PF-6870961

Modify Date: 2024-04-09 15:39:12

PF-6870961 Structure
PF-6870961 structure
Common Name PF-6870961
CAS Number 2857112-06-0 Molecular Weight 528.67
Density N/A Boiling Point N/A
Molecular Formula C29H32N6O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-6870961


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].

 Names

Name PF-6870961

 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
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