K41498 TFA

K41498 (incubated at 22°C for 120 min) TFA exhibits highly selective and high-affinity binding to hCRF₂α and hCRF₂β receptors in membrane homogenates of stably transfected HEK293 cells (K_i = 0.66 nM and 0.62 nM, respectively), which is significantly superior to its binding to hCRF₁ receptor^[1].
K41498 (10 μM in hCRF₁-expressing cells; 100 nM in hCRF₂α- and hCRF₂β-expressing cells; treated at 37°C for 10 min) TFA is a potent, selective antagonist that inhibits cAMP accumulation in Svg-stimulated HEK293 cells expressing hCRF₂α and hCRF₂β. It exhibits only extremely low intrinsic agonist activity across all three receptor subtypes and shows weak activity at the hCRF₁ receptor^[1].
K41498 (100 nM, 10 min at 37°C for CRF₂α/CRF₂β cells; 10 μM, 10 min at 37°C for CRF₁ cells) TFA potently inhibits sauvagine-induced cAMP accumulation in HEK293 cells expressing human CRF₂α and human CRF₂β at a concentration of 100 nM, shows only weak inhibitory effect on HEK293 cells expressing human CRF₁ at a concentration of 10 μM, and exhibits only extremely low intrinsic agonist activity in all three of the above-mentioned cell lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.