ONO-5334
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206464

CAS#: 868273-90-9

Description: ONO-5334 is a potent and orally available inhibitor of cathepsin K (Ki values of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat respectively). ONO-5334 improves bone strength by preferentially increasing cortical bone mass in ovariectomized rats. ONO-5334 inhibits N-terminal and C-terminal collagen crosslinks in serum and urine at similar plasma concentrations in postmenopausal women. ONO-5334 had entered clinical development for metabolic bone disorders with increased bone resorption, such as postmenopausal osteoporosis.


Chemical Structure

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ONO-5334
CAS# 868273-90-9

Theoretical Analysis

MedKoo Cat#: 206464
Name: ONO-5334
CAS#: 868273-90-9
Chemical Formula: C21H34N4O4S
Exact Mass: 438.23008
Molecular Weight: 438.59
Elemental Analysis: C, 57.51; H, 7.81; N, 12.77; O, 14.59; S, 7.31

Size Price Shipping out time Quantity
2mg USD 305 2 Weeks
5mg USD 670 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-08. Prices are subject to change without notice.

ONO-5334, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Synonym: ONO-5334; ONO 5334; ONO5334.

IUPAC/Chemical Name: N-((S)-3-(2-((R,Z)-3,4-dimethylthiazolidin-2-ylidene)hydrazinyl)-2,3-dioxo-1-(tetrahydro-2H-pyran-4-yl)propyl)cycloheptanecarboxamide

InChi Key: BTZCSXIUAFVRTE-CHGLIHOBSA-N

InChi Code: InChI=1S/C21H34N4O4S/c1-14-13-30-21(25(14)2)24-23-20(28)18(26)17(15-9-11-29-12-10-15)22-19(27)16-7-5-3-4-6-8-16/h14-17H,3-13H2,1-2H3,(H,22,27)(H,23,28)/b24-21-/t14-,17+/m1/s1

SMILES Code: O=C(N/N=C1SC[C@@H](C)N\1C)C([C@@H](NC(C2CCCCCC2)=O)C3CCOCC3)=O

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 438.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Duong LT, Leung AT, Langdahl B. Cathepsin K Inhibition: A New Mechanism for the Treatment of Osteoporosis. Calcif Tissue Int. 2015 Sep 3. [Epub ahead of print] PubMed PMID: 26335104.

2: Tanaka M, Hashimoto Y, Hasegawa C. An oral cathepsin K inhibitor ONO-5334 inhibits N-terminal and C-terminal collagen crosslinks in serum and urine at similar plasma concentrations in postmenopausal women. Bone. 2015 Jul 16;81:178-185. doi: 10.1016/j.bone.2015.07.016. [Epub ahead of print] PubMed PMID: 26188109.

3: Gamsjäger M, Resch H. [Cathepsin K antagonists: preclinical and clinical data]. Wien Med Wochenschr. 2015 Feb;165(3-4):65-70. doi: 10.1007/s10354-014-0336-3. Epub 2015 Jan 9. German. PubMed PMID: 25572547.

4: Ochi Y, Yamada H, Mori H, Nakanishi Y, Nishikawa S, Kayasuga R, Kawada N, Kunishige A, Hashimoto Y, Tanaka M, Sugitani M, Kawabata K. Effects of eight-month treatment with ONO-5334, a cathepsin K inhibitor, on bone metabolism, strength and microstructure in ovariectomized cynomolgus monkeys. Bone. 2014 Aug;65:1-8. doi: 10.1016/j.bone.2014.04.023. Epub 2014 Apr 27. PubMed PMID: 24784023.

5: Hasegawa C, Kastrissios H, Monteleone J, Ohno T, Umemura T, Ohyama M, Nagase S, Small M, Deacon S, Ogawa M, Ieiri I. Modeling and simulation of bone mineral density response from a phase 2 study of ONO-5334, a new cathepsin K inhibitor, to support dose selection in osteoporosis. J Clin Pharmacol. 2014 Aug;54(8):937-48. doi: 10.1002/jcph.279. Epub 2014 Feb 28. PubMed PMID: 24615681.

6: Nagase S, Ohyama M, Hashimoto Y, Small M, Sharpe J, Manako J, Kuwayama T, Deacon S. Bone turnover markers and pharmacokinetics of a new sustained-release formulation of the cathepsin K inhibitor, ONO-5334, in healthy post-menopausal women. J Bone Miner Metab. 2015 Jan;33(1):93-100. doi: 10.1007/s00774-013-0558-2. Epub 2014 Jan 24. PubMed PMID: 24458199.

7: Ochi Y, Yamada H, Mori H, Kawada N, Kayasuga R, Nakanishi Y, Tanaka M, Imagawa A, Ohmoto K, Kawabata K. ONO-5334, a cathepsin K inhibitor, improves bone strength by preferentially increasing cortical bone mass in ovariectomized rats. J Bone Miner Metab. 2014 Nov;32(6):645-52. doi: 10.1007/s00774-013-0542-x. Epub 2013 Dec 8. PubMed PMID: 24317478.

8: Hasegawa C, Ohno T, Umemura T, Honda N, Ohyama M, Nagase S, Small M, Deacon S, Ogawa M, Ieiri I. Population pharmacokinetic and pharmacodynamic modeling of different formulations of ONO-5334, cathepsin K inhibitor, in Caucasian and Japanese postmenopausal females. J Clin Pharmacol. 2014 Jan;54(1):23-34. doi: 10.1002/jcph.186. Epub 2013 Oct 10. PubMed PMID: 24115072.

9: Tanaka M, Hashimoto Y, Sekiya N, Honda N, Deacon S, Yamamoto M. Effects of novel cathepsin K inhibitor ONO-5334 on bone resorption markers: a study of four sustained release formulations with different pharmacokinetic patterns. J Bone Miner Metab. 2014 Jul;32(4):447-54. doi: 10.1007/s00774-013-0517-y. Epub 2013 Oct 11. PubMed PMID: 24114194.

10: Engelke K, Nagase S, Fuerst T, Small M, Kuwayama T, Deacon S, Eastell R, Genant HK. The effect of the cathepsin K inhibitor ONO-5334 on trabecular and cortical bone in postmenopausal osteoporosis: the OCEAN study. J Bone Miner Res. 2014 Mar;29(3):629-38. doi: 10.1002/jbmr.2080. PubMed PMID: 24038152.

11: Eastell R, Nagase S, Small M, Boonen S, Spector T, Ohyama M, Kuwayama T, Deacon S. Effect of ONO-5334 on bone mineral density and biochemical markers of bone turnover in postmenopausal osteoporosis: 2-year results from the OCEAN study. J Bone Miner Res. 2014 Feb;29(2):458-66. doi: 10.1002/jbmr.2047. PubMed PMID: 23873670.

12: Nagase S, Hashimoto Y, Small M, Ohyama M, Kuwayama T, Deacon S. Serum and urine bone resorption markers and pharmacokinetics of the cathepsin K inhibitor ONO-5334 after ascending single doses in post menopausal women. Br J Clin Pharmacol. 2012 Dec;74(6):959-70. doi: 10.1111/j.1365-2125.2012.04307.x. PubMed PMID: 22533981; PubMed Central PMCID: PMC3522809.

13: Boonen S, Rosenberg E, Claessens F, Vanderschueren D, Papapoulos S. Inhibition of cathepsin K for treatment of osteoporosis. Curr Osteoporos Rep. 2012 Mar;10(1):73-9. doi: 10.1007/s11914-011-0085-9. Review. PubMed PMID: 22228398.

14: Ochi Y, Yamada H, Mori H, Nakanishi Y, Nishikawa S, Kayasuga R, Kawada N, Kunishige A, Hashimoto Y, Tanaka M, Sugitani M, Kawabata K. Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism. Bone. 2011 Dec;49(6):1351-6. doi: 10.1016/j.bone.2011.09.041. Epub 2011 Sep 18. PubMed PMID: 21982869.

15: Wijkmans J, Gossen J. Inhibitors of cathepsin K: a patent review (2004 - 2010). Expert Opin Ther Pat. 2011 Oct;21(10):1611-29. doi: 10.1517/13543776.2011.616283. Review. PubMed PMID: 21923554.

16: Nagase S, Ohyama M, Hashimoto Y, Small M, Kuwayama T, Deacon S. Pharmacodynamic effects on biochemical markers of bone turnover and pharmacokinetics of the cathepsin K inhibitor, ONO-5334, in an ascending multiple-dose, phase 1 study. J Clin Pharmacol. 2012 Mar;52(3):306-18. doi: 10.1177/0091270011399080. Epub 2011 Jun 30. PubMed PMID: 21719717.

17: Eastell R, Nagase S, Ohyama M, Small M, Sawyer J, Boonen S, Spector T, Kuwayama T, Deacon S. Safety and efficacy of the cathepsin K inhibitor ONO-5334 in postmenopausal osteoporosis: the OCEAN study. J Bone Miner Res. 2011 Jun;26(6):1303-12. doi: 10.1002/jbmr.341. PubMed PMID: 21312264.

18: Manako J. [New approach for osteoporosis treatment: cathepsin K inhibitor, ONO-5334]. Clin Calcium. 2011 Jan;21(1):64-9. doi: CliCa11016469. Review. Japanese. PubMed PMID: 21187596.

19: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Sep;32(7):517-48. doi: 10.1358/mf.2010.32.7.1549223. PubMed PMID: 21069103.