC(C)(CC(C(=O)NC1(CC1)C#N)NC(C2=CC=C(C=C2)C3=CC=C(C=C3)S(=O)(=O)C)C(F)(F)F)F
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

A potent and selective inhibitor of cysteine protease cathepsin K (IC50 0.2 nM), discriminating against cathepsin B (1034 nM), L (2995 nM), and S (60 nM)
Targets	cathepsin K
IC50	0.2nM

Quality Control

Purity = 99.04%

Odanacatib (MK-0822) [603139-19-1]

Referência A2487-5mg

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Marca : APExBIO Technology

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Background

Chemical Properties

Biological Activity

Quality Control

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