A potent cathepsin S inhibitor
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LY3000328

Item No. 29729

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(3R,4S)-3,4-dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluoro-benzamide
CAS Number
1373215-15-6
Molecular Formula
C25H29FN4O5
Formula Weight
484.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml
λmax
235 nm
SMILES
C=C(C1=CC=C(C)C=C1)C[C@@H]2[C@@H](CC(CC)=C)CCC3=CC=C(C4CCC(C5CCC5)CC4)C=C32
InChi Code
InChI=1S/C35H46/c1-5-24(2)21-33-20-18-31-17-19-32(30-15-13-29(14-16-30)28-7-6-8-28)23-35(31)34(33)22-26(4)27-11-9-25(3)10-12-27/h9-12,17,19,23,28-30,33-34H,2,4-8,13-16,18,20-22H2,1,3H3/t29?,30?,33-,34-/m1/s1
InChi Key
YTWOSVWRJQCECI-YUVTWRQCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $90

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    1 mg

    $168

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    5 mg

    $392

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    10 mg

    $696

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    Product Description

    LY3000328 is a potent cathepsin S inhibitor (IC50 = 7.7 nM for the human enzyme).1 It is selective for cathepsin S over cathepsin L, K, B, and V (IC50s = >10,000, >10,000, 4,390, and 21,500 nM, respectively). LY3000328 (1-30 mg/kg) reduces aortic diameter in a mouse model of calcium chloride-induced abdominal aortic aneurysm.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Jadhav, P.K., Schiffler, M.A., Gavardinas, K., et al. Discovery of cathepsin S inhibitor LY3000328 for the treatment of abdominal aortic aneurysm. ACS Med. Chem. Lett. 5(10), 1138-1142 (2014).