Balicatib
featured

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

MedKoo CAT#: 510221

CAS#: 354813-19-7

Description: Balicatib, also known as AAE581, is an inhibitor of the osteoclastic enzyme cathepsin K. Balicatib partially prevented ovariectomy-induced changes in bone mass, inhibited bone turnover at most sites, and had an unexpected stimulatory effect on periosteal bone formation.


Price and Availability

Size
Price

100mg
USD 950
1g
USD 3250
Size
Price

200mg
USD 1650
2g
USD 4950
Size
Price

500mg
USD 2650
5g
USD 8250

Balicatib, 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.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 510221
Name: Balicatib
CAS#: 354813-19-7
Chemical Formula: C23H33N5O2
Exact Mass: 411.26343
Molecular Weight: 411.54
Elemental Analysis: C, 67.12; H, 8.08; N, 17.02; O, 7.78


Synonym: Balicatib; AAE581; AAE-581; AAE 581

IUPAC/Chemical Name: N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide

InChi Key: LLCRBOWRJOUJAE-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H33N5O2/c1-2-14-27-15-17-28(18-16-27)20-8-6-19(7-9-20)21(29)26-23(10-4-3-5-11-23)22(30)25-13-12-24/h6-9H,2-5,10-11,13-18H2,1H3,(H,25,30)(H,26,29)

SMILES Code: O=C(NC1(C(NCC#N)=O)CCCCC1)C2=CC=C(N3CCN(CCC)CC3)C=C2


Technical Data

Appearance:
white to off-white 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).

Harmonized System Code:
293490


Additional Information

  
  
 
 


References

1: Rünger TM, Adami S, Benhamou CL, Czerwiński E, Farrerons J, Kendler DL, Mindeholm L, Realdi G, Roux C, Smith V. Morphea-like skin reactions in patients treated with the cathepsin K inhibitor balicatib. J Am Acad Dermatol. 2012 Mar;66(3):e89-96. doi: 10.1016/j.jaad.2010.11.033. Epub 2011 May 14. PubMed PMID: 21571394.

2: Jerome C, Missbach M, Gamse R. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2012 Jan;23(1):339-49. doi: 10.1007/s00198-011-1593-2. Epub 2011 Mar 5. PubMed PMID: 21380636.

3: Jerome C, Missbach M, Gamse R. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011 Dec;22(12):3001-11. doi: 10.1007/s00198-011-1529-x. Epub 2011 Feb 10. PubMed PMID: 21308366.

4: Chappard D, Libouban H, Mindeholm L, Baslé MF, Legrand E, Audran M. The cathepsin K inhibitor AAE581 induces morphological changes in osteoclasts of treated patients. Microsc Res Tech. 2010 Jul;73(7):726-32. doi: 10.1002/jemt.20813. PubMed PMID: 20025055.

5: Desmarais S, Massé F, Percival MD. Pharmacological inhibitors to identify roles of cathepsin K in cell-based studies: a comparison of available tools. Biol Chem. 2009 Sep;390(9):941-8. doi: 10.1515/BC.2009.092. PubMed PMID: 19453281.

6: Le Gall C, Bonnelye E, Clézardin P. Cathepsin K inhibitors as treatment of bone metastasis. Curr Opin Support Palliat Care. 2008 Sep;2(3):218-22. doi: 10.1097/SPC.0b013e32830baea9. Review. PubMed PMID: 18685424.

7: Peroni A, Zini A, Braga V, Colato C, Adami S, Girolomoni G. Drug-induced morphea: report of a case induced by balicatib and review of the literature. J Am Acad Dermatol. 2008 Jul;59(1):125-9. doi: 10.1016/j.jaad.2008.03.009. Epub 2008 Apr 14. Review. PubMed PMID: 18410981.

8: Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong le T, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. doi: 10.1016/j.bmcl.2007.12.047. Epub 2008 Jan 15. PubMed PMID: 18226527.

9: Desmarais S, Black WC, Oballa R, Lamontagne S, Riendeau D, Tawa P, Duong le T, Pickarski M, Percival MD. Effect of cathepsin k inhibitor basicity on in vivo off-target activities. Mol Pharmacol. 2008 Jan;73(1):147-56. Epub 2007 Oct 16. PubMed PMID: 17940194.

10: Vasiljeva O, Reinheckel T, Peters C, Turk D, Turk V, Turk B. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403. Review. PubMed PMID: 17311556.