THIP

CAS No. 64603-91-4

THIP( Gaboxadol | Gaboxadolum )

Catalog No. M26482 CAS No. 64603-91-4

THIP has a strong affinity for the δ subunit of GABAA receptors. THIP is a functionally selective GABAAR ligand, agonistic to α4β1δ, α4β3δ, and weakly antagonistic to αβγ and α4β2δ GABAARs.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    THIP
  • Note
    Research use only, not for human use.
  • Brief Description
    THIP has a strong affinity for the δ subunit of GABAA receptors. THIP is a functionally selective GABAAR ligand, agonistic to α4β1δ, α4β3δ, and weakly antagonistic to αβγ and α4β2δ GABAARs.
  • Description
    THIP has a strong affinity for the δ subunit of GABAA receptors. THIP is a functionally selective GABAAR ligand, agonistic to α4β1δ, α4β3δ, and weakly antagonistic to αβγ and α4β2δ GABAARs.
  • In Vitro
    THIP (1 μM; 5 s) induces a robust tonic GABAA-mediated current in layer 2/3 neurons.THIP (1 μM; 1 s) shows no affect miniature IPSCs in layer 2/3 neurons.Cell Viability Assay Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)Concentration:1 μM Incubation Time:5 s Result:Induced a tonic current of 43.2 pA.Cell Viability Assay Cell Line:Layer 2/3 neurons (from male postnatal day 13-19 C57BL/6 mice)Concentration:1 μM Incubation Time:1 s Result:Resulted in only minor changes in the amplitude and frequency of mIPSCs.
  • In Vivo
    THIP (Gaboxadol) (0.5, 5.0 mg/kg; p.o.; single) shws a good oral utilization, with Fa values of 110% and 83% for dosage of 0.5 and 5.0 mg/kg, respectively. Animal Model:Sprague-Dawley rats (255-276 g).Dosage:2.5 mg/kg (for i.v.); 0.5 and 5.0 mg/kg (for p.o.).
  • Synonyms
    Gaboxadol | Gaboxadolum
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    PPARγ
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    64603-91-4
  • Formula Weight
    140.142
  • Molecular Formula
    C6H8N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (356.79 mM)
  • SMILES
    Oc1noc2CNCCc12
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Rasmus K Petersen, et al. Pharmacophore-driven identification of PPARγ agonists from natural sources. J Comput Aided Mol Des. 2011 Feb;25(2):107-16.
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