Cart
sales@molnova.com
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
Size Price / USD Stock Quantity
2MG 40 In Stock
5MG 65 In Stock
10MG 115 In Stock
25MG 260 In Stock
100MG Get Quote In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock
Get Quotation Bulk Inquiry Add to Cart

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.
Calculator

Molecular Weight Calculator

Dilution Calculator

Molarity Calculator

molnova catalog
related products

  • ONC212

    ONC212 a fluorinated-ONC201 analogue is a selective agonist of GPR132.

  • Livoletide

    A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

  • Ibutamoren mesylate

    A non-peptidic, poten and selective, orally-active agonist of the ghrelin receptor (GHSR) with EC50 of 1.3 nM (releases GH from rat pituitary cells).

Sign In Join Free