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
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M.Wt
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524.54
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Formula
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C22H26F2N6O5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-(((3,5-difluoropyridin-4-yl)methyl)amino)-N-(4-ethoxy-6-methylpyrimidin-2-yl)-2-methoxy-N-(2-methoxyethyl)pyridine-3-sulfonamide
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References
1. Lees JA, et al. Nat Commun. 2023 Sep 23;14(1):5938.
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