L-755,507

L-755,507 is a partial agonist of β₃-adrenergic receptors (EC₅₀ = 0.43 nM).¹ It displays more than 440-fold selectivity for β₃- over β₁- and β₂-adrenoceptors (EC₅₀s = 580 and >10,000 nM, respectively).¹ At 5 µM, this compound has been used to enhance CRISPR-mediated homology-directed repair efficiency by 3-fold for large fragment insertions and by 9-fold for point mutations.² L-755,507 has been used to identify signaling pathways activated through β₃-adrenergic receptors.³

WARNING This product is not for human or veterinary use.

1. Parmee, E.R., Ok, H.O., Candelore, M.R., et al. Discovery of L-755,507: A subnanomolar humanβ3 adrenergic receptor agonist. Bioorg. Med. Chem. Lett. 8(9), 1107-1112 (1998).

2. Yu, C., Liu, Y., Ma, T., et al. Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell Stem Cell 16(2), 142-147 (2015).

3. Sato, M., Hutchinson, D.S., Evans, B.A., et al. The β3-adrenoceptor agonist 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-phenyl]-benzenesulfonamide (L755507) and antagonist (S)-N-[4-[2-[[3-[3-(acetamidomethyl)phenoxy]-2-hydroxypropyl]amino]-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K₁ cells stably expressing the human β3-adrenoceptor. Mol. Pharmacol. 74(5), 1417-1428 (2008).