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Products Details
Product 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].
Web ID
– HY-153095A
Shipping
– Room temperature
Molecular Formula
– C29H33ClN6O2S
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.
CAS Number
– 2857112-07-1
Molecular Weight
– 565.13
SMILES
– CC1=CN(C(S1)=N2)C=C2CC(N3CCC4(CC3)CN([C@H]5C6=CC=C(C7=NC(O)=NC(C)=C7)C=C6CC5)C4)=O.[H]Cl
Clinical Information
– No Development Reported
Research Area
– Metabolic Disease
Solubility
– 10 mM in DMSO
Target
– GHSR
Pathway
– GPCR/G Protein
Product type
– Reference compound
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