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GPR61 inverse agonist compound 1

Chemical Structure : GPR61 inverse agonist compound 1

CAS No.:

GPR61 inverse agonist compound 1

Catalog No.: PC-21214Not For Human Use, Lab Use Only.

GPR61 inverse agonist compound 1 is a potent and selective GPR61 inverse agonist with functional IC50 of 10-11 nM in cAMP assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GPR61 inverse agonist compound 1 is a potent and selective GPR61 inverse agonist with functional IC50 of 10-11 nM in cAMP assays.
Compound 1 is selective for GPR61 among a panel of GPCRs (off-target IC50 values >10 μM), with an excellent in vitro off-target profile.
Compound 1 binds an induced allosteric site that overlaps the binding site for Gαs and unexpectedly promotes a GPR61 conformation more similar to its active state than the inactive state.
Compound 1 is selective for GPR61 in a panel of common off-target GPCRs and against related receptors GPR62 and GPR101.
Compound 1 shows high potency and excellent off-target profile, Compound 1 is a high-quality tool compound for functional studies of GPR61.

Physicochemical Properties

M.Wt 524.54
Formula C22H26F2N6O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(((3,5-difluoropyridin-4-yl)methyl)amino)-N-(4-ethoxy-6-methylpyrimidin-2-yl)-2-methoxy-N-(2-methoxyethyl)pyridine-3-sulfonamide

References

1. Lees JA, et al. Nat Commun. 2023 Sep 23;14(1):5938.

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