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Home - Products - GPCR/G Protein - GHSR - PF-05190457

PF-05190457

CAS No. 1334782-79-4

PF-05190457( PF05190457 | PF 5190457 | PF5190457 )

Catalog No. M11337 CAS No. 1334782-79-4

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36; displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    PF-05190457
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36; displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM).
  • Description
    A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36; displays excellent off-target activity in the CEREP panel at 10 uM with exception of serotonin 5-HT2B (IC50=3.7 uM); demonstrates robust increases in glucose-stimulated insulin secretion in human islets.Alcoholism Phase 2 Clinical.
  • In Vitro
    PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity.
  • In Vivo
    PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets.
  • Synonyms
    PF05190457 | PF 5190457 | PF5190457
  • Pathway
    GPCR/G Protein
  • Target
    GHSR
  • Recptor
    GHSR
  • Research Area
    Neurological Disease
  • Indication
    Alcoholism

Chemical Information

  • CAS Number
    1334782-79-4
  • Formula Weight
    512.676
  • Molecular Formula
    C29H32N6OS
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (487.64 mM)
  • SMILES
    CC1=CC(C2=CC3=C([C@H](N4CC5(CCN(C(CC(N=C6S7)=CN6C=C7C)=O)CC5)C4)CC3)C=C2)=NC=N1
  • Chemical Name
    (R)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-1-(2-(5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonan-7-yl)ethan-1-one

Shipping & Storage Information

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

Reference

1. Bhattacharya SK, et al. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. 2. Kong J, et al. Br J Pharmacol. 2016 May;173(9):1452-64. 3. Denney WS, et al. Br J Clin Pharmacol. 2017 Feb;83(2):326-338.
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