PF-6870961 hydrochloride

Modify Date: 2024-09-08 19:53:38

PF-6870961 hydrochloride Structure
PF-6870961 hydrochloride structure
Common Name PF-6870961 hydrochloride
CAS Number 2857112-07-1 Molecular Weight 565.13
Density N/A Boiling Point N/A
Molecular Formula C29H33ClN6O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-6870961 hydrochloride


PF-6870961 hydrochloride 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 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].

 Names

Name PF-6870961 hydrochloride

 PF-6870961 hydrochloride Biological Activity

Description PF-6870961 hydrochloride 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 hydrochloride inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 hydrochloride also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].
Related Catalog
In Vivo PF-6870961 hydrochloride (40 mg/kg;腹腔注射) 抑制饱食和禁食大鼠的食物摄入[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 C29H33ClN6O2S
Molecular Weight 565.13