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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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 |
|
|
Solubility |
10 mM in DMSO |
1. Lees JA, et al. Nat Commun. 2023 Sep 23;14(1):5938.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright