Odanacatib Inhibitor CAS No. 603139-19-1

Cat. No.	Name	Size	Price
KI3659	Odanacatib	5 mg	$460
	Odanacatib	10 mg	$800
	Odanacatib	50 mg	$2840

Chemical Characteristic

Product Name	Odanacatib
Synonyms	MK-0822
CAS No.	603139-19-1
Molecular Weight	525.57
Formula	C₂₅H₂₇F₄N₃O₃S
Chemical Name	(2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide
Smiles	C(=O)([C@H](CC(C)(C)F)N[C@H](C(F)(F)F)c1ccc(cc1)c1ccc(cc1)S(=O)(=O)C)NC1(CC1)C#N
Chemical Structure

Biological activities

Odanacatib (pINN; codenamed MK-0822) is an investigational treatment for osteoporosis and bone metastasis^[1]. It is an inhibitor of cathepsin K, an enzyme involved in bone resorption^[2]. Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3. In vivo, in preclinical rats, Odanacatib (10 mg/kg) exhibits excellent pharmacokinetics with clearance (Cl: 2 mL kg-1 min-1), low volume of distribution (Vdss: 1.1 L kg-1), half-life (T1/2: 6 hours) and oral bioavailability (F: 8%), respectively.

References

[1] Le Gall C, Bonnelye E, Cl?zardin P. Cathepsin K inhibitors as treatment of bone metastasis. Current Opinion in Supportive and Palliative Care. 2008, 2 (3): 218. [2] Gauthier JY, Chauret N, Cromlish W, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg. Med. Chem. Lett. 2008,18 (3): 923-928. [3] Zhuo Y, Gauthier JY, Black WC, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014, 67:269-280

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