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SB-612111 hydrochloride

CAS No. 371980-94-8

SB-612111 hydrochloride( SB 612111 | SB612111 )

Catalog No. M14285 CAS No. 371980-94-8

A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    SB-612111 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM.
  • Description
    A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM; displays good selectivity versus mu-(174-fold), delta-(6391-fold), and kappa (486-fold)-opioid receptors; antagonizes the antimorphine action of nociceptin (ED50= 0.69 mg/kg) with no measurable antinociceptive effects in vivo; antagonizes nociceptin-induced thermal hyperalgesia (ED50=0.62 mg/kg i.v.) in rat carrageenan inflammatory pain model.
  • In Vitro
    ——
  • In Vivo
    rel-SB-612111 hydrochloride (intravenous?injection; 0.6-10 nmol/mouse)antagonize nociceptin-induced thermal hyperalgesia in a dose-dependent manner with an ED50 of 0.62 mg/kg.rel-SB-612111 hydrochloride (intravenous?injection; 0.1-5 mg/kg) causes a significant inhibition of the carrageenan-induced reduction in paw withdrawal latencies in rat, however, untreated paw are uneffected. Animal Model:Male rats Dosage:0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 5 mg/kg Administration:Intravenous?injection; single dose Result:Had antihyperalgesic effects on carrageenan-induced rat paw.
  • Synonyms
    SB 612111 | SB612111
  • Pathway
    Endocrinology/Hormones
  • Target
    Opioid Receptor
  • Recptor
    Opioid Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    371980-94-8
  • Formula Weight
    454.86
  • Molecular Formula
    C24H29Cl2NO.HCl
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CC1=C2CCC(CC(C2=CC=C1)O)CN3CCC(CC3)C4=C(C=CC=C4Cl)Cl.Cl
  • Chemical Name
    7-[[4-(2,6-Dichlorophenyl)-1-piperidinyl]methyl]-6,7,8,9-tetrahydro-1-methyl-5H-benzocyclohepten-5-ol hydrochloride

Shipping & Storage Information

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

Reference

1. Liao YY, et al. Eur J Pharmacol. 2011 Apr 25;657(1-3):84-8. 2. Spagnolo B, et al. J Pharmacol Exp Ther. 2007 Jun;321(3):961-7. 3. Rizzi A, et al. J Pharmacol Exp Ther. 2007 Jun;321(3):968-74. 4. Zaratin PF, et al. J Pharmacol Exp Ther. 2004 Feb;308(2):454-61.
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