PF-5190457

For research use only. Not for therapeutic Use.

  • CAT Number: I008714
  • CAS Number: 1334782-79-4
  • Molecular Formula: C29H32N6OS
  • Molecular Weight: 512.676
  • Purity: ≥95%
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PF-5190457 (CAT: I008714) is an orally available and potent ghrelin receptor inverse agonist. It exhibits high selectivity for the ghrelin receptor and acts as an antagonist, effectively blocking the activity of ghrelin, a hormone involved in appetite regulation and energy balance. By inhibiting ghrelin signaling, PF-5190457 has the potential to modulate metabolic processes and has shown promising effects in increasing insulin secretion in glucose-stimulated human islets. The compound has also demonstrated favorable pharmacological and safety profiles, leading to its advancement into human clinical trials. PF-5190457 represents a promising candidate for the treatment of metabolic disorders and further research in this area.


Catalog Number I008714
CAS Number 1334782-79-4
Synonyms

PF-5190457; PF 5190457; PF5190457; PF-05190457; PF05190457; PF 05190457.;(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

Molecular Formula C29H32N6OS
Purity ≥95%
Target GHSR
Solubility Soluble in DMSO, not in water
Storage 0 - 4 °C for short term, or -20 °C for long term
IUPAC Name 2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-[2-[(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]nonan-7-yl]ethanone
InChI InChI=1S/C29H32N6OS/c1-19-11-25(31-18-30-19)22-3-5-24-21(12-22)4-6-26(24)35-16-29(17-35)7-9-33(10-8-29)27(36)13-23-15-34-14-20(2)37-28(34)32-23/h3,5,11-12,14-15,18,26H,4,6-10,13,16-17H2,1-2H3/t26-/m1/s1
InChIKey ZIUDADZJCKGWKR-AREMUKBSSA-N
SMILES CC1=NC=NC(=C1)C2=CC3=C(C=C2)C(CC3)N4CC5(C4)CCN(CC5)C(=O)CC6=CN7C=C(SC7=N6)C
Reference

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1:Development and validation of an UPLC-MS/MS assay for quantitative analysis of the ghrelin receptor inverse agonist PF-5190457 in human or rat plasma and rat brain. Ghareeb M, Leggio L, El-Kattan A, Akhlaghi F.Anal Bioanal Chem. 2015 Jul;407(19):5603-13. doi: 10.1007/s00216-015-8730-2. Epub 2015 May 7. PMID: 25943263 Free PMC Article<br />
2:Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8. PMID: 24900864 Free PMC Article

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