A DPP-8 and DPP-9 inhibitor
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1G244

Item No. 18306

Product Insert (PDF)
Technical Information
Formal Name
2S-amino-4-[4-[bis(4-fluorophenyl)methyl]-1-piperazinyl]-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-butanedione
CAS Number
847928-32-9
Synonyms
  • PTX1210
Molecular Formula
C29H30F2N4O2
Formula Weight
504.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
FC1=CC=C(C(N2CCN(C(C[C@H](N)C(N3CC4=C(C=CC=C4)C3)=O)=O)CC2)C5=CC=C(F)C=C5)C=C1
InChi Code
InChI=1S/C29H30F2N4O2/c30-24-9-5-20(6-10-24)28(21-7-11-25(31)12-8-21)34-15-13-33(14-16-34)27(36)17-26(32)29(37)35-18-22-3-1-2-4-23(22)19-35/h1-12,26,28H,13-19,32H2/t26-/m0/s1
InChi Key
ZKIQFLSGMMYCGS-SANMLTNESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $83

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    10 mg

    $125

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    50 mg

    $413

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    100 mg

    $660

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    1G244 is an inhibitor of dipeptidyl peptidase 8 (DPP-8) and DPP-9 (IC50s = 14 and 53 nM, respectively).1 It is selective for DPP-8 and DPP-9 over DPP-4, DPP-2, and fibroblast activation protein (FAP; IC50s = >100 µM for all). 1G244 (20 µM) inhibits the differentiation of 3T3-L1 cells into adipocytes.2 It induces caspase-1-dependent pyroptosis in RAW 264.7 macrophages when used at a concentration of 10 µM.3 1G244 (2 mg/kg) decreases atherosclerotic lesion area and M1-like macrophage plaque infiltration in apoE-/- mice in a model of atherosclerosis induced by a high-fat diet.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wu, J.J., Tang, H.K., Yeh, T.K., et al. Biochemistry, pharmacokinetics, and toxicology of a potent and selective DPP8/9 inhibitor. Biochem. Pharmacol. 78(2), 203-210 (2009).

    2. Han, R., Wang, X., Bachovchin, W., et al. Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation. Sci. Rep. 5(12348), 1-11 (2015).

    3. Okondo, M.C., Johnson, D.C., Sridharan, R., et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat. Chem. Biol. 13(1), 46-53 (2017).

    4. Wiśniewska, A., Czepiel, K., Stachowicz, A., et al. The antiatherosclerotic action of 1G244 - An inhibitor of dipeptidyl peptidases 8/9 - is mediated by the induction of macrophage death. Eur. J. Pharmacol. 944, 175566 (2023).