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TC-N 22A

CAS No. 1314140-00-5

TC-N 22A( —— )

Catalog No. M33939 CAS No. 1314140-00-5

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TC-N 22A
  • Note
    Research use only, not for human use.
  • Brief Description
    TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier.
  • Description
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
  • In Vitro
    TC-N 22A is selected for mGlu4 and has an EC50 of 9 nM in human mGlu4-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC50>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC50 >10 μM) and shows low potential for hERG channel inhibition.
  • In Vivo
    TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats.
  • Synonyms
    ——
  • Pathway
    Neuroscience
  • Target
    GluR
  • Recptor
    GluR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1314140-00-5
  • Formula Weight
    283.35
  • Molecular Formula
    C14H13N5S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    N(C1=NC=2C=3C(=NNC3)CCCC2S1)C4=CC=CC=N4
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Sang-Phyo Hong, et al. Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators. J Med Chem. 2011 Jul 28;54(14):5070-81.?
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