| Description | CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM. |
| In vitro | CCR7 Ligand 1 (CCR7-Cmp2105) binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8[1]. CCR7 Ligand 1 allosterically inhibits binding of the native chemokine CCL19 ligand in scintillation proximity assays (bottom) with an IC50 of 35 nM[1]. CCR7 Ligand 1 (20, 40, 60, 80, 100 μM) has dose-dependent thermo-stabilizing effect on CCR7[1]. |
| Target activity | CCR7 (human):3 nM (kd) |
| Synonyms | CCR7-Cmp2105 |
| molecular weight | 475.56 |
| Molecular formula | C22H29N5O5S |
| CAS | 681514-83-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 12.5 mg/mL (26.28 mM), Sonication is recommended. |
| References | 1. Jaeger K, et al. Structural Basis for Allosteric Ligand Recognition in the Human CC Chemokine Receptor 7. Cell. 2019 Aug 22;178(5):1222-1230.e10. |