WAY-100635

CAS No. 162760-96-5

WAY-100635( WAY 100635 | WAY100635 )

Catalog No. M12413 CAS No. 162760-96-5

A potent and selective 5-HT1A receptor antagonist; also acts as potent full agonist at the D4 receptor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    WAY-100635
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent and selective 5-HT1A receptor antagonist; also acts as potent full agonist at the D4 receptor.
  • Description
    A potent and selective 5-HT1A receptor antagonist; also acts as potent full agonist at the D4 receptor; completely prevents not only the hyperpolarization, with an IC50 of 1.3 nM, but also the decrease in membrane input resistance produced by 5-HT and 5-carboxamidotryptamine with IC50 of 22.5 μM and 50 nM, respectively. Anxiety Phase 1 Discontinued.
  • In Vitro
    The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors.WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 receptor (3.3 nM) .
  • In Vivo
    WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat. Animal Model:Male Sprague-Dawley rats (220-240 g)Dosage:1 mg/kg Administration:Subcutaneous injection (Pharmacokinetic study)Result:Reduced total abstinence score, increased immobility time and the burying behavior was increased.
  • Synonyms
    WAY 100635 | WAY100635
  • Pathway
    GPCR/G Protein
  • Target
    5-HT Receptor
  • Recptor
    5-HT Receptor
  • Research Area
    Neurological Disease
  • Indication
    Anxiety

Chemical Information

  • CAS Number
    162760-96-5
  • Formula Weight
    422.563
  • Molecular Formula
    C25H34N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C(C1CCCCC1)N(CCN2CCN(C3=CC=CC=C3OC)CC2)C4=NC=CC=C4
  • Chemical Name
    N-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-N-(pyridin-2-yl)cyclohexanecarboxamide

Shipping & Storage Information

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

Reference

1. Corradetti R, et al. J Pharmacol Exp Ther. 1996 Aug;278(2):679-88. 2. Fornal CA, et al. J Pharmacol Exp Ther. 1996 Aug;278(2):752-62. 3. García G, et al. Eur J Med Chem. 2014 Oct 6;85:795-806.
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