CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a K d of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC 50 of 7.3 μM.
性状
Solid
IC50 & Target[1][2]
Human CCR7 3 nM (Kd)
体外研究(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. CCR7 Ligand 1 allosterically inhibits binding of the native chemokine CCL19 ligand in scintillation proximity assays (bottom) with an IC50 of 35 nM. CCR7 Ligand 1 (20, 40, 60, 80, 100 μM) has dose-dependent thermo-stabilizing effect on CCR7. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (210.28 mM; Need ultrasonic)配制储备液