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APD-371

CAS No. 1268881-20-4

APD-371( Olorinab | APD371 | APD 371 )

Catalog No. M11128 CAS No. 1268881-20-4

APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    APD-371
  • Note
    Research use only, not for human use.
  • Brief Description
    APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM).
  • Description
    APD-371 (APD371, Olorinab) is a potent, selective and orally available CB2 agonist with EC50 of 6.2 nM; displays no activity against CB1 receptors (EC50>10 uM); exhibits activity in rat model of osteoarthritis pain.Pain Phase 2 Clinical.
  • In Vitro
    A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed, and that Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Furthermore, Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling.
  • In Vivo
    Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. Seperately, the analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors.
  • Synonyms
    Olorinab | APD371 | APD 371
  • Pathway
    GPCR/G Protein
  • Target
    Cannabinoid Receptor
  • Recptor
    Cannabinoid Receptor
  • Research Area
    Neurological Disease
  • Indication
    Pain

Chemical Information

  • CAS Number
    1268881-20-4
  • Formula Weight
    357.414
  • Molecular Formula
    C18H23N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 200 mg/mL (559.58 mM)
  • SMILES
    O=C(C1=NN(C2=C[N+]([O-])=CC=N2)C3=C1C[C@@]4([H])[C@]3([H])C4)N[C@H](CO)C(C)(C)C
  • Chemical Name
    3-((4aS,5aS)-3-(((S)-1-hydroxy-3,3-dimethylbutan-2-yl)carbamoyl)-4,4a,5,5a-tetrahydro-1H-cyclopropa[4,5]cyclopenta[1,2-c]pyrazol-1-yl)pyrazine 1-oxide

Shipping & Storage Information

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

Reference

1. Sangdon Han, et al. ACS Med. Chem. Lett., 2017, 8 (12), pp 1309-1313.
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