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VU6005649

CAS No. 2137047-43-7

VU6005649( —— )

Catalog No. M26504 CAS No. 2137047-43-7

VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    VU6005649
  • Note
    Research use only, not for human use.
  • Brief Description
    VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).
  • Description
    VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively).(In Vitro):VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor (EC50s: 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively). VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.(In Vivo):In wild-type mice, VU6005649 shows modest but significant pro-cognitive effects on associative learning and the first example of the efficacy of a mGlu7/8 positive allosteric modulator (PAM) in this model.
  • In Vitro
    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively. VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.
  • In Vivo
    When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model.
  • Synonyms
    ——
  • Pathway
    Neuroscience
  • Target
    GluR
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2137047-43-7
  • Formula Weight
    357.284
  • Molecular Formula
    C16H12F5N3O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (139.95 mM)
  • SMILES
    COc1ccc(-c2c(C)nn3c(cc(C)nc23)C(F)(F)F)c(F)c1F
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Chen XL, et al. An uncommon plant growth regulator, diethyl aminoethyl hexanoate, is highly effective in tissue cultures of the important medicinal plant purple coneflower (Echinacea purpurea L.). Biomed Res Int. 2013;2013:540316.
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