L873724

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

Hodoodo CAT#: H532102

CAS#: 603139-12-4

Description: L873724 is a cathepsin K inhibitor.

Chemical Structure

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L873724
CAS# 603139-12-4
Instruction

Theoretical Analysis

Hodoodo Cat#: H532102
Name: L873724
CAS#: 603139-12-4
Chemical Formula: C23H26F3N3O3S
Exact Mass: 481.16
Molecular Weight: 481.530
Elemental Analysis: C, 57.37; H, 5.44; F, 11.84; N, 8.73; O, 9.97; S, 6.66

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: L873724; L 873724; L-873724.

IUPAC/Chemical Name: (2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide

InChi Key: VYFDSJLOCIGIKP-SFTDATJTSA-N

InChi Code: InChI=1S/C23H26F3N3O3S/c1-15(2)14-20(22(30)28-13-12-27)29-21(23(24,25)26)18-6-4-16(5-7-18)17-8-10-19(11-9-17)33(3,31)32/h4-11,15,20-21,29H,13-14H2,1-3H3,(H,28,30)/t20-,21-/m0/s1

SMILES Code: CC(C)C[C@H](N[C@@H](C1=CC=C(C2=CC=C(S(=O)(C)=O)C=C2)C=C1)C(F)(F)F)C(NCC#N)=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

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 481.53 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Zhuo Y, Gauthier JY, Black WC, Percival MD, Duong LT. Inhibition of bone
resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone.
2014 Oct;67:269-80. doi: 10.1016/j.bone.2014.07.013. PubMed PMID: 25038310.


2: Pennypacker BL, Oballa RM, Levesque S, Kimmel DB, Duong LT. Cathepsin K
inhibitors increase distal femoral bone mineral density in rapidly growing
rabbits. BMC Musculoskelet Disord. 2013 Dec 9;14:344. doi:
10.1186/1471-2474-14-344. PubMed PMID: 24321244; PubMed Central PMCID:
PMC3878918.


3: Veilleux A, Black WC, Gauthier JY, Mellon C, Percival MD, Tawa P, Falgueyret
JP. Probing cathepsin S activity in whole blood by the activity-based probe
BIL-DMK: cellular distribution in human leukocyte populations and evidence of
diurnal modulation. Anal Biochem. 2011 Apr 1;411(1):43-9. doi:
10.1016/j.ab.2010.11.022. PubMed PMID: 21094118.


4: 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.


5: Dejica VM, Mort JS, Laverty S, Percival MD, Antoniou J, Zukor DJ, Poole AR.
Cleavage of type II collagen by cathepsin K in human osteoarthritic cartilage. Am
J Pathol. 2008 Jul;173(1):161-9. doi: 10.2353/ajpath.2008.070494. PubMed PMID:
18511517; PubMed Central PMCID: PMC2438294.


6: Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, 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. PubMed PMID: 18226527.


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


8: Black WC, Percival MD. The consequences of lysosomotropism on the design of
selective cathepsin K inhibitors. Chembiochem. 2006 Oct;7(10):1525-35. Review.
PubMed PMID: 16921579.


9: Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger
S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M,
Truong VL, Wesolowski G, Zamboni R, Black WC. Identification of a potent and
selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr
1;16(7):1985-9. PubMed PMID: 16413777.