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    Cathepsin Inhibitor 1
    Cathepsin Inhibitor 1

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0699
    CAS #: 225120-65-0Purity ≥98%

    Description: Cathepsin Inhibitor 1 (CTS-IN-1) is a novel and potent inhibitor of Cathepsin (L, L2, S, K, B) with the potential to be used in the treatment of osteoarthritis. It inhibits Cathepsin (L, L2, S, K, B) with pIC50 values of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. Osteoarthritis is currently recognized as a chronic degenerative disease, which is caused by the loss of articular cartilage and damage to underlying bone, resulting in joint instability and pain. The lysosomal cysteine protease2 Cathepsin L (CatL) is found to be a potential target for intervention in treatment of osteoarthritis. After secreted into the extracellular matrix, CatL can degrade proteoglycans such as aggrecan4 and type II collagen, which are the major components of articular cartilage.

    References: Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.

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    Molecular Weight (MW)401.89
    FormulaC20H24ClN5O2
    CAS No.225120-65-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: 50 mg/mL (124.4 mM)
    Other info

    Chemical Name: (S)-3-(tert-butyl)-N-(3-(3-chlorophenyl)-1-((cyanomethyl)amino)-1-oxopropan-2-yl)-1-methyl-1H-pyrazole-5-carboxamide

    InChi Key: MZRVIHRERYCHBL-HNNXBMFYSA-N

    InChi Code: InChI=1S/C20H24ClN5O2/c1-20(2,3)17-12-16(26(4)25-17)19(28)24-15(18(27)23-9-8-22)11-13-6-5-7-14(21)10-13/h5-7,10,12,15H,9,11H2,1-4H3,(H,23,27)(H,24,28)/t15-/m0/s1

    SMILES Code: ClC1=CC=CC(C[[email protected]@H](C(NCC#N)=O)NC(C2=CC(C(C)(C)C)=NN2C)=O)=C1

    Synonyms

    Cathepsin-Inhibitor-1; CTS-IN-1; Cathepsin Inhibitor 1; CTS IN 1


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    In Vitro

    In vitro activity: The CatL pIC50 value of Cathepsin Inhibitor 1 was found to exceed that of its analog by 1.6 units. Moreover, CatS (ΔpIC50 = -0.1) and CatL2 (ΔpIC50 = 0.5) were much less sensitive to the structural change of Cathepsin Inhibitor 1, leading to an improved selectivity profile relative to its analog. Cathepsin Inhibitor 1 was as least as selective with respect to CatB and CatS as previously described CatL inhibitors. The crystal structure of its another analog bound to CatL provided the rationale for the SAR observed for Cathepsin Inhibitor 1. The 1-methyl group of the pyrazole made some contact with Leu69 and appeared to force the pyrazole ring out of co-planarity with the amide, likely functioning as a conformational lock.

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    References

    Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     
    Relationships between pIC50 and ClogP for Cathepsins L, L2 and S showing ...
     Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.
     
    Crystal structure of 26 bound to Cathepsin L showing molecular surface of the ...
    Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.
     
    Potential binding mode of the adduct of 1 with Cathepsin L showing molecular ...
    Bioorg Med Chem Lett. 2009 Aug 1;19(15):4280-3.


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