PF-6870961

Names

[ Name ]:
PF-6870961

Biological Activity

[Description]:

PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].

[Related Catalog]:

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> GHSR

[In Vivo]

PF-6870961 (40 mg/kg; i.p.) suppresses food intake in both satiated and fasted rats[1]. Animal Model: Satiated and fasted rats model[1] Dosage: 2.5 mg/kg, 10 mg/kg, and 40 mg/kg Administration: Intraperitoneal injection Result: Significantly reduced food intake at 40 mg/kg.

[References]

[1]. Deschaine SL, et al. Initial pharmacological characterization of a major hydroxy metabolite of PF-5190457: inverse agonist activity of PF-6870961 at the ghrelin receptor. J Pharmacol Exp Ther. 2023 Jan 11:JPET-AR-2022-001393.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₂N₆O₂S

[ Molecular Weight ]:
528.67

PF-6870961

Names

Biological Activity

Chemical & Physical Properties

Related Compounds