(-)-CGP-12177, [5,7-³H]-, 250µCi (9.25MBq)

(-)-CGP-12177 is a high affinity antagonist of both β1- and β2-adrenoceptors, and functions as a partial agonist at β3-adrenoceptors. These receptors are part of a group of beta adrenergic G-protein coupled receptors (GPCRs) found in adipose tissue, heart tissue, and vascular smooth muscle tissue that play a role in cardiac output, hormone release, smooth muscle relaxation, and lipolysis. Beta adrenergic receptors have been identified as potential drug targets for congestive heart failure, hypertension, asthma, COPD, and neoplasia.

We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (B_max), dissociation constants (K_d), association and dissociation rates (k_on and k_off), and inhibitor constants (K_i) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.

Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, Revvity has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET1061:

1. Mark Soave, Gabriella Cseke, Catherine J. Hutchings, Alastair J.H. Brown, Jeanette Woolard, Stephen J. Hill, A monoclonal antibody raised against a thermo-stabilised β1-adrenoceptor interacts with extracellular loop 2 and acts as a negative allosteric modulator of a sub-set of β1-adrenoceptors expressed in stable cell lines, In Biochemical Pharmacology, Volume 147, 2018, Pages 38-54.
2. Jan-Peter van Wieringen, Martina B. Michel-Reher, Toshiki Hatanaka, Koji Ueshima, Martin C. Michel, The new radioligand [3H]-L 748,337 differentially labels human and rat β3-adrenoceptors, In European Journal of Pharmacology, Volume 720, Issues 1–3, 2013, Pages 124-130.
3. Violaine Simon, Marie-Thérèse Robin, Chantal Legrand, Joëlle Cohen-Tannoudji; Endogenous G Protein-Coupled Receptor Kinase 6 Triggers Homologous β-Adrenergic Receptor Desensitization in Primary Uterine Smooth Muscle Cells, Endocrinology, Volume 144, Issue 7, 1 July 2003, Pages 3058–3066.