A DPP-4 inhibitor
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Gemigliptin (tartrate)

Item No. 36016

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(2S)-2-amino-4-[5,8-dihydro-2,4-bis(trifluoromethyl)pyrido[3,4-d]pyrimidin-7(6H)-yl]-4-oxobutyl]-5,5-difluoro-2-piperidinone, (2R,3R)-2,3-dihydroxybutanedioate
CAS Number
1374639-74-3
Molecular Formula
C18H19F8N5O2 • XC4H6O6
Formula Weight
489.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 10 mg/mlEthanol: Slightly solublePBS (pH 7.2): 1 mg/ml
SMILES
FC(F)(C1=C2C(CN(CC2)C(C[C@H](N)CN3CC(F)(CCC3=O)F)=O)=NC(C(F)(F)F)=N1)F.OC([C@H](O)[C@@H](O)C(O)=O)=O
InChi Code
InChI=1S/C18H19F8N5O2.C4H6O6/c19-16(20)3-1-12(32)31(8-16)6-9(27)5-13(33)30-4-2-10-11(7-30)28-15(18(24,25)26)29-14(10)17(21,22)23;5-1(3(7)8)2(6)4(9)10/h9H,1-8,27H2;1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1
InChi Key
DPEZWSNXONTJHT-NDAAPVSOSA-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

    $57

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    10 mg

    $102

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    50 mg

    $390

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    100 mg

    $556

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Gemigliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 0.01 µM).1 It is selective for DPP-4 over DPP-8, DPP-9, and fibroblast activation protein-α (FAP-α; IC50s = 277.28, 233.72, 418.43 µM, respectively). Gemigliptin inhibits DPP-4 activity in isolated human, rat, dog, and monkey plasma (IC50s = 11.5, 14.5, 14.5, and 14 nM, respectively). It scavenges methylglyoxal in vitro and inhibits advanced glycation end product (AGE) formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s = 1.15, 11.69, and 1.39 mM, respectively).2 Gemigliptin (100 mg/kg) reduces the levels of circulating AGE and red blood cell IgG content in a db/db mouse model of diabetes when administered for 12 weeks. It decreases blood glucose and hemoglobin A1c (HbA1c) levels and reduces pancreatic β-cell damage in a dose-dependent manner in a mouse model of diabetes induced by a high-fat diet and streptozotocin (STZ; Item No. 13104).1 Gemigliptin also induces cytotoxicity in SW1736 and TPC-1 human thyroid cancer cells.3,4 Formulations containing gemigliptin have been used in the treatment of type 2 diabetes.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, S.-H., Jung, E., Yoon, M.K., et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur. J. Pharmacol. 788, 54-64 (2016).

    2. Jung, E., Kim, J., Kim, S.H., et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur. J. Pharmacol. 744, 98-102 (2014).

    3. Kim, S.H., Kang, J.G., Kim, C.S., et al. Gemigliptin, a novel dipeptidyl peptidase-IV inhibitor, exerts a synergistic cytotoxicity with the histone deacetylase inhibitor PXD101 in thyroid carcinoma cells. J. Endocrinol. Invest. 41(6), 677-689 (2018).

    4. Kim, S.H., Kang, J.G., Kim, C.S., et al. Synergistic cytotoxicity of the dipeptidyl peptidase-IV inhibitor gemigliptin with metformin in thyroid carcinoma cells. Endocrine 59(2), 383-394 (2018).