K41498 TFA

K41498 TFA, an analog of antisauvagine-30 (aSvg-30), is a potent and highly selective antagonist of CRF2 receptors, exhibiting K i values of 0.66 nM, 0.62 nM, and 425 nM for human CRF 2α, CRF 2β, and CRF 1 receptors, respectively. This compound effectively inhibits sauvagine-stimulated cAMP accumulation in cells expressing hCRF 2α and hCRF 2β. It is utilized in studies investigating hypotension [1].

K41498 acetate, an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 acetate is a potent and highly selective antagonist CRF2 receptor with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively.

K-(D-1-Nal)-FwLL-NH2 TFA is a potent and high-affinity inverse agonist of the ghrelin receptor, exhibiting Ki values of 4.9 nM in COS7 cells and 31 nM in HEK293T cells. This compound effectively inhibits ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.

K 41498 is a selective peptide antagonist targeting both corticotropin-releasing factor receptor 2α (CRF2α) and CRF2β, demonstrating high affinity with Kis of 0.66 and 0.62 nM, respectively, in HEK293 cells expressing these human receptors. Its selectivity is evident as it exhibits a significantly reduced affinity for CRF1 receptor (Ki = 425 nM in HEK293 cells expressing the human CRF1 receptor). Additionally, K 41498, when administered intravenously at 1.84 µg/animal, effectively mitigates urocortin-induced hypotension in rats. Furthermore, its intrathecal delivery ranging from 0.075 to 0.5 µmol/animal significantly lowers the mechanical paw withdrawal threshold in a rat model, indicating its potential utility in managing nociception triggered by complete Freund's adjuvant.