Drug Information

Drug (ID: DG00980) and It's Reported Resistant Information

• Name: Gliquidone
• Synonyms: Gliquidone; 33342-05-1; Glurenorm; Gliquidonum; ARDF 26; C27H33N3O6S; UNII-C7C2QDD75P; 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea; Beglynor; MFCD00631870; C7C2QDD75P; ARDF-26; N-(Cyclohexylcarbamoyl)-4-(2-(7-methoxy-4,4-dimethyl-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)benzenesulfonamide; NCGC00016819-01; Gliquidona; CAS-33342-05-1; DSSTox_CID_3096; DSSTox_RID_76873; DSSTox_GSID_23096; Gliquidonum [INN-Latin]; 3-Cyclohexyl-1-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-isoquinolin-2-yl)ethyl]phenyl]sulfonyl-urea; Gliquidona [INN-Spanish]; ARDF 26 SE; AR-DF 26; Glurenorm (TN); 1-cyclohexyl-3-({4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]benzene}sulfonyl)urea; Gliquidone (INN); SMR000685793; Gliquidone [INN:BAN]; EINECS 251-463-2; BRN 1559726; Gliquidon; Gliquidone,(S); Gliquidone, 98%; Prestwick0_000991; Prestwick1_000991; Prestwick2_000991; Prestwick3_000991; Oprea1_069443; SCHEMBL37769; BSPBio_001081; 1-Cyclohexyl-3-((p-(2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolyl)ethyl)phenyl)sulfonyl)urea; 1-Cyclohexyl-3-(p-beta-(4,4-dimethyl-2-methoxy-1,3-(2H,4H)-isoquinolinedione-2-yl)phenethyl)sulfonylurea; Benzenesulfonamide, N-((cyclohexylamino)carbonyl)-4-(2-(3,4-dihydro-7-methoxy-4,4-dimethyl-1,3-dioxo-2(1H)-isoquinolinyl)ethyl)-; MLS000881123; MLS000881174; MLS002154087; SPBio_002972; BPBio1_001191; CHEMBL383634; DTXSID4023096; CHEBI:93416; HMS1571G03; HMS2098G03; HMS2964J06; HMS3652O05; HMS3715G03; ACT06290; BCP11927; HY-B1114; ZINC1482077; Tox21_110629; BDBM50248247; AKOS001037880; Tox21_110629_1; CCG-220991; CM14378; CS-4646; DB01251; KS-5239; MCULE-6775445815; NCGC00016819-02; NCGC00016819-03; NCGC00016819-05; NCGC00016819-06; NCGC00179315-01; AC-23356; N-[(cyclohexylamino)carbonyl]-4-{2-[4,4-dimethyl-7-(methyloxy)-1,3-dioxo-3,4-dihydroisoquinolin-2(1H)-yl]ethyl}benzenesulfonamide; N-(cyclohexylcarbamoyl)-4-(2-(7-methoxy-; AB00513989; FT-0630570; G0332; S3151; SW197285-3; D02430; J10245; T72318; 4,4-dimethyl-1,3-dioxo-3,4-dihydroisoquinolin; AB00513989_07; 342G051; A821736; SR-01000833866; J-019153; Q5569924; SR-01000833866-2; BRD-K80396088-001-03-9; 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-2-isoquinolinyl)ethyl]phenyl]sulfonylurea; 1-Cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-2-isoquinolyl)ethyl]phenyl]sulfonyl-urea;Gliquidone; 3-cyclohexyl-1-({4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]benzene}sulfonyl)urea; N-cyclohexylcarbamoyl-4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-1,2,3,4- tetrahydroisoquinolin-2-yl)ethyl]benzenesulfonamide
• Indication:
  In total 1 Indication(s)
  Diabetic complication [ICD-11: 5A2Y]; Approved; [1]
• Target: Inward rectifier potassium channel Kir1.2 (KCNJ10); KCJ10_HUMAN; [1]
• Formula: C27H33N3O6S
• IsoSMILES: CC1(C2=C(C=C(C=C2)OC)C(=O)N(C1=O)CCC3=CC=C(C=C3)S(=O)(=O)NC(=O)NC4CCCCC4)C
• InChI: 1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)
• InChIKey: LLJFMFZYVVLQKT-UHFFFAOYSA-N
• PubChem CID: 91610
• ChEBI ID: CHEBI:93416
• TTD Drug ID: D06HBQ
• VARIDT ID: DR00405
• INTEDE ID: DR0779
• DrugBank ID: DB01251

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-05: Endocrine/nutritional/metabolic diseases

Insulin-resistance syndrome [ICD-11: 5A44]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: RAC serine/threonine-protein kinase (AKT) [1]

• Molecule Alteration: Function; Activation
• Sensitive Disease: Insulin-resistance syndrome [ICD-11: 5A44.0]
• Experimental Note: Discovered Using In-vivo Testing Model
• In Vivo Model: Sur1 knockout rats model; Rattus norvegicus
• Experiment for Drug Resistance: IPGTT assay; IPITT assay; Hyperinsulinemic-euglycemic clamp test assay
• Mechanism Description: Gliquidone alleviates hepatic insulin resistance by increasing glycogen synthesis and decreasing gluconeogenesis in vivo. The mechanism of gliquidone might be related to the activation of AKT, rather than AMPK.

References

• Ref 1: Gliquidone ameliorates hepatic insulin resistance in streptozotocin-induced diabetic Sur1(-/-) rats .Eur J Pharmacol. 2021 Sep 5;906:174221. doi: 10.1016/j.ejphar.2021.174221. Epub 2021 Jun 1. 10.1016/j.ejphar.2021.174221