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Chemical Structure : 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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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.
| M.Wt | 524.54 | |
| Formula | C22H26F2N6O5S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Lees JA, et al. Nat Commun. 2023 Sep 23;14(1):5938.
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