Temanogrel

CAS No. 887936-68-7

Temanogrel( APD791 )

Catalog No. M24910 CAS No. 887936-68-7

Temanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Temanogrel
  • Note
    Research use only, not for human use.
  • Brief Description
    Temanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).
  • Description
    Temanogrel is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM). (In Vitro):Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50 of 13±7 nM.(In Vivo):There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment.
  • In Vitro
    Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM. Temanogrel inhibits inositol phosphate accumulation with an IC50 of 5.2 nM. Temanogrel exhibits potent inhibition of serotonin mediated amplification of ADP-stimulated human and dog platelet aggregation (IC50=8.7 and 23.1 nM, respectively). Pretreatment of aortic rings with Temanogrel prevents the vasoconstriction caused by 20 μM 5-HT in a concentration-dependent manner. Preincubation with Temanogrel also significantly inhibits the 5-HT-stimulated DNA synthesis with an IC50 of 13±7 nM.
  • In Vivo
    There are no differences in heart rate or mean arterial pressure between saline-treated and Temanogrel-treated groups at any time during the experiment (that is, for mean arterial pressure, P=0.508 between groups, and P=0.540 for group-time interaction). In dogs assigned to receive Temanogrel, plasma Temanogrel levels show a rapid and sustained increase, averaging 25.5±4.1, 28.7±4.6 and 31.2±4.5 ng/mL, respectively, at 10 min, 1.25 h and 2.25 h after the start of treatment.
  • Synonyms
    APD791
  • Pathway
    Endocrinology/Hormones
  • Target
    5-HT Receptor
  • Recptor
    5-HT2A
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    887936-68-7
  • Formula Weight
    436.5
  • Molecular Formula
    C24H28N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:125 mg/mL (286.37 mM; Need ultrasonic)
  • SMILES
    Cn1nccc1-c(cc(cc1)NC(c2cc(OC)ccc2)=O)c1OCCN1CCOCC1
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1.Xiong Y, et al. Discovery and structure-activity relationship of 3-methoxy-N-(3-(1-methyl-1H-pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): a highly selective 5-hydroxytryptamine2A receptor inverse agonist for the treatment of arterial thrombosis. J Med Chem. 2010 Jun 10;53(11):4412-21.
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