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Drug Details

General Information of the Drug (ID: DR5892)
Name
GSK2041706
Synonyms
GPR119 agonist; 1037779-47-7; SCHEMBL2370813; ZINC95929383; 5-[4-[(2R)-4-(3-fluoro-4-methylsulfonylphenoxy)butan-2-yl]piperidin-1-yl]-3-propan-2-yl-1,2,4-oxadiazole
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Molecular Type
Small molecule
Disease Type 2 diabetes mellitus [ICD-11: 5A11] Investigative [1]
Structure
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2D MOL

3D MOL

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Formula
C21H30FN3O4S
PubChem CID
24964226
Canonical SMILES
CC(C)C1=NOC(=N1)N2CCC(CC2)C(C)CCOC3=CC(=C(C=C3)S(=O)(=O)C)F
InChI
1S/C21H30FN3O4S/c1-14(2)20-23-21(29-24-20)25-10-7-16(8-11-25)15(3)9-12-28-17-5-6-19(18(22)13-17)30(4,26)27/h5-6,13-16H,7-12H2,1-4H3/t15-/m1/s1
InChIKey
AJJISMLYIMQAKP-OAHLLOKOSA-N
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Metformin      Galega officinalis     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [1]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    In-vivo Model Diet-induced obese (DIO) mouse models were used in this study.
                    Experimental
                    Result(s)
The combination of GSK2041706 with metformin caused greater reductions in cumulative food intake (22.2% at 30 mg/kg and 37.5% at 100 mg/kg) and higher fed plasma glucagon-like peptide 1 and peptide tyrosine tyrosine levels and decreased plasma insulin and glucose-dependent insulinotropic polypeptide levels compared with their monotherapy groups.
Target and Pathway
Target(s) Programmed cell death protein 5 (PDCD5)  Molecule Info  [2]
References
Reference 1 Synergistic Effects of a GPR119 Agonist with Metformin on Weight Loss in Diet-Induced Obese Mice. J Pharmacol Exp Ther. 2015 Jun;353(3):496-504.
Reference 2 Synergistic antitumoral efficacy of a novel replicative adenovirus SG611-PDCD5 and daunorubicin in human leukemic cells. Onco Targets Ther. 2018 Aug 23;11:5121-5132.
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Cite NPCDR
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Correspondence

X. N. Sun, Y. T. Zhang, Y. Zhou, X. C. Lian, L. L. Yan, T. Pan, T. Jin, H. Xie, Z. M. Liang, W. Q. Qiu, J. X. Wang, Z. R. Li, F. Zhu*, X. B. Sui*. NPCDR: natural product-based drug combination and its disease-specific molecular regulation. Nucleic Acids Research. 50(D1): 1324-1333 (2020). PMID: 34664659

Prof. Feng ZHU  (zhufeng@zju.edu.cn)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China


Prof. Xinbing SUI  (hzzju@hznu.edu.cn)

School of Pharmacy and Department of Medical Oncology, the Affiliated Hospital of Hangzhou Normal University, Hangzhou Normal University, Hangzhou, China