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KHK-IN-1

CAS No. 1303469-70-6

KHK-IN-1( Ketohexokinase inhibitor 8 | KHK-IN-8 )

Catalog No. M26731 CAS No. 1303469-70-6

KHK-IN-1 is a reversible and ATP-competitive inhibitor of ketohexokinase (KHK) with IC50 of 12 nM. In the ATP-binding region of KHK, KHK-IN-1 interacts with Asp-27B.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    KHK-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    KHK-IN-1 is a reversible and ATP-competitive inhibitor of ketohexokinase (KHK) with IC50 of 12 nM. In the ATP-binding region of KHK, KHK-IN-1 interacts with Asp-27B.
  • Description
    KHK-IN-1 is a reversible and ATP-competitive inhibitor of ketohexokinase (KHK) with IC50 of 12 nM. In the ATP-binding region of KHK, KHK-IN-1 interacts with Asp-27B.
  • In Vitro
    KHK-IN-1 stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4).KHK-IN-1 (0-10 μM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC50 value of 400 nM. Cell Viability Assay Cell Line:HepG2 cells Concentration:0-10 μM Incubation Time:Incubate 30 min, then add to 15 mM fructose and incubate for another 3 h Result:Exhibited inhibition of F1P production in HepG2 cell lysates (IC50=400 nM).
  • In Vivo
    KHK-IN-1 (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats. Animal Model:Male Sprague-Dawley rats (~250 g).Dosage:10 mg/kg Administration:Oral gavage; single Result:Exhibited reasonable oral bioavailability in rats (F=34%; oral t1/2=4 h), but had a high volume of distribution (Vdss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).
  • Synonyms
    Ketohexokinase inhibitor 8 | KHK-IN-8
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    GLP-1
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1303469-70-6
  • Formula Weight
    422.56
  • Molecular Formula
    C21H26N8S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CSc1ccccc1Nc1nc(nc2c(NCC3CC3)ncnc12)N1CCNCC1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Elahi D, et al. GLP-1 (9-36) amide, cleavage product of GLP-1 (7-36) amide, is a glucoregulatory peptide. Obesity (Silver Spring). 2008;16(7):1501-1509.
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