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PF-6870961

CAT: 0804-HY-153095Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-153095Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
CAS Number
2857112-06-0
UNSPSC
12352005
Target
GHSR
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/pf-6870961.html
Solubility
10 mM in DMSO
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
Molecular Formula
C29H32N6O2S
Molecular Weight
528.67
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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